• 产品描述： GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC50s of 7.32 and 5.46, respectively. GW9508 shows ~100-fold selectivity for GPR40 over GPR120. GW9508 is inactive against other GPCRs, kinases, proteases, integrins and PPARs. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (KATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities

• 靶点： pEC50: 7.32 (GPR40) and 5.46 (GPR120)

• 体外研究： GW9508 stimulates intracellular Ca2+ mobilization in HEK-293 cells expressing GPR40 (pEC50 of 7.32) or GPR120 (pEC50 of 5.46), but not in the parent HEK-293 cell line.
  GW9508 produces a concentration-dependent increase (pEC50 of 6.14) in glucose-stimulated insulin secretion at high glucose levels (25 mM). This resulted in a 1.52-fold increase in insulin secretion with 20 μM GW9508 in the presence of 25 mM glucose, compared with 25 mM glucose alone. The ability of GW9508 (10 μM) to enhance insulin secretion from MIN6 cells is significantly enhanced as glucose concentrations are increased.
  GW9508 inhibits CCL17 and CCL5 expression in a pertussis toxin-sensitive manner. The inhibitory effect by GW9508 is abrogated by depletion of GPR40 with RNA interference. GW9508 further suppresses expression of IL-11, IL-24, and IL-33 induced in HaCaT cells by TNF-α and IFN-γ. GW9508 also inhibits CCL5 and CXCL10 production by normal human epidermal keratinocytes.

• 体内研究： Administration of GW9508 200 (μM) topically to the skin suppresses ear swelling in a repeated hapten application model (BALB/c and C57BL/6 mice) and contact hypersensitivity with downregulation of CCL5 and CXCL10, respectively.

• 参考文献：
  1. Briscoe CP, 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. 2. Fujita T, et al. 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. 3. Zhao YF, 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, 198(3), 533-540. 4. Suski M, et al. Anti-atherosclerotic action of GW9508 - Free fatty acid receptors activator - In apoE-knockout mice. Pharmacol Rep. 2019 Aug;71(4):551-555.

• 溶解性： Soluble  in  DMSO

• 保存条件： 2-8℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.878 ml	14.392 ml	28.784 ml
  5 mM	0.576 ml	2.878 ml	5.757 ml
  10 mM	0.288 ml	1.439 ml	2.878 ml
  50 mM	0.058 ml	0.288 ml	0.576 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *