V116517 | TRPV1 inhibitor | Probechem Biochemicals

Chemical Structure : V116517

V116517 (V-116517)

Catalog No.: PC-61534Not For Human Use, Lab Use Only.

V116517 is a potent, selective, oral bioavailable TRPV1 antagonist with IC50 of 35.1 nM.

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Biological Activity

V116517 is a potent, selective, oral bioavailable TRPV1 antagonist with IC50 of 35.1 nM.
V116517 shows high selectivity for TRPV1 over TRPV3 and TRPV4 (>10 uM) in a panel of 66 ion channels, receptors, transporters.
V116517 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.

Physicochemical Properties

M.Wt	442.82
Formula	C19H18ClF3N4O3
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-3-chloro-5-(1,2-dihydroxyethyl)-N-(5-(trifluoromethyl)pyridin-2-yl)-3',6'-dihydro-[2,4'-bipyridine]-1'(2'H)-carboxamide

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.

V116517 (V-116517)

Biological Activity

Physicochemical Properties

References

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