Fasiglifam

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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 14nM。

A potent, selective, orally bioavailable GPR40 (FFA1) agonist with EC50 of 14 nM; exhibited excellent agonist potency selectivity over other FFA receptors (GPR41, GPR43, and GPR120, EC50s>10 uM); shows potent plasma glucose-lowering action and insulinotropic action in vivo.Diabetes Phase 3 Discontinued(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 .

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.

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 .

Fasiglifam | TAK 875 | TAK875

GPCR/G Protein

FFAR

GPR40(FFA1)

Metabolic Disease

Diabetes

1000413-72-8

524.6252

C29H32O7S

>98% (HPLC)

DMSO: ≥ 128 mg/mL

CC1=C(C2=CC(COC3=CC=C([C@H](CC(O)=O)CO4)C4=C3)=CC=C2)C(C)=CC(OCCCS(C)(=O)=O)=C1

3-Benzofuranacetic acid, 6-[[2',6'-dimethyl-4'-[3-(methylsulfonyl)propoxy][1,1'-biphenyl]-3-yl]methoxy]-2,3-dihydro-, (3S)-

(-20℃)

With Ice Pack

≥ 2 years