Oltipraz structure
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Common Name | Oltipraz | ||
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CAS Number | 64224-21-1 | Molecular Weight | 226.342 | |
Density | 1.5±0.1 g/cm3 | Boiling Point | 408.1±55.0 °C at 760 mmHg | |
Molecular Formula | C8H6N2S3 | Melting Point | 165-166ºC | |
MSDS | Chinese USA | Flash Point | 200.6±31.5 °C | |
Symbol |
GHS07 |
Signal Word | Warning |
Use of OltiprazOltipraz 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 μMTarget: HIF-1αin 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] |
Name | oltipraz |
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Synonym | More Synonyms |
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 μMTarget: HIF-1αin 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] |
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Related Catalog | |
References |
Density | 1.5±0.1 g/cm3 |
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Boiling Point | 408.1±55.0 °C at 760 mmHg |
Melting Point | 165-166ºC |
Molecular Formula | C8H6N2S3 |
Molecular Weight | 226.342 |
Flash Point | 200.6±31.5 °C |
Exact Mass | 225.969315 |
PSA | 114.35000 |
LogP | 1.92 |
Vapour Pressure | 0.0±0.9 mmHg at 25°C |
Index of Refraction | 1.760 |
Storage condition | 2-8°C |
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATAACUTE TOXICITY DATA
MUTATION DATA
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Symbol |
GHS07 |
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Signal Word | Warning |
Hazard Statements | H315-H319-H335 |
Precautionary Statements | P261-P305 + P351 + P338 |
Personal Protective Equipment | dust mask type N95 (US);Eyeshields;Gloves |
Risk Phrases | R36/37/38 |
Safety Phrases | 26-36/37/39 |
RIDADR | NONH for all modes of transport |
RTECS | JP1293000 |
HS Code | 2933990090 |
~14% Oltipraz CAS#:64224-21-1 |
Literature: CJ CORPORATION Patent: WO2004/48369 A1, 2004 ; Location in patent: Page 9-10 ; |
~% Oltipraz CAS#:64224-21-1 |
Literature: US2004/53989 A1, ; |
HS Code | 2933990090 |
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Summary | 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
Catalase overexpression prevents nuclear factor erythroid 2-related factor 2 stimulation of renal angiotensinogen gene expression, hypertension, and kidney injury in diabetic mice.
Diabetes 63(10) , 3483-96, (2014) This study investigated the impact of catalase (Cat) overexpression in renal proximal tubule cells (RPTCs) on nuclear factor erythroid 2-related factor 2 (Nrf2) stimulation of angiotensinogen (Agt) ge... |
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Antioxidant and mitochondrial protective effects of oxidized metabolites of oltipraz.
Expert Opin. Drug Metab. Toxicol. 6(2) , 213-24, (2010) Comprehensive studies indicate that oltipraz exerts cancer chemopreventive effects. Oltipraz has other therapeutic potentials, which include anti-fibrotic effect, inhibition of insulin resistance, mit... |
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Inhibition of colon carcinogenesis by post-initiation induction of NQO1 in Sprague-Dawley rats.
Oncol. Rep. 21(6) , 1559-65, (2009) Inducers of phase II detoxifying enzymes have been studied as chemopreventive agents for a variety of cancers. Phase II detoxifying enzymes may play a significant role in preventing carcinogen-induced... |
Oltipraz |
4-methyl-5-pyrazin-2-yldithiole-3-thione |
RP-35,972 |
4-Methyl-5-(pyrazin-2-yl)-3H-1,2-dithiole-3-thione |
4-Methyl-5-(2-pyrazinyl)-3H-1,2-dithiole-3-thione |
4-Methyl-5-pyrazinyl-3H-1,2-dithiole-3-thione |
3H-1,2-DITHIOLE-3-THIONE,4-METHYL-5-PYRAZINYL |
4-Methyl-5-pyrazin-2-yl-1,2-dithiole-3-thione |
3H-1,2-Dithiole-3-thione, 4-methyl-5-(2-pyrazinyl)- |