JNJ-17203212

SKU: orb1299739

Description

JNJ-17203212 is a potent, selective TRPV1 antagonist with IC50 values of 65 nM and 102 nM for human and rat receptors, respectively. This compound is a valuable research tool for investigating TRPV1-mediated pathways in pain, inflammation, and neurogenic conditions, supporting both in vitro and in vivo experimental models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 821768-06-3
• MW: 419.32
• Purity: 99.18% (May vary between batches)
• Formula: C₁₇H₁₅F₆N₅O
• SMILES: FC(F)(F)c1ccc(NC(=O)N2CCN(CC2)c2ncccc2C(F)(F)F)nc1
• Target: TRP/TRPV Channel
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (9.54 mM);DMSO:100 mg/mL (238.48 mM)

Bioactivity

• Target IC50:
  TRPV1 (human):65 nM |TRPV1 (rat):102 nM
• In Vivo:
  TRPV1 antagonist, JNJ-17203212, reduces sensitivity to luminal distension in both an acute, noninflammatory and a chronic, post-inflammatory rodent model of colonic hypersensitivity. TRPV1 is involved in the pathogenesis of visceral hypersensitivity and that JNJ-17203212 may be a potential therapeutic agent for functional bowel disorders characterized by abdominal hypersensitivity, such as irritable bowel syndrome.
• Animal Research:
  Colonic sensitivity was assessed via quantification of VMR to CRD in rats following a single, oral administration of JNJ-17203212 (3, 10 or 30 mg/kg) or vehicle.

Storage & Handling

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

Alternative Names

pain, migrainem, JNJ17203212, JNJ-17203212, JNJ 17203212, inhibit, Inhibitor, management, Transient receptor potential channels, TRPV1, TRPVChannel, TRPV Channel, TRPChannel, TRP Channel

Compound Identifiers

PubChem CID

11339118