AMG-333

Research use only, not for human use.

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.

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

AMG333;AMG 333

Membrane Transporter/Ion Channel

TRP/TRPV Channel

TRP/TRPV Channel

Neurological Disease

Migraine

1416799-28-4

453.33

C20H12F5N3O4

>98% (HPLC)

DMSO : ≥ 125 mg/mL 275.74 mM

O=C(O)C1=CN=C(C(N[C@@H](C2=CC=C(OC(F)(F)F)C(F)=C2)C3=NC=CC=C3F)=O)C=C1

(S)-6-(((3-fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic acid

(-20℃)

With Ice Pack

≥ 2 years