AMG-333

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AMG-333 (AMG333, AMG 333) 是一种新型强效、高选择性 TRPM8 拮抗剂，对 hTRPM8 和 rTRPM8 的 IC50 分别为 13 nM 和 20 nM。

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.

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AMG333 | AMG 333

Membrane Transporter/Ion Channel

TRP/TRPV Channel

TRP/TRPV Channel

Neurological Disease

Migraine

1416799-28-4

453.325

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