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Chemical Structure : V-116517
Catalog No.: PC-61534Not For Human Use, Lab Use Only.
V-116517 is a novel potent, selective, oral bioavailable TRPV1 antagonist with IC50 of 35.1 nM.
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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
| M.Wt | 442.82 | |
| Formula | C19H18ClF3N4O3 | |
| Appearance | Solid | |
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| Solubility |
10 mM in DMSO |
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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.
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