产品
编 号：F659441
分子式：C25H26ClN7O2S2
分子量：556.1
分子式：C25H26ClN7O2S2
分子量：556.1
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CAS No: 1065606-97-4
产品详情
生物活性：
AR453588 hydrochloride is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC50 of 42 nM. AR453588 hydrochloride shows anti-hyperglycemic activity.
体内研究：
AR453588 hydrochloride (3-30 mg/kg; p.o) lowers post-prandial glucose in normal C57BL/6J mice.AR453588 hydrochloride (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 hydrochloride (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 hydrochloride (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
AR453588 hydrochloride is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC50 of 42 nM. AR453588 hydrochloride shows anti-hyperglycemic activity.
体内研究：
AR453588 hydrochloride (3-30 mg/kg; p.o) lowers post-prandial glucose in normal C57BL/6J mice.AR453588 hydrochloride (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 hydrochloride (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 hydrochloride (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
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