OLTIPRAZ Cas:64224-21-1

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Product Description:

Product Name: OLTIPRAZ CAS NO: 64224-21-1

 

Synonyms:

3H-1,2-DITHIOLE-3-THIONE,4-METHYL-5-PYRAZINYL;

4-Methyl-5-pyrazin-2-yl-1,2-dithiole-3-thione;

5-(2-pyrazinyl)-4-methyl-1,2-dithiole-3-thione;

 

Chemical & Physical Properties:

Appearance: Red Solid

Assay :≥99.0%

Density: 1.51 g/cm3

Boiling Point: 408.1℃ at 760 mmHg

Melting Point: 165-166℃

Flash Point: 200.6℃

Refractive Index: 1.76

Sensitive: Light Sensitive

 

Safety Information:

Safety Statements: S26; S36/37/39

HS Code: 2933990090

Risk Statements: R36/37/38

 

Oltipraz is a synthetic, substituted 1,2-dithiole-3-thione previously used in humans as an antischistosomal agent. Animal studies have demonstrated that oltipraz is a potent inducer of Phase II detoxification enzymes, most notably glutathione-S-transferase (GST). Oltipraz is now known to be used for tumor prevention purposes.

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.  Oltipraz is also a competitive inhibitor of this cytochrome P450, with an apparent Ki of 10 μM. 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.

 

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