Eletriptan HBr

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h1 itemprop=name style=margin: 0px 20px 0px 0px; padding: 0px; font-size: 24px; float: left;Eletriptan HBr/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.S3180/span/div
p class=new_title style=margin: 5px 0px 10px; padding: 0px; clear: both; font-size: 11px; line-height: 14.399999618530273px;Eletriptan is a selectivenbsp;b style=margin: 0px; padding: 0px;5-HT1B/bnbsp;andnbsp;b style=margin: 0px; padding: 0px;5-HT1D/bnbsp;receptor 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 0.92 nM and 3.14 nM, respectively./p
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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 189/td
td width=62 style=margin: 0px; padding: 3px 8px;In stock/td
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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 844/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);Eletriptan is a selectivenbsp;b style=margin: 0px; padding: 0px;5-HT1B/bnbsp;andnbsp;b style=margin: 0px; padding: 0px;5-HT1D/bnbsp;receptor 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 0.92 nM and 3.14 nM, respectively./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);5-HT1B/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);5-HT1D/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);0.92 nM/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);3.14 nMnbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/eletriptan-hydrobromide.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);[span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]Eletriptan has a total number of binding sites (Bspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;max/span) of 2478 fmol/mg and 1576 fmol/mg for 5-HT1B and 5-HT1D, respectively. [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]Eletriptan has a significantly faster association rate (K(on) 0.249/min/nM) than [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]sumatriptan (K(on) 0.024/min/nM) and a significantly slower off-rate (K(off) 0.027/min compared to 0.037/min for [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]sumatriptan).nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/eletriptan-hydrobromide.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[1]/a/spannbsp;Eletriptan induces concentration-dependent contractions of meningeal artery, coronary artery, and saphenous vein. The potency of Eletriptan is higher in meningeal artery than in coronary artery (86-fold) or saphenous vein (66-fold). The predicted contraction by Eletriptan (40 mg and 80 mg) and sumatriptan (100 mg) at free C(max) observed in clinical trials is similar in meningeal artery.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/eletriptan-hydrobromide.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);Eletriptan (lt;1000 mg/kg, i.v.) produces a dose-dependent reduction of carotid arterial blood flow in the anaesthetised dog. Eletriptan reduces coronary artery diameter with ED50 value of 63 mg/kg in the anaesthetised dog. Eletriptan (lt;300 mg/kg, i.v.) administered prior to electrical stimulation of the trigeminal ganglion produces a dose-related and complete inhibition of plasma protein extravasation in the dura mater rats. Eletriptan (100 mg/kg, i.v.) produces a complete inhibition of plasma protein extravasation in rat dura mater.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/eletriptan-hydrobromide.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[3]/a/spannbsp;Headache response rates are 24% for placebo; 54% for Eletriptan (20 mg);65% for Eletriptan (40 mg);and 77% for Eletriptan (80 mg) at the primary endpoint (2 hours after dosing) in patients with migraine. Headache-free rates at 2 hours are 6% for placebo, 29% for Eletriptan (40 mg) and 37% for Eletriptan (80 mg) at the primary endpoint (2 hours after dosing) in patients with migraine. Eletriptan is well tolerated, and the majority of adverse events are mild or moderate in intensity and transient in patients with migraine.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/eletriptan-hydrobromide.html#s_ref class=sref style=margin: 0px; padding: 0px; text-decoration: none; color: rgb(52, 84, 140); cursor: pointer;[4]/a/spanIontophoretic ejection (50 nA) of Eletriptan suppresses the response in 75% of cells and causes an average suppression of cell firing of 42% in cats.nbsp;span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;a href=http://www.selleckchem.com/products/eletriptan-hydrobromide.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/eletriptan-hydrobromide.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 assay/th
td style=margin: 0px; padding: 5px 15px; text-align: justify; border-style: solid; border-color: rgb(229, 229, 229);Binding studies are performed in a total assay volume of 500 mL containing final protein concentrations of 50ndash;150 mg/mL. Time to equilibrium is determined by incubating 50 mL of [span style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: -0.5em;3/spanH]Eletriptan (85 Ci/mmol) with 400 mL of either 5-HT1B or 5-HT1D membrane homogenate for time points ranging from 1 to 60 min. These experiments are performed at either 4℃ or 22℃ using a Kspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;D/span, or lower, concentration of the appropriate radioligand, as determined from saturation assays. Total and non-specific binding are determined in duplicate at each time point. Non-specific binding is defined by 10 mu;M 5-HT. Following an initial incubation period of 30 min at either 4℃ or 22℃, dissociation is initiated by addition of 10 mM 5-HT, an excess concentration which over time would effectively displace all radioligand from the receptors. Total and non-specific binding are determined in duplicate at time points ranging from 1minndash;90 min./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
pa href=http://file.selleckchem.com/downloads/product-sdf/eletriptan-hbr-s3180.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 Eletriptan HBr SDF/a/p
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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);463.43/td
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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);Formula/th
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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;26/spanNspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;2/spanOspan style=margin: 0px; padding: 0px; position: relative; vertical-align: baseline; top: 0.25em;2/spanS.HBr/p
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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);CAS No./th
td style=margin: 0px; padding: 5px 0px 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);177834-92-3/td
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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
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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
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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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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);93 mg/mL (200 mM)/td
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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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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
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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 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;
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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);(R)-3-((1-methylpyrrolidin-2-yl)methyl)-5-(2-(phenylsulfonyl)ethyl)-1H-indole hydrobromide/td
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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;
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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);0.46343/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);4.6343/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);9.2686/td
td style=margin: 0px; padding: 5px 15px; border-style: solid; border-color: rgb(229, 229, 229);13.9029/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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