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ARRY-403(AMG-151)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CAS NO:1304015-76-6
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
50mg电议
500mg电议

产品介绍

ARRY-403, formerly known as AMG-151, is an orally bioavailable allosteric glucokinase (GK) activator developed for the treatment of type 2 diabetes mellitus (T2DM). ARRY-403 has many favorable physicochemical characteristics and ADME properties (low potential to cause drug–drug interactions (DDIs). ARRY-403 potently activates human glucokinase (GK) in vitro (EC50 = 79 nM at 5 mM glucose), with an S0.5 = 0.93 mM glucose (ARRY-403 at 5 mM) and Vmax = 134% compared to the no activator control. It possesses good in vitro drug-like properties (aqueous solubility, cell permeability, low low potential for drug-drug interactions, low predicted hepatic clearance), and selectivity against broad panels of receptors and enzymes. References: Katz L, Manamley N, Snyder WJ, Dodds M, Agafonova N, Sierra-Johnson J, Cruz M, Kaur P, Mudaliar S, Raskin P, Kewalramani R, Pellacani A. AMG 151 (ARRY-403), a novel glucokinase activator, decreases fasting and postprandial glycaemia in patients with type 2 diabetes. Diabetes Obes Metab. 2016 Feb;18(2):191-5. doi: 10.1111/dom.12586. Epub 2015 Dec 14. PubMed PMID: 26434934.

纯度:≥98%

CAS:1304015-76-6