885101-89-3(GW9508)

生物活性靶点体外研究体内研究 885101-89-3(GW9508) 试剂级价格

885101-89-3(GW9508)

CAS号:885101-89-3
英文名:GW9508
中文名:885101-89-3(GW9508)
CBNumber:CB71074937
分子式:C22H21NO3
分子量:347.41
MOL File:885101-89-3.mol

885101-89-3(GW9508)化学性质

熔点 :90-92°C
沸点 :538.4±45.0 °C(Predicted)
密度 :1.222±0.06 g/cm3(Predicted)
储存条件 :2-8°C
溶解度 :DMSO: >20mg/mL
形态 :white powder
酸度系数(pKa) :4.77±0.10(Predicted)
颜色 :Off-white
稳定性 :Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.

安全信息

危险品标志 :Xn,N
危险类别码 :22-37/38-41-50/53
安全说明 :26-39-60-61
危险品运输编号 :UN 3077 9 / PGIII
WGK Germany :3

885101-89-3(GW9508)性质、用途与生产工艺

生物活性 GW9508 是一种有效的选择性 G 蛋白偶联受体 FFA1 (GPR40) 和 GPR40 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 (KATP) 通道开放剂。GW9508 具有抗炎和抗动脉粥样硬化活性。
靶点

pEC50: 7.32 (GPR40) and 5.46 (GPR120)
体外研究

GW9508 stimulates intracellular Ca ²⁺ mobilization in HEK-293 cells expressing GPR40 (pEC ₅₀ of 7.32) or GPR120 (pEC ₅₀ of 5.46), but not in the parent HEK-293 cell line.
GW9508 produces a concentration-dependent increase (pEC ₅₀ 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.
用途 GW9508 is a GPR40 full agonist, used to regulate glucose in rats. Can be applied to the treatment of diabetes type 2. GPR120 selective and potent agonist also used in the treatment of diabetes type 2 due to GPR120鈥檚 ability to mediate GLP-1 secretion, insulin sensitization and anti-obesity effects.