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CAS No.: 821768-06-3

JNJ-17203212 Catalog No. CSN18446

JNJ-17203212 is a selective TRPV1 antagonist, with IC50 of 65 nM and 102 nM for human TRPV1 and rat TRPV1.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述TRPV1 is a non-selective cation channel, predominantly expressed by peripheral sensory neurons. It plays a key role in the detection of noxious painful stimuli, such as capsaicin, acid and heat. JNJ-17203212 is a potent and selective TRPV1 antagonist with pK_i values of 7.3, 6.5 and 7.14 for equilibrium binding affinities for human TRPV1, rat TRPV1 and Guinea pig TRPV1. JNJ17203212 dose-dependently inhibited 1μM capsaicin-induced Ca²⁺ mobilization in recombinant guinea pig TRPV1-CHO cells with pIC50 value of 6.32, as well as inhibited proton activation (pH 4.5) of guinea pig TRPV1 receptor with pIC50 value of 7.23. Intraperitoneal administration of 20 mg/kg JNJ17203212 attenuated capsaicin evoked coughs and citric acid-induced experimental coughs in guinea pig models.
动物研究
剂量
Rat: 3 mg/kg - 30 mg/kg^[1] (p.o.) Mice: 40 mg/kg^[3] (i.p.)

给药途径
p.o., i.p.
参考文献

动物研究
剂量	Rat: 3 mg/kg - 30 mg/kg^[1] (p.o.) Mice: 40 mg/kg^[3] (i.p.)
给药途径	p.o., i.p.

[1] Wiskur BJ, Tyler K, 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, Dubin AE, 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):1857-72.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3848 mL
- 11.9239 mL
- 23.8479 mL
- 5 mM
- 0.4770 mL
- 2.3848 mL
- 4.7696 mL
- 10 mM
- 0.2385 mL
- 1.1924 mL
- 2.3848 mL

技术信息

CAS号

821768-06-3

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H15F6N5O

运输

蓝冰

分子量

419.32

别名

溶解度

DMSO	100.0 mg/mL (238.5 mM)
Water	Insoluble

动物实验配方

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