Molecular Weight (MW)

501.8

Formula

C22H18Cl2N8.HCl

CAS No.

1797989-42-4 (HCl);

Storage

-20℃ for 3 years in powder form

-80℃ for 2 years in solvent

Solubility (In vitro)

DMSO: 93 mg/mL (185.33 mM)

Water: <1 mg/mL (slightly soluble or insoluble)

Ethanol: <1 mg/mL (slightly soluble or insoluble)

Synonym

CHIR-73911 HCl; CHIR73911; CHIR 73911 hydrochloride ; CHIR-911; CHIR911; CHIR 911; CT- 99021; CT-99021; CT- 99021; GSK 3 inhibitor XVI; GSK 3IXV; CHIR99021; CHIR 99021

General

Oral administration of CHIR-99021 at 30 mg/kg enhances glucose metabolism in a rodent model of type 2 diabetes, with a maximal plasma glucose reduction of nearly 150 mg/dl 3-4 hours after administration, while plasma insulin remains at or below control levels.

Animal model

Female db/db mice or male ZDF rats with type 2 diabetes

Formulation

Formulated as solutions in 20 mM citrate-buffered 15% Captisol or as fine suspensions in 0.5% carboxymethylcellulose.

Dosages

48 mg/kg

Administration

Oral gavage

Reference

[1] Ring DB, et al. Diabetes, 2003, 52(3), 588-595.