1073616-61-1

1073616-61-1 structure

Name: V-116517
Chemical Name: 3-Chloro-5-[(1S)-1,2-dihydroxyethyl]-N-[5-(trifluoromethyl)-2-pyridinyl]-3',6'-dihydro-2,4'-bipyridine-1'(2'H)-carboxamide
CAS Number: 1073616-61-1
Molecular Formula: C₁₉H₁₈ClF₃N₄O₃
Molecular Weight: 442.819
Catalog: Signaling Pathways Membrane Transporter/Ion Channel TRP Channel
Create Date: 2020-01-11 11:07:52
Modify Date: 2024-01-04 19:23:57
V-116517 is a novel potent, selective, oral bioavailable TRPV1 antagonist with IC50 of 35.1 nM; shows high selectivity for TRPV1 over TRPV3 and TRPV4 (>10 uM) in a panel of 66 ion channels, receptors, transporters; dose-dependently reverses thermal hyperalgesia with ED50 of 2 mg/kg (p.o.) in acute inflammatory CFA model; shows excellent aqueous solubility, metabolic stability, oral bioavailability in multiple species, and excellent efficacy in a variety of animal pain models. Pain Phase 2 Clinical

Name	3-Chloro-5-[(1S)-1,2-dihydroxyethyl]-N-[5-(trifluoromethyl)-2-pyridinyl]-3',6'-dihydro-2,4'-bipyridine-1'(2'H)-carboxamide
Synonyms	3-Chloro-5-[(1S)-1,2-dihydroxyethyl]-N-[5-(trifluoromethyl)-2-pyridinyl]-3',6'-dihydro-2,4'-bipyridine-1'(2'H)-carboxamide [2,4'-Bipyridine]-1'(2'H)-carboxamide, 3-chloro-5-[(1S)-1,2-dihydroxyethyl]-3',6'-dihydro-N-[5-(trifluoromethyl)-2-pyridinyl]-

Description	V-116517 is a novel potent, selective, oral bioavailable TRPV1 antagonist with IC50 of 35.1 nM; shows high selectivity for TRPV1 over TRPV3 and TRPV4 (>10 uM) in a panel of 66 ion channels, receptors, transporters; dose-dependently reverses thermal hyperalgesia with ED50 of 2 mg/kg (p.o.) in acute inflammatory CFA model; shows excellent aqueous solubility, metabolic stability, oral bioavailability in multiple species, and excellent efficacy in a variety of animal pain models. Pain Phase 2 Clinical
References	References 1. Tafesse L, et al. J Med Chem. 2014 Aug 14;57(15):6781-94. 2. Arendt-Nielsen L, et al. Pain. 2016 Sep;157(9):2057-67. View Related Products by Target TRP Channel Pain