AR453588 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 具有降血糖作用。

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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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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Hinklin RJ, et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorg Med Chem. 2020 Jan 1;28(1):115232.

In Vitro: DMSO : 100 mg/mL (192.44 mM; Need ultrasonic)配制储备液