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SB 366791
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
SB 366791图片
CAS NO:472981-92-3

SB 366791 是一种有效的选择性香草素受体 (VR1/TRPV1) 拮抗剂 (IC50\u003d5.7 nM)。
Cas No.472981-92-3
别名3-(4-氯苯基)-N-(3-甲氧基苯基)-2-丙烯酰胺
化学名(E)-3-(4-chlorophenyl)-N-(3-methoxyphenyl)acrylamide
Canonical SMILESClC1=CC=C(C=C1)/C=C/C(NC2=CC=CC(OC)=C2)=O
分子式C16H14ClNO2
分子量287.75
溶解度≥ 12.35mg/mL in DMSO
储存条件Store at RT
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

SB-366791 is a potent , competitive and selective vanilloid receptor (VR1/TRPV1) antagonist with IC50 of 5.7±1.2 nMtarget: VR1/TRPV1IC 50: 5.7±1.2 nM [1] SB-366791 produced a concentration-dependent inhibition of the response to capsaicin with an apparent pKb of 7.74±0.08. Schild analysis indicated a competitive mechanism of action with a pA2 of 7.71.[1] SB-366791 showed a concentration-dependent potentiation of pH 5-induced 45Ca2+uptake in CHO cells expressing rat TRPV1 but not in untransfected cells[2]

References:
[1]. M.J. Gunthorpe et al. Identification and characterisation of SB-366791, a potent and selective vanilloid receptor (VR1/TRPV1) antagonist. Neuropharmacology, 2004 Jan, 46(1):133-49.
[2]. Gavva NR et al. Proton Activation Does Not Alter Antagonist Interaction with the Capsaicin-Binding Pocket of TRPV1. Mol Pharmacol, 2005 Dec, 68(6), 1524-33.

 
 
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