AR453588

AR453588 is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC 50 of 42 nM. AR453588 shows anti-hyperglycemic activity. In Vivo 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 T max , AUC inf , Vss, C max 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, AUC inf , Vss, and t 1/2 are 21.6 mL/min/kg, 0.77 h μg /mL, 0.746 L/kg and 1.28 hours, respectively . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 T max , AUC inf , Vss, C max and F were 1.0 mL/min/kg, 4.65 h μg /mL, 1.67 μg /mL and 60.3%, respectively. Form:Solid

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