S87719 |
APD597 |
源叶(MedMol) | 98% |
- 产品描述: 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) Target: hGPR119 The 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.
- 靶点: GPR119;GPR
- 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. 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. 3. 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.
- 溶解性: Soluble in DMSO
- 保存条件: -20°C
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.085 ml 10.426 ml 20.853 ml 5 mM 0.417 ml 2.085 ml 4.171 ml 10 mM 0.209 ml 1.043 ml 2.085 ml 50 mM 0.042 ml 0.209 ml 0.417 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)