AMG-333( AMG333 | AMG 333 )

Catalog No. M11738 CAS No. 1416799-28-4

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

AMG-333
Note

Research use only, not for human use.
Brief Description

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.
Description

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.
In Vitro

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In Vivo

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Synonyms

AMG333 | AMG 333
Pathway

Membrane Transporter/Ion Channel
Target

TRP/TRPV Channel
Recptor

TRP/TRPV Channel
Research Area

Neurological Disease
Indication

Migraine

CAS Number

1416799-28-4
Formula Weight

453.325
Molecular Formula

C20H12F5N3O4
Purity

>98% (HPLC)
Solubility

DMSO : ≥ 125 mg/mL 275.74 mM
SMILES

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
Chemical Name

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

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

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