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GSK137647A
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。
GSK137647A图片
CAS NO:349085-82-1
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 305.39
Formula C16H19NO3S
CAS No. 349085-82-1
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: ≥ 30 mg/mL
Water: N/A
Ethanol: N/A
SMILES Code O=S(C1=CC=C(OC)C=C1)(NC2=C(C)C=C(C)C=C2C)=O
Synonyms GSK137647; GSK-137647; GSK 137647; GSK137647A; GSK-137647A; GSK 137647A
实验参考方法
In Vitro

In vitro activity: GSK137647A, a diarylsulfonamide analog, is a novel, potent and selective agonists of the free fatty acid receptor 4 (FFA4/GPR120) with pEC50 of 6.3, 6.2, and 6.1 for human, mouse and rat FFA4, respectively. GSK137647A is selective for GPR120 over a panel of 61 other targets, including other FFARs. The free fatty acid receptor 4 (FFA4/GPR120) is a member of the G protein-coupled receptor family and is a potential 7TM (transmembrane) receptor that is 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.


Kinase Assay: GSK137647A is a selective FFA4 agonist, with pEC50 of 6.3, 6.2, and 6.1 for human, Mouse and Rat FFA4, respectively. The pEC50s for Human , Mouse and Rat FFA1/2/3 are < 4.5. GSK137647A is evaluated against a panel of 65 targets in both full curve functional and binding assays and was shown to provide at least 100-fold selectivity against the panel which included 41 G-protein-coupled receptors (GPCRs), including additional members of the free fatty acid receptors (FFA1, FFA2, and FFA3). GSK137647A produces a concentration-dependent increase in glucose stimulated insulin secretion under high glucose conditions (25 mM).

In Vivo
Animal model
Formulation & Dosage
References Bioorg Med Chem Lett. 2014 Jul 15;24(14):3100-3.