| Identification | Back Directory | [Name]
AMG-333 | [CAS]
1416799-28-4 | [Synonyms]
AMG-333
AMG333;AMG 333
3-Pyridinecarboxylic acid, 6-[[[(S)-(3-fluoro-2-pyridinyl)[3-fluoro-4-(trifluoromethoxy)phenyl]methyl]amino]carbonyl]- | [Molecular Formula]
C20H12F5N3O4 | [MDL Number]
MFCD31813692 | [MOL File]
1416799-28-4.mol | [Molecular Weight]
453.32 |
| Hazard Information | Back Directory | [Uses]
AMG 333 is an orally active and highly selective TRPM8 antagonist with an IC50 of 13 nM. | [in vivo]
AMG 333 (0.6-3 mg/kg, p.o., single dose) dose-dependently inhibits wet-dog shake behavior in the Icilin (HY-11062)-induced wet-dog shake Sprague?Dawley rat model, demonstrating that AMG 333 effectively blocks the TRPM8 target[1].
AMG 333 (1-3 mg/kg, p.o., single dose) dose-dependently blocks blood pressure elevation in the cold stimulation-induced blood pressure elevation Sprague?Dawley rat model, indicating that AMG 333 effectively acts on the TRPM8 target[1]. | Animal Model: | Icilin (HY-11062)-induced wet-dog shake (WDS) behavior in Sprague?Dawley rat model[1] | | Dosage: | 0.6, 1, 3 mg/kg | | Administration: | Oral gavage (p.o.), single dose | | Result: | Demonstrated significant dose-dependent inhibition;
3 mg/kg fully inhibited WDS. |
| Animal Model: | Cold stimulation-induced blood pressure elevation Sprague?Dawley rat model[1] | | Dosage: | 1, 3 mg/kg | | Administration: | Oral gavage (p.o.), single dose | | Result: | Showed significant inhibition of cold-induced blood pressure elevation at 1 mg/kg and 3 mg/kg;
3 mg/kg fully blocked cold-pressor response. |
| [storage]
Store at -20°C | [References]
[1] Horne DB, et al. Discovery of TRPM8 Antagonist ( S)-6-(((3-Fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic Acid (AMG 333), a Clinical Candidate for the Treatment of Migraine. J Med Chem. 2018 Sep 27;61(18):8186-8201. DOI:10.1021/acs.jmedchem.8b00518 |
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