CAS:821768-06-3JNJ-17203212

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

规格	价格	促销价格	库存

18817579266

立即询价

咨询

18817579266

立即询价

实验数据

技术信息

CAS号

821768-06-3

储存条件

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

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.