JNJ-17203212

SKU: orb1223937

Description

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.

Key Properties

• CAS Number: 821768-06-3
• MW: 419.3243
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₅F₆N₅O
• SMILES: O=C(N1CCN(C2=NC=CC=C2C(F)(F)F)CC1)NC3=NC=C(C(F)(F)F)C=C3
• Target: TRP/TRPV Channel
• Solubility: 10 mM in DMSO

Bioactivity

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

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

JNJ17203212 | JNJ 17203212

Quick Database Links

Gene Symbol

TRP/TRPV Channel