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首页-小分子抑制剂&激动剂-GPCR-Free Fatty Acid Receptor (FFAR)-GSK137647A
GSK137647A

Chemical Structure : GSK137647A

CAS No.: 349085-82-1

GSK137647A (GSK-137647A, GSK137647)

货号: PC-45779Not For Human Use, Lab Use Only.

GSK-137647 (GSK-137647A) is a potent, selective GPR120 (FFA4) agonist with pEC50 of 6.3, >100-fold selectivity over the FFA1, FFA2, and FFA3 receptors.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GSK137647A (GSK137647) is a potent, selective GPR120 (FFA4) agonist with pEC50 of 6.3, >100-fold selectivity over the FFA1, FFA2, and FFA3 receptors.
GSK137647A augments insulin release from rat/mouse islets and rat β-cell line INS-1E.
GSK137647A attenuats both basal and LPS-induced production of IL-6 and CCL2, reduces the phosphorylation of IκBα and nuclear translocation of NFkappa-B p65 subunit (p65) in 3T3-L1 adipocytes.
GSK137647A improves postprandial hyperglycaemia of diabetic mice.

物理化学性质&存储条件

分子量 305.392
分子式 C16H19NO3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 32 mg/mL; H2O: < 0.06 mg/mL (Need ultrasonic and warming)

Chemical Name/SMILES

Benzenesulfonamide,4-methoxy-N-(2,4,6-trimethylphenyl)-

参考文献

1. Sparks SM, et al. Bioorg Med Chem Lett. 2014 Jul 15;24(14):3100-3.

2. Zhang D, et al. Clin Sci (Lond). 2017 Feb 1;131(3):247-260.

3. Hasan AU, et al. Biochem Biophys Res Commun. 2017 Apr 22;486(1):76-82.

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