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GW9508

CAS No. : 885101-89-3

MCE 站：GW9508

产品活性：GW9508 是一种有效的选择性 G 蛋白偶联受体 FFA1 (GPR40) 和 GPR120 激动剂，pEC₅₀ 值分别为 7.32 和 5.46。GW9508 对 GPR40 的选择性是 GPR120 的 100 倍左右，对其他 GPCR，激酶，蛋白酶，整联蛋白和 PPAR 无活性。GW9508 是一种葡萄糖敏感性胰岛素促分泌剂和 ATP 敏感性钾 (K_ATP) 通道开放剂。GW9508 具有抗炎和抗动脉粥样硬化活性。

研究领域：GPCR/G Protein  |  Membrane Transporter/Ion Channel

作用靶点：GPR40  |  Potassium Channel

In Vitro: 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.

In Vivo: 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.

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