product name Oltipraz
Description: Oltipraz 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.
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
Solubility (In vivo)
Synonyms
other peoduct :
| 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. Kinase Assay: 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. |
