AR453588 is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC50 of 42 nM. AR453588 shows anti-hyperglycemic activity.
体内研究
AR453588 (3-30 mg/kg; p.o) lowers post-prandial glucose in normal C57BL/6J mice.
AR453588 (3-30 mg/kg; p.o.; once-daily for 14 days) shows anti-hyperglycemic activity in a dose-ranging 14 day ob/ob mouse.
AR453588 (10 mg/kg; p.o.) treatment shows that the Tmax, AUCinf, Vss, Cmax and F are 1.0 mL/min/kg, 4.65 h μg /mL, 1.67 μg /mL and 60.3%, respectively.
AR453588 (1 mg/kg; i.v.) treatment shows that the CL, AUCinf, Vss, and t1/2 are 21.6 mL/min/kg, 0.77 h μg /mL, 0.746 L/kg and 1.28 hours, respectively.
Animal Model:
Male diabetic ob/ob mice
Dosage:
3, 10, 30 mg/kg
Administration:
Orally once-daily for 14 days
Result:
Lowered the fasted blood glucose from the control animals on day 14 as well as the AUC of the OGTT (oral glucose tolerance tests).
Animal Model:
Male CD-1 mice
Dosage:
10 mg/kg
Administration:
p.o. (Pharmacokinetic Analysis)
Result:
The Tmax, AUCinf, Vss, Cmax and F were 1.0 mL/min/kg, 4.65 h μg /mL, 1.67 μg /mL and 60.3%, respectively.
分子式
C25H25N7O2S2
分子量
519.64
CAS号
1065609-00-8
运输条件
Room temperature in continental US; may vary elsewhere.