Chemical Structure : AMG-333
Catalog No.: PC-35612Not For Human Use, Lab Use Only.
AMG-333 (AMG333, AMG 333) is a novel potent, highly selective TRPM8 antagonist with IC50 of 13 nM and 20 nM for hTRPM8 and rTRPM8, respectively.
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AMG-333 (AMG333, AMG 333) is a novel potent, highly selective TRPM8 antagonist with IC50 of 13 nM and 20 nM for hTRPM8 and rTRPM8, respectively; displays high selectivity over other TRP channels (IC50>20 uM, TRPV1/V3/V4/A1); exhibits statistically significant and dose-dependent prevention of icilin-induced rat WDS, at 0.6, 1 and 3 mg/kg, inhibits cold-induced increase in blood pressure in the rat CPT in a dose-dependent manner with 1 and 3 mg/kg producing significant inhibition with an ED90 of 1.1 mg/kg, also fully blocks the cold pressor response at 3 mg/kg.
Migraine
Phase 1 Clinical
M.Wt | 453.325 | |
Formula | C20H12F5N3O4 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
1. Horne DB, et al. J Med Chem. 2018 Aug 27. doi: 10.1021/acs.jmedchem.8b00518.
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