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    CHIR99021 (CT 99021)
    CHIR99021 (CT 99021)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0211
    CAS #: 252917-06-9 Purity ≥98%

    Description: CHIR-99021 (CT99021; CT-99021) is a novel, potent and orally bioavailable inhibitor of GSK-3α/β (glycogen synthase kinase 3α/β) with the potential to treat  type 2 diabetes. It inhibits GSK-3α/β with an IC50 of 10 nM/6.7 nM in cell-free assays, also is a Wnt/β-catenin activator which induces autophagy. Oral gavage of CHIR-99021 (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.

    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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    Molecular Weight (MW)465.34
    FormulaC22H18Cl2N8
    CAS No.252917-06-9 (free base);
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 10 mg/mL warmed (21.48 mM)
    Water: <1 mg/mL (slightly soluble or insoluble)
    Ethanol: <1 mg/mL (slightly soluble or insoluble)
    Solubility (In vivo)4% DMSO+30% PEG 300+ddH2O
    SynonymCHIR-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


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    GeneralOral 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 modelFemale db/db mice or male ZDF rats with type 2 diabetes
    FormulationFormulated as solutions in 20 mM citrate-buffered 15% Captisol or as fine suspensions in 0.5% carboxymethylcellulose.
    Dosages48 mg/kg
    AdministrationOral gavage
    Reference[1] Ring DB, et al. Diabetes, 2003, 52(3), 588-595.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    CHIR99021

     

    CHIR99021



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