GW9508

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Chemical Structure| 885101-89-3 同义名 : -
CAS号 : 885101-89-3
货号 : A144748
分子式 : C22H21NO3
纯度 : 99%+
分子量 : 347.41
MDL号 : MFCD09753282
存储条件：

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：

2% DMSO+40% PEG 300+2% Tween 80+water 2 mg/mL

生物活性
描述 G protein-coupled receptors are seven-transmembrane proteins that can be activated by free fatty acid. GW950 is a small-molecule agonist of GPR40 and GPR120 with pEC50 values of 7.32±0.03 and 5.46±0.09, respectively. It also induced intracellular Ca2+ mobilization in HEK293 cells expressing GPR40 (pEC50=7.32±0.03) or GPR120 (pEC50=5.46±0.09). In MIN6 mouse insulinoma cell line, GW9508 induced a concentration-dependent increase in high glucose (25mM)-stimulated insulin secretion with a pEC50 of 6.14±0.03[3]. The administration of 200mM GW9508 to the ear 1h before each DNFB treatment significantly attenuated ear swelling in BALB/c mice compared with the controls. GW9508 treatment also significantly reduced the expression of CCL5 and eosinophils infiltrating in the skin compared to the vehicle-treated group. In C57BL/6 mice subjected to DNFB-induced CHS, application of GW9508 at 10-100μM suppressed ear swelling in a dose-dependent manner[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.88mL

0.58mL

0.29mL

14.39mL

2.88mL

1.44mL

28.78mL

5.76mL

2.88mL
参考文献

[1]Zhao YF, Pei J, et al. Activation of ATP-sensitive potassium channels in rat pancreatic beta-cells by linoleic acid through both intracellular metabolites and membrane receptor signalling pathway. J Endocrinol. 2008 Sep;198(3):533-40.

[2]Briscoe CP, Peat AJ, et al. Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules. Br J Pharmacol. 2006 Jul;148(5):619-28. Epub 2006 May 15.

[3]Briscoe CP, Peat AJ, McKeown SC, et al. Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules. Br J Pharmacol. 2006;148(5):619-628. doi:10.1038/sj.bjp.0706770

[4]Fujita T, Matsuoka T, Honda T, Kabashima K, Hirata T, Narumiya S. A GPR40 agonist GW9508 suppresses CCL5, CCL17, and CXCL10 induction in keratinocytes and attenuates cutaneous immune inflammation. J Invest Dermatol. 2011;131(8):1660-1667. doi:10.1038/jid.2011.123