AR453588 hydrochloride 是一种有效的口服生物利用的抗糖尿病葡萄糖激酶(glucokinase)激活剂，EC50为 42 nM。AR453588 hydrochloride 具有降血糖作用。
| 生物活性 | AR453588 hydrochloride is a potent and orally bioavailable anti-diabeticglucokinase activator, with anEC50of 42 nM. AR453588 hydrochloride shows anti-hyperglycemic activity[1]. |
体内研究
(In Vivo) | AR453588 hydrochloride (3-30 mg/kg; p.o) lowers post-prandial glucose in normal C57BL/6J mice[1].
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[1].
AR453588 hydrochloride (10 mg/kg; p.o.) treatment shows that the Tmax, AUCinf, Vss, CmaxandFare 1.0 mL/min/kg, 4.65 h μg /mL, 1.67 μg /mL and 60.3%, respectively[1].
AR453588 hydrochloride (1 mg/kg; i.v.) treatment shows that the CL, AUCinf, Vss, and t1/2are 21.6 mL/min/kg, 0.77 h μg /mL, 0.746 L/kg and 1.28 hours, respectively[1].
| Animal Model: | Male diabetic ob/ob mice[1] | | 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[1] | | Dosage: | 10 mg/kg | | Administration: | p.o. (Pharmacokinetic Analysis) | | Result: | The Tmax, AUCinf, Vss, CmaxandFwere 1.0 mL/min/kg, 4.65 h μg /mL, 1.67 μg /mL and 60.3%, respectively |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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