1. Metabolic Enzyme/Protease
  2. HIF/HIF Prolyl-Hydroxylase

Oltipraz (Synonyms: RP 35972; NSC 347901)

Cat. No.: HY-12519 Purity: 99.15%
Data Sheet SDS Handling Instructions

Oltipraz has an inhibitory effect on HIF-1α activation by insulin in a time-dependent manner, completely abrogating HIF-1α induction at ≥10 μM concentrations, the IC50 of Oltipraz for HIF-1α inhibition is 10 μM.

For research use only. We do not sell to patients.
Oltipraz Chemical Structure

Oltipraz Chemical Structure

CAS No. : 64224-21-1

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10 mM * 1 mL in DMSO $55 In-stock
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Oltipraz has an inhibitory effect on HIF-1α activation by insulin in a time-dependent manner, completely abrogating HIF-1α induction at ≥10 μM concentrations, the IC50 of Oltipraz for HIF-1α inhibition is 10 μM. IC50 value: 10 μM Target: HIF-1α in vitro: Oltipraz inhibits HIF-1α activity and HIF-1α-dependent tumor growth, which may result from a decrease in HIF-1α stability through S6K1 inhibition in combination with an H2O2-scavenging effect. Oltipraz treatment also inhibits HIF-1α activation stimulated by either hypoxia or CoCl2. Oltipraz is a cancer chemopreventive agent and has an inhibitory effect on angiogenesis and tumor growth. [1] Oltipraz is also a competitive inhibitor of this cytochrome P450, with an apparent Ki of 10 μM. [2] in vivo: In wild-type mice, hepatic levels of mRNA for all of the genes analyzed were significantly increased after Oltipraz treatment, with the highest increase (treated/control) for NQO1 mRNA levels (7.6-fold). The Northern blot analyses demonstrated that the observed increases in GST and NQO1 activities by Oltipraz in wild-type mice were preceded by significant elevations in RNA expression. Interestingly, mRNA levels of Nrf2 itself were increased more than 3-fold by Oltipraz treatment. [2]

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT00956098 CJ HealthCare Corporation Liver Fibrosis|Liver Cirrhosis February 2006 Phase 2
NCT01373554 PharmaKing Non-alcoholic Fatty Liver Disease May 2011 Phase 2
NCT00006457 Northwestern University|National Cancer Institute (NCI) Lung Cancer August 2000 Phase 1
NCT02068339 PharmaKing Non-alcholic Fatty Liver Disease February 2014 Phase 3
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References
Molecular Weight

226.34

Formula

C₈H₆N₂S₃

CAS No.

64224-21-1

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

Oltipraz is prepared in coin oil[3].

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

References

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Product Name:
Oltipraz
Cat. No.:
HY-12519
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