Antibodies
Rimonabant
- 貨號 Cat. No.
- S3021
- 規格 Size
- 10mM/1mL~100mg
- 品牌 Brand
- Selleckchem
Description
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h1 itemprop=name style=margin: 0px 20px 0px 0px; padding: 0px; font-size: 24px; float: left;Rimonabant/h1
div class=product_c_title style=margin: 0px 20px 0px 0px; padding: 0px; height: 25px; font-size: 12px; float: left;span class=p_title style=margin: 0px 15px 0px 0px; padding: 0px; float: left;Catalog No.S3021/span/div
p class=new_title style=margin: 5px 0px 10px; padding: 0px; clear: both; font-size: 11px; line-height: 14.399999618530273px;Rimonabant is a selective antagonist ofnbsp;b style=margin: 0px; padding: 0px;CB1/bnbsp;withnbsp;b style=margin: 0px; padding: 0px;IC50/bnbsp;of 13.6 nM andnbsp;b style=margin: 0px; padding: 0px;EC50/bnbsp;of 17.3 nM in hCB1 transfected HEK 293 membrane./p
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td width=139 style=margin: 0px; padding: 3px 8px;label style=margin: 0px; padding: 0px;10mM/1mL/labelspan class=in_bg style=margin: 0px 0px 0px 4px; padding: 0px 3px; background-color: rgb(255, 120, 0); color: rgb(255, 255, 255); font-size: 11px; background-position: initial initial; background-repeat: initial initial;In DMSO/span/td
td width=80 style=margin: 0px; padding: 3px 8px;USD 151/td
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td width=80 style=margin: 0px; padding: 3px 8px;USD 113/td
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td width=139 style=margin: 0px; padding: 3px 8px;label style=margin: 0px; padding: 0px;25mg/label/td
td width=80 style=margin: 0px; padding: 3px 8px;USD 214/td
td width=62 style=margin: 0px; padding: 3px 8px;In stock/td
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td width=80 style=margin: 0px; padding: 3px 8px;USD 340/td
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h3 id=biologicalActivity style=margin: 25px 0px 0px; padding: 0px; height: 25px; font-size: 14px; font-family: Arial, Tahoma, Helvetica; line-height: 19.200000762939453px;Biological Activity/h3
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th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Description/th
td colspan=6 style=margin: 0px; padding: 5px 15px; text-align: justify; border-style: solid; border-color: rgb(229, 229, 229);Rimonabant is a selective antagonist ofnbsp;b style=margin: 0px; padding: 0px;CB1/bnbsp;withnbsp;b style=margin: 0px; padding: 0px;IC50/bnbsp;of 13.6 nM andnbsp;b style=margin: 0px; padding: 0px;EC50/bnbsp;of 17.3 nM in hCB1 transfected HEK 293 membrane./td
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th style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Targets/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);hCB1/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);hCB2/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Acuyl coenzyme A:cholesterol acyltransferase (ACAT/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);nbsp;/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);nbsp;/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);nbsp;/td
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th style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);IC50/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);13.6 nM/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);1.64 mu;Mnbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/rimonabant-sr141716.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[1]/a/span/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);1.5-2.9 mu;Mnbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/rimonabant-sr141716.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[2]/a/span/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);nbsp;/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);nbsp;/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);nbsp;/td
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th style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);i style=margin: 0px; padding: 0px;In vitro/i/th
td colspan=6 style=margin: 0px; padding: 5px 15px; text-align: justify; border-style: solid; border-color: rgb(229, 229, 229);Rimonabant dose-dependently reduces ACAT activity in Raw264.7macrophages with IC50 of 2.9 mu;M and isolated peritoneal macrophages. Rimonabant inhibits ACATactivity in intact CHO-ACAT1 and CHO-ACAT2 cells and in cell-free assays with approximately equal efficiency with IC50 of 1.5 mu;M and 2.2 mu;M for CHO-ACAT1 and CHO-ACAT2, respectively. Consistent with ACAT inhibition, Rimonabant treatment blocks ACAT dependent processes in macrophages, oxysterol-induced apoptosis and acetylated-LDL induced foam cell formation.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/rimonabant-sr141716.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[2]/a/spanRimonabant antagonizes the inhibitory effects of cannabinoid receptor agonists on both mouse vas deferens contractions and adenylyl cyclase activity in rat brain membranes in a concentration-dependent manner.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/rimonabant-sr141716.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[3]/a/spanRimonabant significantly reduces cell growth and induces cell death of human colorectal cancer cells (DLD-1, CaCo-2 and SW620). Rimonabant is able to alter cell cycle distribution in all the cell lines tested. Particularly, Rimonabant produces a G2/M cell cycle arrest in DLD-1 cells without inducing apoptosis or necrosis.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/rimonabant-sr141716.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[4]/a/span/td
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th style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);i style=margin: 0px; padding: 0px;In vivo/i/th
td colspan=6 style=margin: 0px; padding: 5px 15px; text-align: justify; border-style: solid; border-color: rgb(229, 229, 229);Rimonabant is administered intraperitoneally or orally potently and dose-dependently antagonize classical pharmacological and behavioural effectos of cannabinoid receptor agonists.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/rimonabant-sr141716.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[3]/a/spannbsp;In the mouse model of azoxymethane-induced colon carcinogenesis, Rimonabant significantly decreased aberrant crypt foci (ACF) formation, which precedes colorectal cancer.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/rimonabant-sr141716.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[4]/a/spannbsp;Rimonabant (10 mg/kg by gavage) is fed for 2 weeks to 3-month-old male obese Zucker rats as an impaired glucose tolerance model and for 10 weeks to 6-month-old male obese Zucker rats as a model of the metabolic syndrome. RANTES (Regulated upon Activation, Normal T cell Expressed, and Secreted) and MCP-1 (monocyte chemotactic protein-1) serum levels are increased in obese vs lean Zucker rats and significantly reduced by long-term treatment with Rimonabant, which slowes weight gain in rats with the metabolic syndrome. Neutrophils and monocytes are significantly increased in young and old obese vs lean Zucker rats and lowered by Rimonabant. Platelet-bound fibrinogen is significantly enhanced in obese vs lean Zucker rats of both age, and is reduced by Rimonabant. Platelets from obese rats are more sensitive to thrombin-induced aggregation and adhesion to fibrinogen, which are both attenuated by Rimonabant therapy.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/rimonabant-sr141716.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[5]/a/span/td
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th style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Features/th
td colspan=6 style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Efficacious to induce weight reduction and improvements in cardiometabolic risk factors, however was withdrawn in 2009 due to severe depressive disorder and anxiety./td
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h3 id=protocol style=margin: 25px 0px 0px; padding: 0px; height: 25px; font-size: 14px; font-family: Arial, Tahoma, Helvetica; line-height: 19.200000762939453px;Protocolspan style=margin: 0px; padding: 0px; font-weight: normal;(Only for Reference)/span/h3
h4 style=margin: 0px; padding: 0px; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;Kinase Assay:nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/rimonabant-sr141716.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[1]/a/span/h4
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th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Radioligand Binding Assay/th
td style=margin: 0px; padding: 5px 15px; text-align: justify; border-style: solid; border-color: rgb(229, 229, 229);Human CB1 and CB2 stably transfect HEK 293 cells and cell membrane is purified. 0.2-8 mu;g of the purified membrane is incubated with 0.75 nM [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH] CP55,940 and Rimonabant in the incubation buffer (50 mM Tris-HCl, 5 mM MgClspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;2/span, 1 mM EDTA, 0.3%BSA, pH 7.4). The non-specific binding is defined in the presence of 1 mu;M of CP55,940. The reactions are incubated for one and a half hours at 30 deg;C in Multiscreen. The reactions are terminated by manifold filtration and washed four times with ice-cold wash buffer (50mM Tris, pH 7.4, 0.25% BSA).The radioactivity bound to the filters is measured by Topcount. The IC50 is determined as the concentration of Rimonabant required to inhibit 50% of the binding of [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH] CP55,940 and calculated by non-linear regression./td
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th style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Eu-GTP Binding Assay/th
td style=margin: 0px; padding: 5px 15px; text-align: justify; border-style: solid; border-color: rgb(229, 229, 229);The Eu-GTP binding assay is performed using the DELFIA Eu-GTP binding kit based on methods developed by Frang et al., with minor modifications as described in the following: 1-4 mu;g of purified membrane is incubated with Rimonabant and 20 nM CP55,940 in the assay buffer (50 mM HEPES, pH 7.4, 100 mM NaCl, 100 mu;g/mL saponin, 5 mMMgClspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;2/span, 2 mu;M GDP, 0.5% BSA) at 30 deg;C for 60 minutes in acroplates. Following the addition of Eu-GTP and incubation for 30 minutes at 30 deg;C, the assay is terminated by washing four times with the washing buffer provided in the kit. The fluorescence signal of the Eu-GTP is determined with a Victor 2 multilabel reader. The EC50 of Rimonabant at inhibiting 50% of the CP55,940-stimulated Eu-GTP binding is determined from the dose-response curves using non-linear regression.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/rimonabant-sr141716.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[2]/a/span/td
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h4 style=margin: 0px; padding: 0px; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;Cell Assay:nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/rimonabant-sr141716.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[2]/a/span/h4
table width=100% border=0 cellspacing=0 cellpadding=0 class=product_show_table style=margin: 0px; padding: 0px; border-collapse: collapse; border-spacing: 0px; border-style: solid; border-color: rgb(229, 229, 229); color: rgb(0, 0, 0); font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;
tbody style=margin: 0px; padding: 0px;
tr style=margin: 0px; padding: 0px;
th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Cell lines/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Raw 264.7 cells/td
/tr
tr style=margin: 0px; padding: 0px;
th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Concentrations/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);0,1,4 mu;M/td
/tr
tr style=margin: 0px; padding: 0px;
th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Incubation Time/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);17 hours/td
/tr
tr style=margin: 0px; padding: 0px;
th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Method/th
td style=margin: 0px; padding: 5px 15px; text-align: justify; border-style: solid; border-color: rgb(229, 229, 229);Raw 264.7 cells (2 times; 10span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;6/spannbsp;/well) in 12-well plates are rinsed with PBS and refed culture media supplemented with varying amounts of Rimonabant 1 hour prior to supplementation with 7-ketocholesterol (7KC). All wells are adjusted to receive equal amounts of vehicle. Following 16-hour incubation, caspase-3 and caspase 3-like activity are determined using a fluorogenic substrate (Ac-DEVD-AFC) and a spectrofluorometer equipped with a microplate reader./td
/tr
/tbody
/table
h4 style=margin: 0px; padding: 0px; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;Animal Study:nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/rimonabant-sr141716.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[3]/a/span/h4
table width=100% border=0 cellspacing=0 cellpadding=0 class=product_show_table style=margin: 0px; padding: 0px; border-collapse: collapse; border-spacing: 0px; border-style: solid; border-color: rgb(229, 229, 229); color: rgb(0, 0, 0); font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;
tbody style=margin: 0px; padding: 0px;
tr style=margin: 0px; padding: 0px;
th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Animal Models/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Male mice and male rats/td
/tr
tr style=margin: 0px; padding: 0px;
th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Formulation/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Rimonabant is dissolved in two drops of Tween 80, diluted in distilled water./td
/tr
tr style=margin: 0px; padding: 0px;
th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Dosages/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);20 ml/kg (mice) and 5 ml/kg (rats)/td
/tr
tr style=margin: 0px; padding: 0px;
th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Administration/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Rimonabant is administered i.p. (30 minutes) or p.o. (1hour) before the i.v. injection of WIN55212-2./td
/tr
tr style=margin: 0px; padding: 0px;
th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Solubility/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);30% PEG400/0.5% Tween80/5% propylene glycol, 30 mg/mL/td
/tr
tr style=margin: 0px; padding: 0px;
td colspan=4 style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);span class=red style=margin: 0px; padding: 0px; color: rgb(255, 0, 0);*/spannbsp;Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations./td
/tr
/tbody
/table
pa id=s_ref style=margin: 0px; padding: 0px; color: rgb(52, 84, 140); cursor: pointer; font-family: Arial, Tahoma, Helvetica; line-height: 19.200000762939453px; clear: both; float: left; height: 0px; font-size: 0px;1/a/p
h4 class=reference margin_t style=margin: 10px 0px 0px; padding: 0px; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;References/h4
h3 id=chemicalInformation style=margin: 25px 0px 0px; padding: 0px; height: 25px; font-size: 14px; font-family: Arial, Tahoma, Helvetica; line-height: 19.200000762939453px;Chemical Information/h3
pa href=http://file.selleckchem.com/downloads/product-sdf/rimonabant-sr141716-s3021.SDF style=margin: -25px 0px 0px 180px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px; float: left;Download Rimonabant SDF/a/p
div class=clear-both style=margin: 0px; padding: 0px; clear: both; height: 0px; overflow: hidden; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;nbsp;/div
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table width=100% border=0 cellspacing=0 cellpadding=0 class=show_tab01 fl style=margin: 0px 0px 10px; padding: 0px; border-collapse: collapse; border-spacing: 0px; width: 375px; float: left;
tbody style=margin: 0px; padding: 0px;
tr style=margin: 0px; padding: 0px;
th width=45% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Molecular Weight (MW)/th
td width=55% style=margin: 0px; padding: 5px 0px 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);463.79/td
/tr
tr style=margin: 0px; padding: 0px;
th width=45% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Formula/th
td style=margin: 0px; padding: 5px 0px 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);
p style=margin: 0px; padding: 0px;Cspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;22/spanHspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;21/spanClspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;3/spanNspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;4/spanO/p
/td
/tr
tr style=margin: 0px; padding: 0px;
th width=45% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);CAS No./th
td style=margin: 0px; padding: 5px 0px 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);168273-06-1/td
/tr
/tbody
/table
table width=100% border=0 cellspacing=0 cellpadding=0 class=show_tab fr style=margin: 0px 0px 10px; padding: 0px; border-collapse: collapse; border-spacing: 0px; width: 375px; float: right;
tbody style=margin: 0px; padding: 0px;
tr style=margin: 0px; padding: 0px;
th rowspan=2 valign=top class=padding5 style=margin: 0px; padding: 5px 0px 5px 10px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Storage/th
td class=padding5 style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);3 yearsnbsp;span class=margin_l style=margin: 0px 0px 0px 10px; padding: 0px;-20℃/spanspan class=margin_l style=margin: 0px 0px 0px 10px; padding: 0px;Powder/span/td
/tr
tr style=margin: 0px; padding: 0px;
td class=padding5 style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);6 monthsspan class=margin_l style=margin: 0px 0px 0px 10px; padding: 0px;-80℃/spanspan class=margin_l style=margin: 0px 0px 0px 10px; padding: 0px;in DMSO/span/td
/tr
tr style=margin: 0px; padding: 0px;
th width=161 valign=top class=padding5 style=margin: 0px; padding: 5px 0px 5px 10px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Syonnyms/th
td width=214 class=padding5 style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);SR141716/td
/tr
/tbody
/table
div class=clear-both style=margin: 0px; padding: 0px; clear: both; height: 0px; overflow: hidden;nbsp;/div
table width=100% border=0 cellspacing=0 cellpadding=0 class=product_show_table mb15 style=margin: 0px 0px 15px; padding: 0px; border-collapse: collapse; border-spacing: 0px; border-style: solid; border-color: rgb(229, 229, 229);
tbody style=margin: 0px; padding: 0px;
tr style=margin: 0px; padding: 0px;
th width=12% rowspan=4 style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);strong style=margin: 0px; padding: 0px;Solubility (25deg;C)nbsp;/strongspan class=red style=margin: 0px; padding: 0px; color: rgb(255, 0, 0);*/span/th
td width=10% rowspan=3 class=italic style=margin: 0px; padding: 5px 15px; font-style: italic; border-style: solid; border-color: rgb(229, 229, 229);In vitro/td
td width=50% style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);DMSO/td
td width=28% style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);25 mg/mL (53 mM)/td
/tr
tr style=margin: 0px; padding: 0px;
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Water/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);lt;1 mg/mL (lt;1 mM)/td
/tr
tr style=margin: 0px; padding: 0px;
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Ethanol/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);2 mg/mL (4 mM)/td
/tr
tr style=margin: 0px; padding: 0px;
td class=italic style=margin: 0px; padding: 5px 15px; font-style: italic; border-style: solid; border-color: rgb(229, 229, 229);In vivo/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);30% PEG400/0.5% Tween80/5% propylene glycol,/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);30 mg/mL/td
/tr
tr style=margin: 0px; padding: 0px;
td colspan=4 style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);span class=red style=margin: 0px; padding: 0px; color: rgb(255, 0, 0);*/spannbsp;lt;1 mg/ml means slightly soluble or insoluble.br style=margin: 0px; padding: 0px; /
span class=red style=margin: 0px; padding: 0px; color: rgb(255, 0, 0);*/spannbsp;Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations./td
/tr
/tbody
/table
/div
div style=margin: 0px; padding: 0px; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px; height: 10px;nbsp;/div
table width=100% border=0 cellspacing=0 cellpadding=0 class=product_show_table style=margin: 0px; padding: 0px; border-collapse: collapse; border-spacing: 0px; border-style: solid; border-color: rgb(229, 229, 229); color: rgb(0, 0, 0); font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;
tbody style=margin: 0px; padding: 0px;
tr style=margin: 0px; padding: 0px;
th width=153px style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Chemical Name/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide/td
/tr
/tbody
/table
div class=clear-both style=margin: 0px; padding: 0px; clear: both; height: 0px; overflow: hidden; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;nbsp;/div
h3 id=chemicalInformation style=margin: 25px 0px 0px; padding: 0px; height: 25px; font-size: 14px; font-family: Arial, Tahoma, Helvetica; line-height: 19.200000762939453px;Preparing Stock Solutions/h3
table width=100% border=0 cellspacing=0 cellpadding=0 class=product_show_table style=margin: 0px; padding: 0px; border-collapse: collapse; border-spacing: 0px; border-style: solid; border-color: rgb(229, 229, 229); color: rgb(0, 0, 0); font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;
tbody style=margin: 0px; padding: 0px;
tr style=margin: 0px; padding: 0px;
th width=153px style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Stock Solution (1ml DMSO)/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);1mM/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);10mM/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);20mM/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);30mM/td
/tr
tr style=margin: 0px; padding: 0px;
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Mass(mg)/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);0.46379/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);4.6379/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);9.2758/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);13.9137/td
/tr
/tbody
/table
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pnbsp;/p
pnbsp;/p
pnbsp;/p
h1 itemprop=name style=margin: 0px 20px 0px 0px; padding: 0px; font-size: 24px; float: left;Rimonabant/h1
div class=product_c_title style=margin: 0px 20px 0px 0px; padding: 0px; height: 25px; font-size: 12px; float: left;span class=p_title style=margin: 0px 15px 0px 0px; padding: 0px; float: left;Catalog No.S3021/span/div
p class=new_title style=margin: 5px 0px 10px; padding: 0px; clear: both; font-size: 11px; line-height: 14.399999618530273px;Rimonabant is a selective antagonist ofnbsp;b style=margin: 0px; padding: 0px;CB1/bnbsp;withnbsp;b style=margin: 0px; padding: 0px;IC50/bnbsp;of 13.6 nM andnbsp;b style=margin: 0px; padding: 0px;EC50/bnbsp;of 17.3 nM in hCB1 transfected HEK 293 membrane./p
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th width=153 style=margin: 0px; padding: 0px 0px 0px 15px; line-height: 14px; font-size: 14px; border-bottom-style: solid; border-bottom-color: rgb(211, 217, 225); background-color: rgb(221, 228, 236);label style=margin: 0px; padding: 0px;Size/label/th
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th width=402 style=margin: 0px; padding: 8px; line-height: 14px; font-size: 14px; border-bottom-style: solid; border-bottom-color: rgb(211, 217, 225); background-color: rgb(221, 228, 236);nbsp;/th
/tr
tr style=margin: 0px; padding: 0px;
td colspan=4 valign=top class=pt style=margin: 0px; padding: 3px 8px;
table width=91% border=0 cellspacing=0 cellpadding=0 style=margin: 0px; padding: 0px; border-collapse: collapse; border-spacing: 0px; width: 373px;
tbody style=margin: 0px; padding: 0px;
tr style=margin: 0px; padding: 0px;
td width=139 style=margin: 0px; padding: 3px 8px;label style=margin: 0px; padding: 0px;10mM/1mL/labelspan class=in_bg style=margin: 0px 0px 0px 4px; padding: 0px 3px; background-color: rgb(255, 120, 0); color: rgb(255, 255, 255); font-size: 11px; background-position: initial initial; background-repeat: initial initial;In DMSO/span/td
td width=80 style=margin: 0px; padding: 3px 8px;USD 151/td
td width=62 style=margin: 0px; padding: 3px 8px;In stock/td
td width=61 style=margin: 0px; padding: 3px 8px;select name=cartDTOs[1].quantity style=margin: 0px; padding: 0px; border-color: rgb(171, 171, 171); width: 40px;nbsp;
option value=0 style=margin: 0px; padding: 0px;0/option
nbsp;
option value=1 style=margin: 0px; padding: 0px;1/option
nbsp;
option value=2 style=margin: 0px; padding: 0px;2/option
nbsp;
option value=3 style=margin: 0px; padding: 0px;3/option
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option value=4 style=margin: 0px; padding: 0px;4/option
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option value=5 style=margin: 0px; padding: 0px;5/option
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option value=6 style=margin: 0px; padding: 0px;6/option
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option value=7 style=margin: 0px; padding: 0px;7/option
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option value=8 style=margin: 0px; padding: 0px;8/option
nbsp;
option value=9 style=margin: 0px; padding: 0px;9/option
nbsp;
option value=10 style=margin: 0px; padding: 0px;10/option
nbsp;/select/td
/tr
tr style=margin: 0px; padding: 0px;
td width=139 style=margin: 0px; padding: 3px 8px;label style=margin: 0px; padding: 0px;10mg/label/td
td width=80 style=margin: 0px; padding: 3px 8px;USD 113/td
td width=62 style=margin: 0px; padding: 3px 8px;In stock/td
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nbsp;
option value=1 style=margin: 0px; padding: 0px;1/option
nbsp;
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option value=3 style=margin: 0px; padding: 0px;3/option
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option value=4 style=margin: 0px; padding: 0px;4/option
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option value=5 style=margin: 0px; padding: 0px;5/option
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option value=6 style=margin: 0px; padding: 0px;6/option
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option value=7 style=margin: 0px; padding: 0px;7/option
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option value=8 style=margin: 0px; padding: 0px;8/option
nbsp;
option value=9 style=margin: 0px; padding: 0px;9/option
nbsp;
option value=10 style=margin: 0px; padding: 0px;10/option
nbsp;/select/td
/tr
tr style=margin: 0px; padding: 0px;
td width=139 style=margin: 0px; padding: 3px 8px;label style=margin: 0px; padding: 0px;25mg/label/td
td width=80 style=margin: 0px; padding: 3px 8px;USD 214/td
td width=62 style=margin: 0px; padding: 3px 8px;In stock/td
td width=61 style=margin: 0px; padding: 3px 8px;select name=cartDTOs[2].quantity style=margin: 0px; padding: 0px; border-color: rgb(171, 171, 171); width: 40px;nbsp;
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td width=139 style=margin: 0px; padding: 3px 8px;label style=margin: 0px; padding: 0px;50mg/label/td
td width=80 style=margin: 0px; padding: 3px 8px;USD 340/td
td width=62 style=margin: 0px; padding: 3px 8px;In stock/td
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td width=80 style=margin: 0px; padding: 3px 8px;USD 466/td
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h3 id=biologicalActivity style=margin: 25px 0px 0px; padding: 0px; height: 25px; font-size: 14px; font-family: Arial, Tahoma, Helvetica; line-height: 19.200000762939453px;Biological Activity/h3
table width=100% border=0 cellspacing=0 cellpadding=0 class=product_show_table style=margin: 0px; padding: 0px; border-collapse: collapse; border-spacing: 0px; border-style: solid; border-color: rgb(229, 229, 229); color: rgb(0, 0, 0); font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;
tbody style=margin: 0px; padding: 0px;
tr style=margin: 0px; padding: 0px;
th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Description/th
td colspan=6 style=margin: 0px; padding: 5px 15px; text-align: justify; border-style: solid; border-color: rgb(229, 229, 229);Rimonabant is a selective antagonist ofnbsp;b style=margin: 0px; padding: 0px;CB1/bnbsp;withnbsp;b style=margin: 0px; padding: 0px;IC50/bnbsp;of 13.6 nM andnbsp;b style=margin: 0px; padding: 0px;EC50/bnbsp;of 17.3 nM in hCB1 transfected HEK 293 membrane./td
/tr
tr style=margin: 0px; padding: 0px;
th style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Targets/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);hCB1/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);hCB2/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Acuyl coenzyme A:cholesterol acyltransferase (ACAT/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);nbsp;/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);nbsp;/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);nbsp;/td
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tr style=margin: 0px; padding: 0px;
th style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);IC50/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);13.6 nM/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);1.64 mu;Mnbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/rimonabant-sr141716.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[1]/a/span/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);1.5-2.9 mu;Mnbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/rimonabant-sr141716.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[2]/a/span/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);nbsp;/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);nbsp;/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);nbsp;/td
/tr
tr style=margin: 0px; padding: 0px;
th style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);i style=margin: 0px; padding: 0px;In vitro/i/th
td colspan=6 style=margin: 0px; padding: 5px 15px; text-align: justify; border-style: solid; border-color: rgb(229, 229, 229);Rimonabant dose-dependently reduces ACAT activity in Raw264.7macrophages with IC50 of 2.9 mu;M and isolated peritoneal macrophages. Rimonabant inhibits ACATactivity in intact CHO-ACAT1 and CHO-ACAT2 cells and in cell-free assays with approximately equal efficiency with IC50 of 1.5 mu;M and 2.2 mu;M for CHO-ACAT1 and CHO-ACAT2, respectively. Consistent with ACAT inhibition, Rimonabant treatment blocks ACAT dependent processes in macrophages, oxysterol-induced apoptosis and acetylated-LDL induced foam cell formation.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/rimonabant-sr141716.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[2]/a/spanRimonabant antagonizes the inhibitory effects of cannabinoid receptor agonists on both mouse vas deferens contractions and adenylyl cyclase activity in rat brain membranes in a concentration-dependent manner.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/rimonabant-sr141716.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[3]/a/spanRimonabant significantly reduces cell growth and induces cell death of human colorectal cancer cells (DLD-1, CaCo-2 and SW620). Rimonabant is able to alter cell cycle distribution in all the cell lines tested. Particularly, Rimonabant produces a G2/M cell cycle arrest in DLD-1 cells without inducing apoptosis or necrosis.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/rimonabant-sr141716.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[4]/a/span/td
/tr
tr style=margin: 0px; padding: 0px;
th style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);i style=margin: 0px; padding: 0px;In vivo/i/th
td colspan=6 style=margin: 0px; padding: 5px 15px; text-align: justify; border-style: solid; border-color: rgb(229, 229, 229);Rimonabant is administered intraperitoneally or orally potently and dose-dependently antagonize classical pharmacological and behavioural effectos of cannabinoid receptor agonists.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/rimonabant-sr141716.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[3]/a/spannbsp;In the mouse model of azoxymethane-induced colon carcinogenesis, Rimonabant significantly decreased aberrant crypt foci (ACF) formation, which precedes colorectal cancer.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/rimonabant-sr141716.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[4]/a/spannbsp;Rimonabant (10 mg/kg by gavage) is fed for 2 weeks to 3-month-old male obese Zucker rats as an impaired glucose tolerance model and for 10 weeks to 6-month-old male obese Zucker rats as a model of the metabolic syndrome. RANTES (Regulated upon Activation, Normal T cell Expressed, and Secreted) and MCP-1 (monocyte chemotactic protein-1) serum levels are increased in obese vs lean Zucker rats and significantly reduced by long-term treatment with Rimonabant, which slowes weight gain in rats with the metabolic syndrome. Neutrophils and monocytes are significantly increased in young and old obese vs lean Zucker rats and lowered by Rimonabant. Platelet-bound fibrinogen is significantly enhanced in obese vs lean Zucker rats of both age, and is reduced by Rimonabant. Platelets from obese rats are more sensitive to thrombin-induced aggregation and adhesion to fibrinogen, which are both attenuated by Rimonabant therapy.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/rimonabant-sr141716.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[5]/a/span/td
/tr
tr style=margin: 0px; padding: 0px;
th style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Features/th
td colspan=6 style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Efficacious to induce weight reduction and improvements in cardiometabolic risk factors, however was withdrawn in 2009 due to severe depressive disorder and anxiety./td
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h3 id=protocol style=margin: 25px 0px 0px; padding: 0px; height: 25px; font-size: 14px; font-family: Arial, Tahoma, Helvetica; line-height: 19.200000762939453px;Protocolspan style=margin: 0px; padding: 0px; font-weight: normal;(Only for Reference)/span/h3
h4 style=margin: 0px; padding: 0px; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;Kinase Assay:nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/rimonabant-sr141716.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[1]/a/span/h4
table width=100% border=0 cellspacing=0 cellpadding=0 class=product_show_table style=margin: 0px; padding: 0px; border-collapse: collapse; border-spacing: 0px; border-style: solid; border-color: rgb(229, 229, 229); color: rgb(0, 0, 0); font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;
tbody style=margin: 0px; padding: 0px;
tr style=margin: 0px; padding: 0px;
th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Radioligand Binding Assay/th
td style=margin: 0px; padding: 5px 15px; text-align: justify; border-style: solid; border-color: rgb(229, 229, 229);Human CB1 and CB2 stably transfect HEK 293 cells and cell membrane is purified. 0.2-8 mu;g of the purified membrane is incubated with 0.75 nM [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH] CP55,940 and Rimonabant in the incubation buffer (50 mM Tris-HCl, 5 mM MgClspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;2/span, 1 mM EDTA, 0.3%BSA, pH 7.4). The non-specific binding is defined in the presence of 1 mu;M of CP55,940. The reactions are incubated for one and a half hours at 30 deg;C in Multiscreen. The reactions are terminated by manifold filtration and washed four times with ice-cold wash buffer (50mM Tris, pH 7.4, 0.25% BSA).The radioactivity bound to the filters is measured by Topcount. The IC50 is determined as the concentration of Rimonabant required to inhibit 50% of the binding of [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH] CP55,940 and calculated by non-linear regression./td
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th style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Eu-GTP Binding Assay/th
td style=margin: 0px; padding: 5px 15px; text-align: justify; border-style: solid; border-color: rgb(229, 229, 229);The Eu-GTP binding assay is performed using the DELFIA Eu-GTP binding kit based on methods developed by Frang et al., with minor modifications as described in the following: 1-4 mu;g of purified membrane is incubated with Rimonabant and 20 nM CP55,940 in the assay buffer (50 mM HEPES, pH 7.4, 100 mM NaCl, 100 mu;g/mL saponin, 5 mMMgClspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;2/span, 2 mu;M GDP, 0.5% BSA) at 30 deg;C for 60 minutes in acroplates. Following the addition of Eu-GTP and incubation for 30 minutes at 30 deg;C, the assay is terminated by washing four times with the washing buffer provided in the kit. The fluorescence signal of the Eu-GTP is determined with a Victor 2 multilabel reader. The EC50 of Rimonabant at inhibiting 50% of the CP55,940-stimulated Eu-GTP binding is determined from the dose-response curves using non-linear regression.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/rimonabant-sr141716.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[2]/a/span/td
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h4 style=margin: 0px; padding: 0px; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;Cell Assay:nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/rimonabant-sr141716.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[2]/a/span/h4
table width=100% border=0 cellspacing=0 cellpadding=0 class=product_show_table style=margin: 0px; padding: 0px; border-collapse: collapse; border-spacing: 0px; border-style: solid; border-color: rgb(229, 229, 229); color: rgb(0, 0, 0); font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;
tbody style=margin: 0px; padding: 0px;
tr style=margin: 0px; padding: 0px;
th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Cell lines/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Raw 264.7 cells/td
/tr
tr style=margin: 0px; padding: 0px;
th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Concentrations/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);0,1,4 mu;M/td
/tr
tr style=margin: 0px; padding: 0px;
th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Incubation Time/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);17 hours/td
/tr
tr style=margin: 0px; padding: 0px;
th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Method/th
td style=margin: 0px; padding: 5px 15px; text-align: justify; border-style: solid; border-color: rgb(229, 229, 229);Raw 264.7 cells (2 times; 10span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;6/spannbsp;/well) in 12-well plates are rinsed with PBS and refed culture media supplemented with varying amounts of Rimonabant 1 hour prior to supplementation with 7-ketocholesterol (7KC). All wells are adjusted to receive equal amounts of vehicle. Following 16-hour incubation, caspase-3 and caspase 3-like activity are determined using a fluorogenic substrate (Ac-DEVD-AFC) and a spectrofluorometer equipped with a microplate reader./td
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/table
h4 style=margin: 0px; padding: 0px; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;Animal Study:nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/rimonabant-sr141716.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[3]/a/span/h4
table width=100% border=0 cellspacing=0 cellpadding=0 class=product_show_table style=margin: 0px; padding: 0px; border-collapse: collapse; border-spacing: 0px; border-style: solid; border-color: rgb(229, 229, 229); color: rgb(0, 0, 0); font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;
tbody style=margin: 0px; padding: 0px;
tr style=margin: 0px; padding: 0px;
th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Animal Models/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Male mice and male rats/td
/tr
tr style=margin: 0px; padding: 0px;
th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Formulation/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Rimonabant is dissolved in two drops of Tween 80, diluted in distilled water./td
/tr
tr style=margin: 0px; padding: 0px;
th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Dosages/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);20 ml/kg (mice) and 5 ml/kg (rats)/td
/tr
tr style=margin: 0px; padding: 0px;
th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Administration/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Rimonabant is administered i.p. (30 minutes) or p.o. (1hour) before the i.v. injection of WIN55212-2./td
/tr
tr style=margin: 0px; padding: 0px;
th width=16% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Solubility/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);30% PEG400/0.5% Tween80/5% propylene glycol, 30 mg/mL/td
/tr
tr style=margin: 0px; padding: 0px;
td colspan=4 style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);span class=red style=margin: 0px; padding: 0px; color: rgb(255, 0, 0);*/spannbsp;Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations./td
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/tbody
/table
pa id=s_ref style=margin: 0px; padding: 0px; color: rgb(52, 84, 140); cursor: pointer; font-family: Arial, Tahoma, Helvetica; line-height: 19.200000762939453px; clear: both; float: left; height: 0px; font-size: 0px;1/a/p
h4 class=reference margin_t style=margin: 10px 0px 0px; padding: 0px; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;References/h4
h3 id=chemicalInformation style=margin: 25px 0px 0px; padding: 0px; height: 25px; font-size: 14px; font-family: Arial, Tahoma, Helvetica; line-height: 19.200000762939453px;Chemical Information/h3
pa href=http://file.selleckchem.com/downloads/product-sdf/rimonabant-sr141716-s3021.SDF style=margin: -25px 0px 0px 180px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px; float: left;Download Rimonabant SDF/a/p
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div class=clear style=margin: 0px; padding: 0px; zoom: 1; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;
table width=100% border=0 cellspacing=0 cellpadding=0 class=show_tab01 fl style=margin: 0px 0px 10px; padding: 0px; border-collapse: collapse; border-spacing: 0px; width: 375px; float: left;
tbody style=margin: 0px; padding: 0px;
tr style=margin: 0px; padding: 0px;
th width=45% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Molecular Weight (MW)/th
td width=55% style=margin: 0px; padding: 5px 0px 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);463.79/td
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tr style=margin: 0px; padding: 0px;
th width=45% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Formula/th
td style=margin: 0px; padding: 5px 0px 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);
p style=margin: 0px; padding: 0px;Cspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;22/spanHspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;21/spanClspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;3/spanNspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;4/spanO/p
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tr style=margin: 0px; padding: 0px;
th width=45% style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);CAS No./th
td style=margin: 0px; padding: 5px 0px 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);168273-06-1/td
/tr
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/table
table width=100% border=0 cellspacing=0 cellpadding=0 class=show_tab fr style=margin: 0px 0px 10px; padding: 0px; border-collapse: collapse; border-spacing: 0px; width: 375px; float: right;
tbody style=margin: 0px; padding: 0px;
tr style=margin: 0px; padding: 0px;
th rowspan=2 valign=top class=padding5 style=margin: 0px; padding: 5px 0px 5px 10px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Storage/th
td class=padding5 style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);3 yearsnbsp;span class=margin_l style=margin: 0px 0px 0px 10px; padding: 0px;-20℃/spanspan class=margin_l style=margin: 0px 0px 0px 10px; padding: 0px;Powder/span/td
/tr
tr style=margin: 0px; padding: 0px;
td class=padding5 style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);6 monthsspan class=margin_l style=margin: 0px 0px 0px 10px; padding: 0px;-80℃/spanspan class=margin_l style=margin: 0px 0px 0px 10px; padding: 0px;in DMSO/span/td
/tr
tr style=margin: 0px; padding: 0px;
th width=161 valign=top class=padding5 style=margin: 0px; padding: 5px 0px 5px 10px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Syonnyms/th
td width=214 class=padding5 style=margin: 0px; padding: 5px 0px 5px 10px; border-style: solid; border-color: rgb(229, 229, 229);SR141716/td
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div class=clear-both style=margin: 0px; padding: 0px; clear: both; height: 0px; overflow: hidden;nbsp;/div
table width=100% border=0 cellspacing=0 cellpadding=0 class=product_show_table mb15 style=margin: 0px 0px 15px; padding: 0px; border-collapse: collapse; border-spacing: 0px; border-style: solid; border-color: rgb(229, 229, 229);
tbody style=margin: 0px; padding: 0px;
tr style=margin: 0px; padding: 0px;
th width=12% rowspan=4 style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);strong style=margin: 0px; padding: 0px;Solubility (25deg;C)nbsp;/strongspan class=red style=margin: 0px; padding: 0px; color: rgb(255, 0, 0);*/span/th
td width=10% rowspan=3 class=italic style=margin: 0px; padding: 5px 15px; font-style: italic; border-style: solid; border-color: rgb(229, 229, 229);In vitro/td
td width=50% style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);DMSO/td
td width=28% style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);25 mg/mL (53 mM)/td
/tr
tr style=margin: 0px; padding: 0px;
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Water/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);lt;1 mg/mL (lt;1 mM)/td
/tr
tr style=margin: 0px; padding: 0px;
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Ethanol/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);2 mg/mL (4 mM)/td
/tr
tr style=margin: 0px; padding: 0px;
td class=italic style=margin: 0px; padding: 5px 15px; font-style: italic; border-style: solid; border-color: rgb(229, 229, 229);In vivo/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);30% PEG400/0.5% Tween80/5% propylene glycol,/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);30 mg/mL/td
/tr
tr style=margin: 0px; padding: 0px;
td colspan=4 style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);span class=red style=margin: 0px; padding: 0px; color: rgb(255, 0, 0);*/spannbsp;lt;1 mg/ml means slightly soluble or insoluble.br style=margin: 0px; padding: 0px; /
span class=red style=margin: 0px; padding: 0px; color: rgb(255, 0, 0);*/spannbsp;Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations./td
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/div
div style=margin: 0px; padding: 0px; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px; height: 10px;nbsp;/div
table width=100% border=0 cellspacing=0 cellpadding=0 class=product_show_table style=margin: 0px; padding: 0px; border-collapse: collapse; border-spacing: 0px; border-style: solid; border-color: rgb(229, 229, 229); color: rgb(0, 0, 0); font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;
tbody style=margin: 0px; padding: 0px;
tr style=margin: 0px; padding: 0px;
th width=153px style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Chemical Name/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide/td
/tr
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div class=clear-both style=margin: 0px; padding: 0px; clear: both; height: 0px; overflow: hidden; font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;nbsp;/div
h3 id=chemicalInformation style=margin: 25px 0px 0px; padding: 0px; height: 25px; font-size: 14px; font-family: Arial, Tahoma, Helvetica; line-height: 19.200000762939453px;Preparing Stock Solutions/h3
table width=100% border=0 cellspacing=0 cellpadding=0 class=product_show_table style=margin: 0px; padding: 0px; border-collapse: collapse; border-spacing: 0px; border-style: solid; border-color: rgb(229, 229, 229); color: rgb(0, 0, 0); font-family: Arial, Tahoma, Helvetica; font-size: 12px; line-height: 19.200000762939453px;
tbody style=margin: 0px; padding: 0px;
tr style=margin: 0px; padding: 0px;
th width=153px style=margin: 0px; padding: 5px 0px 5px 15px; font-weight: normal; border-style: solid; border-color: rgb(229, 229, 229);Stock Solution (1ml DMSO)/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);1mM/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);10mM/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);20mM/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);30mM/td
/tr
tr style=margin: 0px; padding: 0px;
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Mass(mg)/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);0.46379/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);4.6379/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);9.2758/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);13.9137/td
/tr
/tbody
/table
div class=counter style=margin: 10px 0px 0px; padding: 0px; font-size: 14px; font-weight: bold; font-family: Arial, Tahoma, Helvetica; line-height: 19.200000762939453px;a href=http://www.selleckchem.com/molaritycalculator.jsp style=margin: 0px 5px 0px 0px; padding: 5px 15px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer; display: inline-block; background-color: rgb(255, 239, 187); border: 1px solid rgb(237, 218, 159); background-position: initial initial; background-repeat: initial initial;Molarity Calculator/anbsp;a href=http://www.selleckchem.com/dilutioncalculator.jsp style=margin: 0px 5px 0px 0px; padding: 5px 15px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer; display: inline-block; background-color: rgb(255, 239, 187); border: 1px solid rgb(237, 218, 159); background-position: initial initial; background-repeat: initial initial;Dilution Calculator/anbsp;a href=http://www.selleckchem.com/molecular-weight-calculator.html style=margin: 0px 5px 0px 0px; padding: 5px 15px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer; display: inline-block; background-color: rgb(255, 239, 187); border: 1px solid rgb(237, 218, 159); background-position: initial initial; background-repeat: initial initial;Molecular Weight Calculator/a/div
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