TAK-875 | CAS:1000413-72-8

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Name:TAK-875; Fasiglifam
Cat. No. :CS-0282
CAS No. :1000413-72-8
Formula:C29H32O7S
M. Wt. : 524.63
Solubility:DMSO: ≥ 128 mg/mL

TAK-875 is a potent, selective and orally bioavailable GPR40 agonist with EC50 of 72 nM.IC50 & Target: EC50: 72 nM (GPR40)In Vitro: TAK-875 (0.01-10 μM) produces a concentration-dependent increase in intracellular IP production in CHO-hGPR40, with EC50 of 0.072 μM. TAK-875 (0.1-10 μM) dose-dependently augments intracellular IP production in CHO cells[1]. 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[2].In Vivo: TAK-875 (10 mg/kg, p.o.) increases plasma insulin levels in ZDF rats. TAK-875 (30 mg/kg, p.o.) improves fasting hyperglycemia without affecting fasting normoglycemia. 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, TAK-875 does not significantly alter insulin secretion in SD rats with normal fasting glucose levels [1].

Tsujihata Y,et al. TAK-875, an orally available G protein-coupled receptor 40/free fatty acid receptor 1 agonist, enhances glucose-dependent insulin secretion and improves both postprandial and fasting hyperglycemia in type 2 diabetic rats.J Pharmacol Exp Yoshiyuki Tsujihata, et al. TAK-875, an Orally Available GPR40/FFA1 Agonist Enhances Glucose-Dependent Insulin Secretion and Improves Both Postprandial and Fasting Hyperglycemia in Type 2 Diabetic Rats. JPET July 13, 2011