AMG 333

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Chemical Structure| 1416799-28-4 同义名 : -
CAS号 : 1416799-28-4
货号 : A1155029
分子式 : C20H12F5N3O4
纯度 : 99%+
分子量 : 453.32
MDL号 : MFCD31813692
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(264.71 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
描述 AMG 333 is TRPM8 antagonist with IC50 values of 13nM and 20nM for hTRPM8 and rTRPM8, respectively, but no efficiency on mTRPM8. It exhibited statistically significant and dose-dependent prevention of icilin-induced rat wet-dog shakes at 0.6, 1, and 3 mg/kg[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.21mL

0.44mL

0.22mL

11.03mL

2.21mL

1.10mL

22.06mL

4.41mL

2.21mL
参考文献

[1]Horne DB, Biswas K, 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.

[2]Horne DB, Biswas K, Brown J, Bartberger MD, Clarine J, Davis CD, Gore VK, Harried S, Horner M, Kaller MR, Lehto SG, Liu Q, Ma VV, Monenschein H, Nguyen TT, Yuan CC, Youngblood BD, Zhang M, Zhong W, Allen JR, Chen JJ, Gavva NR. 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. Epub 2018 Sep 10. PMID: 30148953.