|4-((6-((6-甲基磺酰基-2-甲基吡啶-3-基)氨基)-5-甲氧基嘧啶-4-基)氧基)哌啶-1-羧酸异丙酯|CsnPharm

CAS No.: 897732-93-3

APD597 Catalog No. CSN18543

Synonyms: JNJ-38431055

APD597 is an agonist of GPR119 with EC50 of 46 nM and is used for the treatment of type 2 diabetes.

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生物活性

实验方案

技术信息

生物活性

描述GPR119 is a class A GPCR expressed on pancreatic β-cells and certain enteroendocrine cells which upon activation with an agonist, increases insulin secretion in response to rising glucose levels. APD597, an anti-type 2 diabetic drug, is a GPR119 agonist with EC₅₀ values of 46 and 421 nM for hGPR119 and rGPR119, respectively^[3]. In normal lean mice during an oGTT (oral glucose tolerance test), treatment with APD597 (1 and 10 mg/kg PO) significantly reduced the AUC_glu. In addition, in the Sprague–Dawley rat treatment with APD597 (3 – 30 mg/kg PO) significantly improved glucose handling and markedly reduced the AUC_glu during oGTT^[4].
参考文献

[1] Buzard DJ, Kim SH, et al. Discovery and optimization of 5-fluoro-4,6-dialkoxypyrimidine GPR119 agonists. Bioorg Med Chem Lett. 2014 Sep 1;24(17):4332-5.
[2] Semple G, Lehmann J, et al. Discovery of a second generation agonist of the orphan G-protein coupled receptor GPR119 with an improved profile. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1750-5.
[3] Buzard DJ, Kim SH, Lehmann J, et al. Discovery and optimization of 5-fluoro-4,6-dialkoxypyrimidine GPR119 agonists. Bioorg Med Chem Lett. 2014 Sep 1;24(17):4332-5
[4] Semple G, Lehmann J, et al. Discovery of a second generation agonist of the orphan G-protein coupled receptor GPR119 with an improved profile

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0853 mL
- 10.4264 mL
- 20.8529 mL
- 5 mM
- 0.4171 mL
- 2.0853 mL
- 4.1706 mL
- 10 mM
- 0.2085 mL
- 1.0426 mL
- 2.0853 mL

技术信息

CAS号

897732-93-3

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H29N5O6S

运输

蓝冰

分子量

479.55

别名

JNJ-38431055

溶解度

DMSO	180.0 mg/mL (375.4 mM) warming
Water	insoluble

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