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Description: CHIR-99021 (CT99021; CT-99021) is a novel, potent and orally bioavailable inhibitor of GSK-3alpha/beta (glycogen synthase kinase 3alpha/beta) with the potential to treat type 2 diabetes. It inhibits GSK-3alpha/beta with an IC50 of 10 nM/6.7 nM in cell-free assays, also is a Wnt/beta-catenin activator which induces autophagy. Oral gavage of CHIR-99021 (30mg/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 hoursafter administration, while plasma insulin remains at or below controllevels.
Reference: PLoS One. 2013; 8(3):e58501.
Related CAS: 1782235-14-6 (3HCl); 2109414-84-6 (2HCl); 1797989-42-4 (HCl); 252917-06-9 (free base)
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