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.
仕様
仕様と純度
10mM in DMSO
生化学的・生理学的メカニズム
AR453588 is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC 50 of 42 nM. AR453588 shows anti-hyperglycemic activity.
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よくある質問
How should this product be stored?
Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.
How is this product shipped?
This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.
What are the CAS number, molecular formula and molecular weight?
The CAS Number is 1065609-00-8, the molecular formula is C25H25N7O2S2, and the molecular weight is 519.64 g/mol.
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