[CAS NO. 1065609-00-8] AR453588

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Catalog:	HY-133127
Brand:	MCE
CAS:	1065609-00-8

Overview

MDL	-
Molecular Weight	519.64
Molecular Formula	C25H25N7O2S2
SMILES	CC(N1CCC(C2=NSC(NC3=NC=C(SC4=NC=CC=C4)C=C3OC5=CC=CN=C5C)=N2)CC1)=O

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

Summary

AR453588 is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC ₅₀ of 42 nM. AR453588 shows anti-hyperglycemic activity ^[1] .

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 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 (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] .

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.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 192.44 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9244 mL	9.6220 mL	19.2441 mL
5 mM	0.3849 mL	1.9244 mL	3.8488 mL
10 mM	0.1924 mL	0.9622 mL	1.9244 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (4.81 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (4.81 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.81 mM); Clear solution

* All of the co-solvents are available by MCE.

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.

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