RGNCY-0006 (V116517, TRPV1 antagonist)

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A novel TRPV1 (Transient Receptor Potential Vanilloid) antagonist (35nM) that was evaluated in pharmacokinetic, efficacy, and body temperature study. Data suggests that this compound should be evaluated further in human clinical trials for pain management.

SMILES: OC[C@@H](O)C1=CN=C(C2=CCN(C(NC3=CC=C(C(F)(F)F)C=N3)=O)CC2)C(Cl)=C1

Systematic Name: (S)-3-chloro-5-(1,2-dihydroxyethyl)-N-(5-(trifluoromethyl)pyridin-2-yl)-5',6'-dihydro-[2,4'-bipyridine]-1'(2'H)-carboxamide

Molecular Weight: 442.82

Formula: C19H18ClF3N4O3

Reference: Tafesse, Laykea, et al. "Structure–Activity Relationship Studies and Discovery of a Potent Transient Receptor Potential Vanilloid (TRPV1) Antagonist 4-[3-Chloro-5-[(1 S)-1, 2-dihydroxyethyl]-2-pyridyl]-N-[5-(trifluoromethyl)-2-pyridyl]-3, 6-dihydro-2 H-pyridine-1-carboxamide (V116517) as a Clinical Candidate for Pain Management." Journal of Medicinal Chemistry 57.15 (2014): 6781-6794.

PMID: 25057800

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Tags: TRPV1, RGNCY-0006, V116517, Pain