Oltipraz

Catalog No.S7864

Oltipraz Chemical Structure

Molecular Weight(MW): 226.34

Oltipraz is a potent Nrf2 activator and a potent inducer of Phase II detoxification enzymes, most notably glutathione-S-transferase (GST). Phase 3.

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  • Effects of p21 depletion and Nrf2 activation on dexamethasone-induced apoptosis in MC3T3-E1 cells. Cells were transfected with control siRNA or p21 siRNA. Subsequently, transfected cells were pre incubated with oltipraz (20 μM) for 1 h, and then co-incubated with 1 μM dexamethasone for 24 h. Apoptosis was measured by flow cytometry, followed by Annexin V-FITC/PI double staining. Effects of p21 depletion and Nrf2 activation on dexamethasone-induced apoptosis in MC3T3-E1 cells. Cells were transfected with control siRNA or p21 siRNA. Subsequently, transfected cells were pre-incubated with oltipraz (20 μM) for 1 h, and then co-incubated with 1 μM dexamethasone for 24 h. Apoptosis was measured by flow cytometry, followed by Annexin V-FITC/PI double staining.

    Arch Toxicol, 2017. Oltipraz purchased from Selleck.

Purity & Quality Control

Choose Selective Nrf2 Inhibitors

Biological Activity

Description Oltipraz is a potent Nrf2 activator and a potent inducer of Phase II detoxification enzymes, most notably glutathione-S-transferase (GST). Phase 3.
Targets
Nrf2 [1]
In vitro

Oltipraz, as a chemoprotective agent, induces Phase II detoxification enzyme activity in a Nrf2-dependent manner. [1] 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. [2]

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. [1] 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. [2] In rats on a CDAA diet, Oltipraz attenuate the progression of nonalcoholic steatohepatitis-related fibrosis. [3]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: Female wild-type and nrf2-disrupted mice
  • Formulation: Suspended in 1% cremophor and 25% glycerol
  • Dosages: 500 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 39 mg/mL warmed (172.3 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 226.34
Formula

C8H6N2S3

CAS No. 64224-21-1
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02068339 Completed Non-alcholic Fatty Liver Disease PharmaKing February 2014 Phase 3
NCT01373554 Completed Non-alcoholic Fatty Liver Disease PharmaKing May 2011 Phase 2
NCT00956098 Completed Liver Fibrosis|Liver Cirrhosis CJ HealthCare Corporation February 2006 Phase 2
NCT00006457 Completed Lung Cancer Northwestern University|National Cancer Institute (NCI) August 2000 Phase 1

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID