GSK256073 是一种有效的、选择性的、口服活性的 GPR109A 激动剂，是一种持久的 HCA2 激动剂，其 pEC50 为 7.5 (Human HCA2)。GSK256073 可通过抑制脂降解而明显改善葡萄糖稳态，具有研究 2 型糖尿病 (T2DM) 和血脂异常的潜力。
货号:ajcx17036
CAS:862892-90-8
分子式:C10H13ClN4O2
分子量：256.69
溶解度:Soluble in DMSO
纯度：98%
存储：Store at -20°C
库存：现货

Background:

GSK256073 is a potent, selective and orally active GPR109A agonist and a long-lasting and non-flushing HCA2 full agonist with a pEC50 of 7.5 (human HCA2). GSK256073 acutely improves glucose homeostasis via inhibition of lipolysis and has the potential for the study of type 2 diabetes mellitus (T2DM)and dyslipidemia[1][2]. GPR109A: G-protein coupled receptor 109A; HCA2: hydroxy-carboxylic acid receptor 2

[1]. Dobbins RL, et al. GSK256073, a selective agonist of G-protein coupled receptor 109A (GPR109A) reduces serum glucose in subjects with type 2 diabetes mellitus.Diabetes Obes Metab. 2013 Nov;15(11):1013-21. [2]. Sprecher D, et al. Discovery and characterization of GSK256073, a non-flushing hydroxy-carboxylic acid receptor 2 (HCA2) agonist.Eur J Pharmacol. 2015 Jun 5;756:1-7.