A TRPV1 antagonist (Ki = 72 nM for the recombinant guinea pig channel); inhibits capsaicin- or pH decrease-induced guinea pig TRPV1 channel activation (IC50s = 58 and 470 nM

JNJ-17203212 – 5 mg

Brand:
Cayman
CAS:
821768-06-3
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

JNJ-17203212 is a transient receptor potential vanilloid 1 (TRPV1) antagonist (Ki = 72 nM for the recombinant guinea pig channel).{56185} It inhibits guinea pig TRPV1 channel activation induced by capsaicin (Item Nos. 92350 | 10010743) or pH decrease (IC50s = 58 and 470 nM, respectively). JNJ-17203212 (20 mg/kg) reduces the number of citric acid- or capsaicin-induced coughs in guinea pigs. It reduces spontaneous and palpitation-induced flinching and guarding in a mouse model of bone cancer pain when administered at a dose of 30 mg/kg.{14469} JNJ-17203212 decreases capsaicin-induced production of calcitonin gene-related peptide (CGRP) in a dose-dependent manner and inflammatory soup-induced trigeminal expression of cfos in rat models of migraine.{56186}  

 

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SKU: 30930 - 5 mg Category:

Description

A TRPV1 antagonist (Ki = 72 nM for the recombinant guinea pig channel); inhibits capsaicin- or pH decrease-induced guinea pig TRPV1 channel activation (IC50s = 58 and 470 nM, respectively); reduces the number of citric acid- or capsaicin-induced coughs in guinea pigs at 20 mg/kg; reduces spontaneous and palpitation-induced flinching and guarding in a mouse model of bone cancer pain at 30 mg/kg; decreases capsaicin-induced production of CGRP and inflammatory soup-induced trigeminal expression of cfos in rat models of migraine

Formal name: 4-[3-(trifluoromethyl)-2-pyridinyl]-N-[5-(trifluoromethyl)-2-pyridinyl]-1-piperazinecarboxamide

Synonyms: 

Molecular weight: 419.3

CAS: 821768-06-3

Purity: ≥98%

Formulation: A crystalline solid

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