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AMG-333

Chemical Structure : AMG-333

CAS No.: 1416799-28-4

AMG-333 (AMG333;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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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

Physicochemical Properties

M.Wt 453.325
Formula C20H12F5N3O4
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)-6-(((3-fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic acid

References

1. Horne DB, et al. J Med Chem. 2018 Aug 27. doi: 10.1021/acs.jmedchem.8b00518.

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