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