V-116517

Names

[ Name ]:
V-116517

[Synonym ]:
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]-

Biological Activity

[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

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
679.3±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₉H₁₈ClF₃N₄O₃

[ Molecular Weight ]:
442.819

[ Flash Point ]:
364.6±31.5 °C

[ Exact Mass ]:
442.101959

[ LogP ]:
0.47

[ Vapour Pressure ]:
0.0±2.2 mmHg at 25°C

[ Index of Refraction ]:
1.624

Related Compounds

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