| CAS NO: | 64224-21-1 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| Molecular Weight (MW) | 226.34 |
|---|---|
| Formula | C8H6N2S3 |
| 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 |
| 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 Vivo | Oltipraz (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 model | Female wild-type and nrf2-disrupted mice |
| Formulation & Dosage | Suspended 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. |
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