JNJ-17203212

• CAT Number: I004973
• CAS Number: 821768-06-3
• Molecular Formula: C17H15F6N5O
• Molecular Weight: 419.32
• Purity: ≥95%
• Synonyms: 4-(3-(trifluoromethyl)pyridin-2-yl)-N-(5-(trifluoromethyl)pyridin-2-yl)piperazine-1-carboxamide
• Target: Neuronal Signaling
• Solubility: 10 mM in DMSO
• Storage: Store at +4C
• IC50: 65 nM (human TRPV1), 102 nM (rat TRPV1)
• IUPAC Name: 4-[3-(trifluoromethyl)pyridin-2-yl]-N-[5-(trifluoromethyl)pyridin-2-yl]piperazine-1-carboxamide
• InChI: 1S/C17H15F6N5O/c18-16(19,20)11-3-4-13(25-10-11)26-15(29)28-8-6-27(7-9-28)14-12(17(21,22)23)2-1-5-24-14/h1-5,10H,6-9H2,(H,25,26,29)
• InChIKey: JFRYYGVYCWYIDQ-UHFFFAOYSA-N
• SMILES: C1CN(CCN1C2=C(C=CC=N2)C(F)(F)F)C(=O)NC3=NC=C(C=C3)C(F)(F)F

JNJ-17203212 (Cat No.: I004973) is a potent and selective transient receptor potential vanilloid 1 (TRPV1) antagonist. TRPV1, also known as the capsaicin receptor, plays a crucial role in pain perception, thermoregulation, and inflammation. By blocking TRPV1 activation, JNJ-17203212 is studied for its potential in treating chronic pain, neuropathic pain, and inflammatory disorders. Its ability to modulate nociceptive signaling makes it a valuable tool in pain research and drug discovery, particularly for developing non-opioid analgesic therapies.

Reference

1:Methods Find Exp Clin Pharmacol. 2010 Oct;32(8):557-64. doi: 10.1358/mf.2010.32.8.1507853. A novel TRPV1 receptor antagonist JNJ-17203212 attenuates colonic hypersensitivity in rats.Wiskur BJ,Tyler K,Campbell-Dittmeyer K,Chaplan SR,Wickenden AD,Greenwood-Van Meerveld B, PMID: 21132125 DOI: 10.1358/mf.2010.32.8.1507853 Abstract: This study examined the efficacy of a novel TRPV1 antagonist, JNJ-17203212, in two experimental rat models that exhibit a hypersensitive visceral motor response (VMR) to colorectal distension (CRD). In the first model, intraluminal administration of acetic acid (1% solution) into the distal colon produced an acute colonic hypersensitivity. In the second model, intraluminal administration of 2,4,6-trinitrobenzenesulfonic acid (TNBS) into the distal colon produced a chronic, post-inflammatory colonic hypersensitivity 30 days post-TNBS administration. Throughout this study, 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. Intraluminal administration of acetic acid and TNBS resulted in increased VMR to CRD when compared to controls. In both groups, VMR to CRD was significantly reduced by administration of JNJ-17203212 at 30 mg/kg. The results of this study show that the selective TRPV1 antagonist, JNJ-17203212, reduces sensitivity to luminal distension in both an acute, noninflammatory and a chronic, post-inflammatory rodent model of colonic hypersensitivity. These data indicate that 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.Copyright 2010 Prous Science, S.A.U. or its licensors. All rights reserved.