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1065609-00-8

1065609-00-8 structure
1065609-00-8 structure
  • Name: AR453588
  • Chemical Name: AR453588
  • CAS Number: 1065609-00-8
  • Molecular Formula: C25H25N7O2S2
  • Molecular Weight: 519.64
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease Glucokinase
  • Create Date: 2020-01-23 20:20:51
  • Modify Date: 2024-01-23 17:42:57
  • AR453588 is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC50 of 42 nM. AR453588 shows anti-hyperglycemic activity[1].

Name AR453588
Description AR453588 is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC50 of 42 nM. AR453588 shows anti-hyperglycemic activity[1].
Related Catalog
In Vivo AR453588 (3-30 mg/kg; p.o) lowers post-prandial glucose in normal C57BL/6J mice[1]. 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[1]. AR453588 (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[1]. AR453588 (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[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, Cmax and F were 1.0 mL/min/kg, 4.65 h μg /mL, 1.67 μg /mL and 60.3%, respectively.
References

[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.

Molecular Formula C25H25N7O2S2
Molecular Weight 519.64