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    Oltipraz (RP 35972; NSC 347901)
    Oltipraz (RP 35972; NSC 347901)

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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 #: V1892
    CAS #: 64224-21-1 Purity ≥98%

    Description: Oltipraz (RP 35972; NSC 347901), a potential anticancer agent, is a potent Nrf2 activator and an inducer of Phase II detoxification enzymes such as glutathione-S-transferase (GST). Oltipraz is a synthetic, substituted 1,2-dithiole-3-thione originally used in humans as an antischistosomal agent. Oltipraz has been classified as a monofunctional inducer since it advantageously elevates Phase II detoxification enzymes, while only slightly altering the expression of the Phase I “activating” enzymes.

    References: Proc Natl Acad Sci U S A. 2001 Mar 13;98(6):3410-5; Mol Cancer Ther. 2009 Oct;8(10):2791-802.

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    Molecular Weight (MW)226.34 
    FormulaC8H6N2S3 
    CAS No.64224-21-1 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 39 mg/mL (172.3 mM) 
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other info

    Chemical Name: 4-methyl-5-(pyrazin-2-yl)-3H-1,2-dithiole-3-thione

    InChi Key: CKNAQFVBEHDJQV-UHFFFAOYSA-N

    InChi Code: InChI=1S/C8H6N2S3/c1-5-7(12-13-8(5)11)6-4-9-2-3-10-6/h2-4H,1H3

    SMILES Code: S=C1SSC(C2=NC=CN=C2)=C1C

    Synonyms

    CD-1400; CD1400; CD 1400


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    In Vitro

    In vitro activity: Oltipraz, as a chemoprotective agent, induces Phase II detoxification enzyme activity in a Nrf2-dependent manner. In human HT29 colon cancer cells, oltipraz inhibits the induction of HIF-1α by insulin, hypoxia or CoCl2 by significantly accelerating degradation of HIF-1α protein.


    Cell Assay: Oltipraz has been classified as a monofunctional inducer since it advantageously elevates Phase II detoxification enzymes, while only slightly altering the expression of the Phase I “activating” enzymes. Oltipraz effectively induced quinone reductase in Hepa 1c1c7 cells defective in the aryl hydrocarbon receptor function required by bifunctional inducers 

    In VivoOltipraz (500 mg/kg, p.o.) significantly reduces multiplicity of gastric neoplasia in wild-type mice by 55%, but has no effect on tumor burden in nrf2-deficient mice. In BALB/c nude mice transplanted with HCT116 cells, Oltipraz (200 mg/kg, p.o.) inhibits tumor growth and angiogenesis via inhibition of HIF-1α. In rats on a CDAA diet, Oltipraz attenuate the progression of nonalcoholic steatohepatitis-related fibrosis.  
    Animal modelFemale wild-type and nrf2-disrupted mice 
    Formulation & DosageSuspended in 1% cremophor and 25% glycerol; 500 mg/kg; p.o. 
    References

    Proc Natl Acad Sci U S A. 2001 Mar 13;98(6):3410-5; Mol Cancer Ther. 2009 Oct;8(10):2791-802; Mol Pharmacol. 2013 Jul;84(1):62-70. 


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

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