885101-89-3
885101-89-3 结构式
基本信息
4-[[(3-苯氧基苯基)甲基]氨基]苯丙酸
3-(4-((3-苯氧基苄基)氨基)苯基)丙酸
CS-618
GPR40 Agonist
GW9508, >=99%
GW9508 USP/EP/BP
885101-89-3(GW9508)
GW-9508
GW9508
GW 9508
4-(3-Phenoxybenzylamino)phenylpropionic acid
GPR40 Agonist - CAS 885101-89-3 - Calbiochem
3-(4-((3-Phenoxybenzyl)aMino)phenyl)propanoic acid
物理化学性质
应用领域
常见问题列表
pEC50: 7.32 (GPR40) and 5.46 (GPR120)
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.
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.