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GSK137647A

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Chemical Structure| 349085-82-1 同义名 : GSK 137647
CAS号 : 349085-82-1
货号 : A115691
分子式 : C16H19NO3S
纯度 : 99%+
分子量 : 305.392
MDL号 : MFCD02007969
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(343.82 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 FFA4 (GPR120) is a potential 7TM receptor involved in long-chain fatty acid-stimulated secretion of antidiabetic hormone glucagon-like peptide-1 (GLP1). GSK137647A is a selective FFA4 agonist with pEC50 values of 6.3, 6.2, and 6.1 for human, mouse, and rat FFA4, respectively. GSK137647A dose-dependently increased high glucose (25mM)-stimulated insulin secretion from MIN6 mouse insulinoma cells. Treatment of human intestinal cell line NCI-H716 with GSK137647A (100μM) resulted in a modest increase in GLP-1 secretion[2]. Incubation with 50μM GSK137647A induced the release of active GLP-1 by freshly isolated mouse circumvallate papillae[3]. Supplementation with GSK137647A (20mg/kg) every 2 days for 4 weeks ameliorated fat diet-induced glucose intolerance and insulin insensitivity in WT mice but not GPR120 knockout mice[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.27mL

0.65mL

0.33mL

16.37mL

3.27mL

1.64mL

32.74mL

6.55mL

3.27mL
参考文献

[1]Sparks SM, Chen G, et al. Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). Bioorg Med Chem Lett. 2014 Jul 15;24(14):3100-3.

[2]Sparks SM, Chen G, Collins JL, et al. Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). Bioorg Med Chem Lett. 2014;24(14):3100-3103. doi:10.1016/j.bmcl.2014.05.012

[3]Martin C, Passilly-Degrace P, Chevrot M, et al. Lipid-mediated release of GLP-1 by mouse taste buds from circumvallate papillae: putative involvement of GPR120 and impact on taste sensitivity. J Lipid Res. 2012;53(11):2256-2265. doi:10.1194/jlr.M025874

[4]Wang Y, Xie T, Zhang D, Leung PS. GPR120 protects lipotoxicity-induced pancreatic β-cell dysfunction through regulation of PDX1 expression and inhibition of islet inflammation. Clin Sci (Lond). 2019;133(1):101-116. Published 2019 Jan 11. doi:10.1042/CS20180836