APD597

An agonist of GPR119

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库存: 现货

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5mg

￥1300.00

1040.00

- +
10mg

￥2400.00

1920.00

- +
50mg

￥6475.00

5180.00

- +
100mg

￥10787.00

8630.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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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.