Azilsartan Medoxomil

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h1 itemprop=name style=margin: 0px 20px 0px 0px; padding: 0px; font-size: 24px; float: left;Azilsartan Medoxomil/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.S3057/span/div
p class=new_title style=margin: 5px 0px 10px; padding: 0px; clear: both; font-size: 11px; line-height: 14.399999618530273px;Azilsartan Medoxomil is a potentnbsp;b style=margin: 0px; padding: 0px;angiotensin II type 1 (AT1) receptor/bnbsp;antagonist, inhibits thenbsp;b style=margin: 0px; padding: 0px;RAAS/b, with annbsp;b style=margin: 0px; padding: 0px;IC50/bnbsp;of 2.6 nM, exhibits gt;10,000-fold selectivity over AT2. Phase 3./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 491/td
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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 2356/td
td width=62 style=margin: 0px; padding: 3px 8px;In stock/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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td colspan=6 style=margin: 0px; padding: 5px 15px; text-align: justify; border-style: solid; border-color: rgb(229, 229, 229);Azilsartan Medoxomil is a potentnbsp;b style=margin: 0px; padding: 0px;angiotensin II type 1 (AT1) receptor/bnbsp;antagonist, inhibits thenbsp;b style=margin: 0px; padding: 0px;RAAS/b, with anb style=margin: 0px; padding: 0px;IC50/bnbsp;of 2.6 nM, exhibits gt;10,000-fold selectivity over AT2. Phase 3./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);AT1/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
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);2.6 nMnbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/azilsartan-medoxomil-tak-491.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
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);Azilsartan medoxomil is a prodrug, which is rapidly converted to the active moiety, azilsartan (TAK-536), by ester hydrolysis in the gut and plasma during absorption after oral administration. Azilsartan selectively blocks the binding of angiotensin II to the AT1 (angiotensin II type 1) receptors found in the vascular smooth muscle and the adrenal gland, thereby promoting vasodilation and a decrease in the effects of aldosterone.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/azilsartan-medoxomil-tak-491.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[2]/a/spannbsp;Azilsartan is a highly selective antagonist to the AT1 receptor, with an IC50 of 2.6 nM, exhibiting a gt;10,000-fold affinity for the AT1 receptor compared with the AT2 receptor, and has not shown affinity for other cardiac receptors or ion channels. The inhibitory effect of Azilsartan persists after washout of the free compound (IC50 value of 7.4 nM). Azilsartan also inhibits the accumulation of angiotensin II -induced inositol 1-phosphate (IP1) in the cell-based assay with an IC50 value of 9.2 nM, and this effect is resistant to washout (IC50 value of 81.3 nM).nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/azilsartan-medoxomil-tak-491.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[1]/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);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);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/azilsartan-medoxomil-tak-491.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/th
td style=margin: 0px; padding: 5px 15px; text-align: justify; border-style: solid; border-color: rgb(229, 229, 229);A radioligand binding assay is performed by using human AT1 receptor-coated microplates containing 4.4 to 6.2 fmol of receptors/well (10 mu;g of membrane protein/well). Membrane-coated wells are incubated with 45 mu;l of assay 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, and 0.005% CHAPS, pH 7.4) containing various concentrations of test compounds at room temperature. After 90 min, 5 mu;l ofnbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;125/spanI-Sarspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;1/span-Ilespan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;8/span-AII (final concentration 0.6 nM) dissolved in assay buffer is added to the wells, and the plate is incubated for 5 h. In each step, the plate is briefly and gently shaken on a plate shaker./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/azilsartan-medoxomil-tak-491.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);Cell lines/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);COS-7/td
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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);Concentrations/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);~10 nM/td
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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);Incubation Time/th
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);2 h/td
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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);Method/th
td style=margin: 0px; padding: 5px 15px; text-align: justify; border-style: solid; border-color: rgb(229, 229, 229);Measurement of Inositol 1-Phosphate Accumulation. Twentyfour hours after transfections with human AT1-expressing plasmids, the cells are starved by changing the culture medium to starvation buffer (1 mM CaCl2, 0.5 mM MgClspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;2/span, 4.2 mM KCl, 146 mM NaCl, 5.5 mM glucose, and 10 mM HEPES, pH 7.3). Then, 5 mu;l/well of the test compounds dissolved in starvation buffer is added to the cells at the indicated concentrations, and they are pretreated for the indicated times. Two hours after starvation, LiCl is added to a final concentration of 50 mM with or without angiotensin II 10 nM, and the cells are further incubated for the indicated times at 37deg;C. In washout experiments, the cells are washed once with 100 mu;l/well of starvation buffer to remove unbound compounds before stimulation with angiotensin II. The accumulation of inositol 1-phosphate (IP1) is measured by using a IP-One Tb kit. The fluorescence resonance energy transfer signal is measured on a plate reader./td
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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
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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);568.53/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;30/spanHspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;24/spanNspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;4/spanOspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;8/span/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);863031-21-4/td
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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
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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=3 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);114 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
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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);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 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);1H-Benzimidazole-7-carboxylic acid, 1-[[2rsquo;-(2,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)[1,1rsquo;-biphenyl]-4-yl]methyl]-2-ethoxy-, (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester/td
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/tbody
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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);0.56853/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);5.6853/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);11.3706/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);17.0559/td
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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; color: rgb(52, 84, 140); cursor: pointer; display: inline-block; background-color: rgb(255, 239, 187); border: 1px solid rgb(237, 218, 159);Molecular Weight Calculator/a/div
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