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GSK 137647
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GSK 137647图片
CAS NO:349085-82-1
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
GSK 137647 (GSK 137647) 是一种有效的选择性游离脂肪酸受体 4 (FFA4) 激动剂,对于人类、小鼠和大鼠 FFA4 的 pEC50 值分别为 6.3、6.2 和 6.1,对于所有三个物种的 FFA1,pEC50 值< 4.5,分别为 FFA2 和 FFA3。
Cas No.349085-82-1
别名4-甲氧基-N-(2,4,6-三甲基苯)苯磺酰胺,GSK 137647
化学名N-mesityl-4-methoxybenzenesulfonamide
Canonical SMILESCC1=CC(C)=C(NS(C2=CC=C(OC)C=C2)(=O)=O)C(C)=C1
分子式C16H19NO3S
分子量305.39
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
储存条件Store at RT
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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].

References:
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.