Antibodies
AM1241
- 貨號 Cat. No.
- S1544
- 規格 Size
- 10mM/1mL~25mg
- 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;AM1241/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.S1544/spanspan class=star01 fl style=margin: 2px 0px 0px; padding: 0px; float: left; width: 70px; height: 13px; vertical-align: middle; background-image: url(http://file.selleckchem.com/images/bg.gif); background-position: -200px -70px; background-repeat: no-repeat no-repeat;
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/spana class=pro_a href=http://www.selleckchem.com/products/AM-1241.html#customerReviews date-widget=scrollMove style=margin: 0px 15px 0px 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer; float: left;span class=margin_l style=margin: 0px 0px 0px 10px; padding: 0px;1 Reviews/span/aa class=pro_a href=http://www.selleckchem.com/products/AM-1241.html#productCitations date-widget=scrollMove style=margin: 0px 15px 0px 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer; float: left;1 Product Citations/a/div
p class=new_title style=margin: 5px 0px 10px; padding: 0px; clear: both; font-size: 11px; line-height: 14.399999618530273px;AM-1241 is a selectivenbsp;b style=margin: 0px; padding: 0px;cannabinoid CB2 receptor/bnbsp;agonist withnbsp;b style=margin: 0px; padding: 0px;Kspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;i/span/bnbsp;of 3.4 nM, exhibits 82-fold selectivity over CB1 receptor./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 176/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 88/td
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td width=80 style=margin: 0px; padding: 3px 8px;USD 151/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);AM-1241 is a selectivenbsp;b style=margin: 0px; padding: 0px;cannabinoid CB2 receptor/bnbsp;agonist withnbsp;b style=margin: 0px; padding: 0px;Kspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;i/span/bnbsp;of 3.4 nM, exhibits 82-fold selectivity over CB1 receptor./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);CB2/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);CB1/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
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);3.4 nM (Kspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;i/span)/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);280 nM (Kspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;i/span)nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/AM-1241.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);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
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);AM-1241 is a protean agonist of CB2 based on the different effect observed in various assays (calcium influx, extracellular signal-regulated kinase (ERK) phosphorylatin and cAMP measurement)) and on the switch from neutral antagonism to agonism in the cAMP assay when forskolin concentration is lowered. In [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]CP 55,940 competition binding assays, AM-1241 displays high affinity at the human CB2 receptor with a Kspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;i/spannbsp;value of about 7 nM, whereas its affinity at the human CB1 receptor is more than 80-fold weaker, using membrane preparations from stable HEK and CHO cell lines expressing the recombinant human CB2 and CB1 receptors, respectively.span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/AM-1241.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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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);AM-1241 dose-dependently reverses tactile and thermal hypersensitivity produced by ligation of the L5 and L6 spinal nerves in rats. AM-1241 is also active in blocking spinal nerve ligation-induced tactile and thermal hypersensitivity in mice lacking CB1 receptors (CB1-/- mice), confirming that AM-1241 reverses sensory hypersensitivity independent of actions at CB1 receptors.span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/AM-1241.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[1]/a/spannbsp;AM-1241 (100, 330 mu;g/kg i.p.) suppresses the development of carrageenan-evoked thermal and mechanical hyperalgesia and allodynia. And this suppression is blocked by CB2 antagonist SR144528 but not by CB1 antagonist SR141716A.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/AM-1241.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[3]/a/spannbsp;AM1241 produces dose-dependent antinociception to a thermal stimulus applied to the hindpaw, when administered into the hindpaw on the side of testing (ipsilateral i. paw), while much less active into the contralateral to the side. A50 (analgesic dose yielding a 50% effect) of AM1241 is 847 mu;g/kg with the maximum possible effect (100% MPE) being achieved at 3.3 mg/kg. AM1241 also produces dose-dependent antinociception when administered intraperitoneally (i.p.), with an A50 of 103mu;g/kg. The antinociceptive actions of AM1241 are blocked by the CB2 receptor-selective antagonist AM630, but not by the CB1 receptor-selective antagonist AM251. AM1241 dosnrsquo;ï½”roduce the CNS cannabinoid effects of hypothermia, catalepsy, inhibition of activity or impaired ambulation, while this tetrad of effects is produced by the mixed CB1/CB2 receptor agonist WIN55,212-2.span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/AM-1241.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[4]/a/spanDaily injections of AM-1241 through a i.p. route, initiated at symptom onset, increases the survival interval after amyotrophic lateral sclerosis (ALS) onset by 56% in a transgenic mouse model of ALS.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/AM-1241.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);nbsp;/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/AM-1241.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);Binding Assays/th
td style=margin: 0px; padding: 5px 15px; text-align: justify; border-style: solid; border-color: rgb(229, 229, 229);Binding to cannabinoid receptors is tested by using competition-equilibrium binding vs. [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]CP55,940. AM-1241 is diluted into 25 mM Tris base (pH 7.4)/5 mM MgClspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;2/span/1 mM EDTA/0.1% essentially fatty acid-free BSA and transferred to Regisil-treated 96-well plates. [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]CP55,940 (DuPont_NEN; specific activity 100ndash;180 Ci/ mmol; 1 Ci =37 GBq) is added to a concentration of 0.8 nM. Membranes prepared from rat brain (containing CB1 receptors) or mouse spleen (containing CB2 receptors) are added (asymp;50 mu;g of membrane protein per well), plates are incubated at 30 deg;C for 1 hour, and the contents are filtered over Packard Unifilter GF/B 96-well filters by using a Packard Filtermate 196 cell harvester. Filters are washed with ice-cold 50 mM Tris base/5 mM MgClspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;2/span/0.5% BSA and dried. Bound radioactivity is quantitated and corrected for nonspecific binding, and results are normalized between 0% and 100% [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]CP-55,940 specifically bound. IC50 is determined by nonlinear regression analysis using GraphPad PRISM and transformed to a Ki value. All data are collected in duplicate. IC50 and Ki values are determined from three independent experiments./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/AM-1241.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[2]/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);Cell lines/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);HEK cells and CHO cell lines stably express human CB2 receptor and CB1 receptor./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);12 concentrations between 0.1 nMndash;10 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);90 minutes/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);Membrane samples are prepared from HEK cells stably expressing the human CB2 receptors previously generated (Mukherjee et al., 2004), or the CHO cell line that stably expresses the human CB1 receptor. Radioligand binding assays are performed as following. Briefly, the cells are harvested and homogenized using a Polytron for 2 times; 10 s bursts in a buffer containing 50 mM Tris-HCl, pH 7.4, 1 mM MgClspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;2/span, and 1mM EDTA in the presence of protease inhibitors followed by centrifugation at 45 000 g for 20 minutes. The membrane pellets are washed and frozen at -80 deg;C in aliquots until use. Saturation binding reactions are performed at 30 deg;C for 90 minutes using [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]CP 55,940 (0.01ndash;8 nM) in an assay buffer containing 50 mM Tris-HCl, pH 7.4, 2.5 mM EDTA, 5mM MgClspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;2/span, and 0.05% fatty acid free bovine serum albumin (BSA) and the reactions are terminated by rapid vacuum filtration through UniFilter-96 GF/C filter plates and four washes with cold assay buffer. Competition experiments are conducted using 0.5 nM [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]CP 55,940 in the presence of test compounds (0.1 nMndash;10 mu;M). Nonspecific binding is defined by 10 mM unlabeled CP 55,940. Kspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;D/spannbsp;values from saturation binding assays and Ki values from competition binding assays are determined with one site binding or one site competition curve fitting using the Prism software./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/AM-1241.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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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);250-350 g male Sprague-Dawley 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);AM-1241 is dissolved in dimethyl sulfoxide./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);0, 100, 300, 1000, 3000 mu;g/kg/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);Administered via i.p./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);1% DMSO/30% polyethylene glycol/1% Tween 80, 8 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/am-1241-s1544.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 AM1241 SDF/a/p
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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);503.33/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;22/spanINspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;3/spanOspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;3/span/p
/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);CAS No./th
td style=margin: 0px; padding: 5px 0px 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);444912-48-5/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);N/A/td
/tr
/tbody
/table
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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);101 mg/mL (200 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);lt;1 mg/mL (lt;1 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);1% DMSO/30% polyethylene glycol/1% Tween 80,/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);8 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);(2-iodo-5-nitrophenyl)(1-((1-methylpiperidin-2-yl)methyl)-1H-indol-3-yl)methanone/td
/tr
/tbody
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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);0.50333/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);5.0333/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);10.0666/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);15.0999/td
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/tbody
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td class=italic style=margin: 0px; padding: 5px 15px; font-style: italic; border-style: solid; border-color: rgb(229, 229, 229);Sci China Life Sci, 2014, 57(2):201-8.span style=margin: 0px; padding: 0px; font-style: normal;nbsp;AM1241 purchased from Selleck/span/td
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td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Method/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Massonrsquo;ｓ trichrome staining/td
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td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Concentrations/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);20 mg kg-1 d-1/td
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tr style=margin: 0px; padding: 0px;
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Incubation Time/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);7 d/td
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td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Results/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);AM1241 increased ki67+ positive cells and decreased cardiac fibrosis after MI./td
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p class=product_citation_p style=margin: 0px; padding: 0px; float: left; width: 760px;Effects of cannabinoid receptor type 2 on endogenous myocardial regeneration by activating cardiac progenitor cells in mouse infarcted heart. [Wang Y, et al. Sci China Life Sci 2014;57(2):201-8]/p
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pnbsp;/p
pnbsp;/p
h1 itemprop=name style=margin: 0px 20px 0px 0px; padding: 0px; font-size: 24px; float: left;AM1241/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.S1544/spanspan class=star01 fl style=margin: 2px 0px 0px; padding: 0px; float: left; width: 70px; height: 13px; vertical-align: middle; background-image: url(http://file.selleckchem.com/images/bg.gif); background-position: -200px -70px; background-repeat: no-repeat no-repeat;
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/spana class=pro_a href=http://www.selleckchem.com/products/AM-1241.html#customerReviews date-widget=scrollMove style=margin: 0px 15px 0px 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer; float: left;span class=margin_l style=margin: 0px 0px 0px 10px; padding: 0px;1 Reviews/span/aa class=pro_a href=http://www.selleckchem.com/products/AM-1241.html#productCitations date-widget=scrollMove style=margin: 0px 15px 0px 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer; float: left;1 Product Citations/a/div
p class=new_title style=margin: 5px 0px 10px; padding: 0px; clear: both; font-size: 11px; line-height: 14.399999618530273px;AM-1241 is a selectivenbsp;b style=margin: 0px; padding: 0px;cannabinoid CB2 receptor/bnbsp;agonist withnbsp;b style=margin: 0px; padding: 0px;Kspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;i/span/bnbsp;of 3.4 nM, exhibits 82-fold selectivity over CB1 receptor./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 176/td
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td width=80 style=margin: 0px; padding: 3px 8px;USD 88/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);AM-1241 is a selectivenbsp;b style=margin: 0px; padding: 0px;cannabinoid CB2 receptor/bnbsp;agonist withnbsp;b style=margin: 0px; padding: 0px;Kspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;i/span/bnbsp;of 3.4 nM, exhibits 82-fold selectivity over CB1 receptor./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);CB2/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);CB1/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
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);IC50/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);3.4 nM (Kspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;i/span)/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);280 nM (Kspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;i/span)nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/AM-1241.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);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
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);AM-1241 is a protean agonist of CB2 based on the different effect observed in various assays (calcium influx, extracellular signal-regulated kinase (ERK) phosphorylatin and cAMP measurement)) and on the switch from neutral antagonism to agonism in the cAMP assay when forskolin concentration is lowered. In [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]CP 55,940 competition binding assays, AM-1241 displays high affinity at the human CB2 receptor with a Kspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;i/spannbsp;value of about 7 nM, whereas its affinity at the human CB1 receptor is more than 80-fold weaker, using membrane preparations from stable HEK and CHO cell lines expressing the recombinant human CB2 and CB1 receptors, respectively.span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/AM-1241.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[2]/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);AM-1241 dose-dependently reverses tactile and thermal hypersensitivity produced by ligation of the L5 and L6 spinal nerves in rats. AM-1241 is also active in blocking spinal nerve ligation-induced tactile and thermal hypersensitivity in mice lacking CB1 receptors (CB1-/- mice), confirming that AM-1241 reverses sensory hypersensitivity independent of actions at CB1 receptors.span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/AM-1241.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[1]/a/spannbsp;AM-1241 (100, 330 mu;g/kg i.p.) suppresses the development of carrageenan-evoked thermal and mechanical hyperalgesia and allodynia. And this suppression is blocked by CB2 antagonist SR144528 but not by CB1 antagonist SR141716A.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/AM-1241.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[3]/a/spannbsp;AM1241 produces dose-dependent antinociception to a thermal stimulus applied to the hindpaw, when administered into the hindpaw on the side of testing (ipsilateral i. paw), while much less active into the contralateral to the side. A50 (analgesic dose yielding a 50% effect) of AM1241 is 847 mu;g/kg with the maximum possible effect (100% MPE) being achieved at 3.3 mg/kg. AM1241 also produces dose-dependent antinociception when administered intraperitoneally (i.p.), with an A50 of 103mu;g/kg. The antinociceptive actions of AM1241 are blocked by the CB2 receptor-selective antagonist AM630, but not by the CB1 receptor-selective antagonist AM251. AM1241 dosnrsquo;ï½”roduce the CNS cannabinoid effects of hypothermia, catalepsy, inhibition of activity or impaired ambulation, while this tetrad of effects is produced by the mixed CB1/CB2 receptor agonist WIN55,212-2.span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/AM-1241.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[4]/a/spanDaily injections of AM-1241 through a i.p. route, initiated at symptom onset, increases the survival interval after amyotrophic lateral sclerosis (ALS) onset by 56% in a transgenic mouse model of ALS.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/AM-1241.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);nbsp;/td
/tr
/tbody
/table
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/AM-1241.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);Binding Assays/th
td style=margin: 0px; padding: 5px 15px; text-align: justify; border-style: solid; border-color: rgb(229, 229, 229);Binding to cannabinoid receptors is tested by using competition-equilibrium binding vs. [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]CP55,940. AM-1241 is diluted into 25 mM Tris base (pH 7.4)/5 mM MgClspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;2/span/1 mM EDTA/0.1% essentially fatty acid-free BSA and transferred to Regisil-treated 96-well plates. [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]CP55,940 (DuPont_NEN; specific activity 100ndash;180 Ci/ mmol; 1 Ci =37 GBq) is added to a concentration of 0.8 nM. Membranes prepared from rat brain (containing CB1 receptors) or mouse spleen (containing CB2 receptors) are added (asymp;50 mu;g of membrane protein per well), plates are incubated at 30 deg;C for 1 hour, and the contents are filtered over Packard Unifilter GF/B 96-well filters by using a Packard Filtermate 196 cell harvester. Filters are washed with ice-cold 50 mM Tris base/5 mM MgClspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;2/span/0.5% BSA and dried. Bound radioactivity is quantitated and corrected for nonspecific binding, and results are normalized between 0% and 100% [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]CP-55,940 specifically bound. IC50 is determined by nonlinear regression analysis using GraphPad PRISM and transformed to a Ki value. All data are collected in duplicate. IC50 and Ki values are determined from three independent experiments./td
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/tbody
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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/AM-1241.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);HEK cells and CHO cell lines stably express human CB2 receptor and CB1 receptor./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);12 concentrations between 0.1 nMndash;10 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);90 minutes/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);Membrane samples are prepared from HEK cells stably expressing the human CB2 receptors previously generated (Mukherjee et al., 2004), or the CHO cell line that stably expresses the human CB1 receptor. Radioligand binding assays are performed as following. Briefly, the cells are harvested and homogenized using a Polytron for 2 times; 10 s bursts in a buffer containing 50 mM Tris-HCl, pH 7.4, 1 mM MgClspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;2/span, and 1mM EDTA in the presence of protease inhibitors followed by centrifugation at 45 000 g for 20 minutes. The membrane pellets are washed and frozen at -80 deg;C in aliquots until use. Saturation binding reactions are performed at 30 deg;C for 90 minutes using [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]CP 55,940 (0.01ndash;8 nM) in an assay buffer containing 50 mM Tris-HCl, pH 7.4, 2.5 mM EDTA, 5mM MgClspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;2/span, and 0.05% fatty acid free bovine serum albumin (BSA) and the reactions are terminated by rapid vacuum filtration through UniFilter-96 GF/C filter plates and four washes with cold assay buffer. Competition experiments are conducted using 0.5 nM [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]CP 55,940 in the presence of test compounds (0.1 nMndash;10 mu;M). Nonspecific binding is defined by 10 mM unlabeled CP 55,940. Kspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;D/spannbsp;values from saturation binding assays and Ki values from competition binding assays are determined with one site binding or one site competition curve fitting using the Prism software./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/AM-1241.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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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);250-350 g male Sprague-Dawley 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);AM-1241 is dissolved in dimethyl sulfoxide./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);0, 100, 300, 1000, 3000 mu;g/kg/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);Administered via i.p./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);1% DMSO/30% polyethylene glycol/1% Tween 80, 8 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/am-1241-s1544.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 AM1241 SDF/a/p
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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);503.33/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;22/spanINspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;3/spanOspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;3/span/p
/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);CAS No./th
td style=margin: 0px; padding: 5px 0px 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);444912-48-5/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);N/A/td
/tr
/tbody
/table
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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);101 mg/mL (200 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);lt;1 mg/mL (lt;1 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);1% DMSO/30% polyethylene glycol/1% Tween 80,/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);8 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);(2-iodo-5-nitrophenyl)(1-((1-methylpiperidin-2-yl)methyl)-1H-indol-3-yl)methanone/td
/tr
/tbody
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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);0.50333/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);5.0333/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);10.0666/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);15.0999/td
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/tbody
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td class=italic style=margin: 0px; padding: 5px 15px; font-style: italic; border-style: solid; border-color: rgb(229, 229, 229);Sci China Life Sci, 2014, 57(2):201-8.span style=margin: 0px; padding: 0px; font-style: normal;nbsp;AM1241 purchased from Selleck/span/td
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td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Method/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Massonrsquo;ｓ trichrome staining/td
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td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);20 mg kg-1 d-1/td
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tr style=margin: 0px; padding: 0px;
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Incubation Time/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);7 d/td
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td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);Results/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);AM1241 increased ki67+ positive cells and decreased cardiac fibrosis after MI./td
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p class=product_citation_p style=margin: 0px; padding: 0px; float: left; width: 760px;Effects of cannabinoid receptor type 2 on endogenous myocardial regeneration by activating cardiac progenitor cells in mouse infarcted heart. [Wang Y, et al. Sci China Life Sci 2014;57(2):201-8]/p
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