1. Metabolic Enzyme/Protease
  2. Glucokinase
  3. AR453588 hydrochloride

AR453588 hydrochloride 

Cat. No.: HY-133127A
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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

AR453588 hydrochloride Chemical Structure

CAS No. : 1065606-97-4

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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 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 hydrochloride (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
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

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Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

AR453588AR 453588AR-453588GlucokinaseHexokinase IVHexokinase Dorallybioavailableanti-diabeticanti-hyperglycemicob/obmicetype2diabetesInhibitorinhibitorinhibit

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AR453588 hydrochloride
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HY-133127A
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