APD597 is a GPR119 agonist intended for the treatment of type 2 diabetes, with EC50 of 46 nM for hGPR119.
CAS：897732-93-3
分子式：C21H29N5O6S
分子量：479.55
纯度：98%
存储：Store at -20°C

Background:

APD597 is a GPR119 agonist intended for the treatment of type 2 diabetes, with EC50 of 46 nM for hGPR119.IC50 value: 46 nM (EC50) [1]Target: hGPR119The design and synthesis of a second generation GPR119-agonist clinical candidate for the treatment of diabetes is described. APD597 was selected for preclinical development based on a good balance between agonist potency, intrinsic activity and in particular on its good solubility and reduced drug-drug interaction potential. [1]

参考文献:
[1]. Buzard DJ, et al. Discovery and optimization of 5-fluoro-4,6-dialkoxypyrimidine GPR119 agonists. Bioorg Med Chem Lett. 2014 Sep 1;24(17):4332-4335.
[2]. Semple G, et al. Discovery of a second generation agonist of the orphan G-protein coupled receptor GPR119 with an improvedprofile. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1750-1755.
[3]. Huan Y, et al. The dual DPP4 inhibitor and GPR119 agonist HBK001 regulates glycemic control and beta cell function ex and in vivo. Sci Rep. 2017 Jun 28;7(1):4351.