JNJ-17203212

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、选择性的、口服生物可利用的 TRPV1 受体拮抗剂，对 hTRPV1 和 rTRPV1 的 IC50 分别为 65 nM 和 102 nM。

A potent, selective and orally bioavailable TRPV1 receptor antagonist with IC50 of 65 nM and 102 nM for hTRPV1 and rTRPV1, respectively; exhibits high selectivity against a panel of receptors and transporters, and does not inhibits related TRP channels TRPV2, TRPV4, or TRPA1; inhibits both pH (pIC50=7.23) and capsaicin (pIC50=6.32)-induced channel activation; attenuates capsaicin evoked coughs, prevents core hypothermia evoked by capsaicin in vivo.Pain Preclinical.

JNJ-17203212 (0.5 μM) potently inhibits imperatorin-induced TRPV1 activation (Ca2+ increases) in TRPV1-expressing HEK cells.

JNJ-17203212 (0.3 mg/kg; i.v.) dose-dependently reduces inflammatory soup (IS)-induced the immediate early gene c-fos expression.JNJ-17203212 completely blocks capsaicin-induced CGRP (the neurotransmitter calcitonin gene-related peptide) release in a dose-dependent manner. Animal Model:Male Sprague-Dawley rats (260-300 g)Dosage:0.3 mg/kg Administration:Intravenous injection Result:Had a dose-dependent effect on the elevated c-fos expression that occurred after intracisternal injection of IS.

JNJ17203212 | JNJ 17203212

Membrane Transporter/Ion Channel

TRP/TRPV Channel

TRP/TRPV Channel

Neurological Disease

Pain

821768-06-3

419.3243

C17H15F6N5O

>98% (HPLC)

10 mM in DMSO

O=C(N1CCN(C2=NC=CC=C2C(F)(F)F)CC1)NC3=NC=C(C(F)(F)F)C=C3

1-Piperazinecarboxamide, 4-[3-(trifluoromethyl)-2-pyridinyl]-N-[5-(trifluoromethyl)-2-pyridinyl]-

(-20℃)

With Ice Pack

≥ 2 years