GSK 137647

A selective GPR120 agonist

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库存: 现货

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5mg

￥462.00

370.00

- +
10mg

￥737.00

590.00

- +
25mg

￥1525.00

1220.00

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50mg

￥2712.00

2170.00

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100mg

￥4362.00

3490.00

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货号: ajci16594
CAS: 349085-82-1
别名: 4-甲氧基-N-(2,4,6-三甲基苯)苯磺酰胺,GSK 137647
分子式: C16H19NO3S
分子量: 305.39
纯度: >98%
溶解度: DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS(pH 7.2) (1:2): 0.25 mg/ml,Ethanol: 1 mg/ml
储存: Store at RT
库存: 现货

Background

Target: FFA4/GPR120

IC50: N/A

GSK137647A is potent and selective FFA4/GPR120 agonist with pEC50 values of 6.3, 6.2, and 6.1 at the human, mouse and rat receptor, respectively [1]. The free fatty acid receptor 4 (FFA4/GPR120), a member of the G protein-coupled receptor family, is a potential 7TM receptor involved in long-chain fatty acid-stimulated glucagon-like peptide-1 (GLP-1) secretion. FFA4 is highly expressed in the intestinal endocrine cell line STC-1 and the intestine [1]. GLP-1 regulates multiple physiological functions including eating behavior [2].

In vitro: GSK137647A (50 μM) induced a concentration-dependent increase in glucose (25 mM)-stimulated insulin secretion in MIN6 mouse insulinoma cell line [1]. In addition, GSK137647A (100 μM) induced a modest increase in GLP-1 secretion in the human intestinal cell line NCI-H716. Moreover, GSK137647A induced intracellular calcium accumulation in U2OS cells [1].

In vivo: GSK137647A (50 μM) induced active GLP-1 release by mouse circumvallate papillae (CVPs) [2].

参考文献:
1.? Sparks SM, Chen G, Collins JL, Danger D, Dock ST, Jayawickreme C, et al. Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). Bioorg Med Chem Lett. 2014;24(14):3100-3.
2.? Martin C, Passilly-Degrace P, Chevrot M, Ancel D, Sparks SM, Drucker DJ, 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):2256-65.