AR453588 hydrochloride

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AR453588 hydrochloride is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC₅₀ of 42 nM. AR453588 hydrochloride shows anti-hyperglycemic activity.

For research use only. We do not sell to patients.

AR453588 hydrochloride Chemical Structure

CAS No. : 1065606-97-4

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Biological Activity
Purity & Documentation
References
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Description

AR453588 hydrochloride is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC₅₀ of 42 nM. AR453588 hydrochloride shows anti-hyperglycemic activity^[1].

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 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^[1].
AR453588 hydrochloride (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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 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

Molecular Weight

556.10

Formula

C₂₅H₂₆ClN₇O₂S₂

CAS No.

1065606-97-4

SMILES

CC(N1CCC(C2=NSC(NC3=NC=C(SC4=NC=CC=C4)C=C3OC5=CC=CN=C5C)=N2)CC1)=O.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

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. [Content Brief]