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Fasiglifam

CAS No. : 1000413-72-8

MCE 站：Fasiglifam

产品活性：Fasiglifam (TAK-875) 是一种有效的，可口服的，具有选择性的 GPR40 激动剂，EC₅₀ 值为 72 nM。

研究领域：GPCR/G Protein

作用靶点：GPR40

In Vitro: Fasiglifam (TAK-875) (0.01-10 μM) produces a concentration-dependent increase in intracellular IP production in CHO-hGPR40, with EC₅₀ of 0.072 μM.?Fasiglifam (TAK-875) (0.1-10 μM) dose-dependently augments intracellular IP production in CHO cells. Fasiglifam (TAK-875) (3-30 μM) concentration-dependently augments [Ca²⁺]_i. In the presence of 10 mM glucose, TAK-875 (0.001-10 μM) dose-dependently stimulats insulin secretion from INS-1 833/15 cells.

In Vivo: Fasiglifam (TAK-875) (10 mg/kg, p.o.) increases plasma insulin levels in ZDF rats. Fasiglifam (TAK-875) (30 mg/kg, p.o.) improves fasting hyperglycemia without affecting fasting normoglycemia. Fasiglifam (TAK-875) at 30 mg/kg, which is a 3- to 10-fold higher dose compared with the dose that improved glucose tolerance in diabetic rats, does not alter fasting glucose levels in SD rats with normal glucose homeostasis. Likewise, Fasiglifam (TAK-875) does not significantly alter insulin secretion in SD rats with normal fasting glucose levels .

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