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JNJ 17203212
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。
JNJ 17203212图片
CAS NO:821768-06-3
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
JNJ 17203212 是一种选择性、有效和竞争性的 TRPV1 拮抗剂。
Cas No.821768-06-3
别名4-(3-(三氟甲基)吡啶-2-基)-N-(5-三氟甲基)吡啶-2-基)哌嗪-1-甲酰胺
化学名4-(3-(trifluoromethyl)pyridin-2-yl)-N-(5-(trifluoromethyl)pyridin-2-yl)piperazine-1-carboxamide
Canonical SMILESFC(F)(C1=CC=CN=C1N2CCN(C(NC3=NC=C(C(F)(F)F)C=C3)=O)CC2)F
分子式C17H15F6N5O
分子量419.32
溶解度DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml
储存条件Store at -20℃
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

JNJ-17203212 is a novel and selective TRPV1 antagonist, with IC50 of 65 nM and 102 nM for human TRPV1 and rat TRPV1.IC50 value: 65 nM (human TRPV1), 102 nM (rat TRPV1)Target: TRPVin vivo: JNJ-17203212 reduces sensitivity to luminal distension in both an acute, noninflammatory and a chronic, post-inflammatory rodent model of colonic hypersensitivity. Throughout this study, colonic sensitivity was assessed via quantification of VMR to CRD in rats following a single, oral administration of JNJ-17203212 (3, 10 or 30 mg/kg) or vehicle. [1] Oral pretreatment with JNJ-17203212 is a novel and selective TRPV1 antagonist, with partially prevents core hypothermia evoked by sc capsaicin. Oral pretreatment with JNJ-17203212 is a novel and selective TRPV1 antagonist, with partially prevents capsaicin-evoked hypothermia in a dose-response manner. [2]

References:
[1]. Wiskur BJ, et al. A novel TRPV1 receptor antagonist JNJ-17203212 attenuates colonic hypersensitivity in rats. Methods Find Exp Clin Pharmacol. 2010 Oct;32(8):557-64.
[2]. Swanson DM, et al. Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist. J Med Chem. 2005 Mar 24;48(6):185