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CAS No. : 1103523-24-5
MCE 国际站:AMG7703
产品活性:AMG7703 是一种 FFA2 (GPR43) 的选择性变构激动剂,FFA2 是短链脂肪酸 (SCFA)、醋酸盐 (acetate) 和丙酸 (methylacetic) 的受体。AMG7703可用于炎症和代谢的研究。
研究领域:GPCR/G Protein
作用靶点:Free Fatty Acid Receptor
In Vitro: AMG7703 (phenylacetamide 1) (30 μM) shows selectivity on FFA2 (GPR43) over FFA1 (GPR40) and FFA3 (GPR41) with in Chinese hamster ovary cells.
AMG7703 (0.041, 0.123, 0.37, 1.11 μM) acts as an FFA2 allosteric agonist, activates Gαi coupled signaling pathway.
AMG7703 (1, 3, 10, 30 μM) results in Gαi-dependent inhibition of lipolysis in adipocytes (3T3L1).
AMG7703 (0.041, 0.123, 0.37, 1.11 μM) exhibits allosteric activity and inhibits Gαi-coupled cAMP with IC50 values of 0.7 μM (hFFA2) and 0.96 μM (mFFA2), respectively; as for Gαq-coupled aequorin inhibition, with EC50s of 0.45 μM (hFFA2) and 1.27 μM (mFFA2), respectively.
AMG7703 (0-1 μM) shows the positive cooperating effect of acetate and stimulates calcium mobilization in a concentration-dependent manner in CHO cell stably expressing hFFA2 and aequorin.
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货号: HY-114011
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