Molecular Formula | C8H6N2S3 |
Molar Mass | 226.34 |
Density | 1.51±0.1 g/cm3(Predicted) |
Melting Point | 165-166 |
Boling Point | 408.1±55.0 °C(Predicted) |
Flash Point | 200.6°C |
Solubility | DMSO: >20mg/mL |
Vapor Presure | 1.69E-06mmHg at 25°C |
Appearance | Solid |
Color | red |
pKa | 0.18±0.10(Predicted) |
Storage Condition | 2-8°C |
Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month. |
Sensitive | Light Sensitive |
Refractive Index | 1.76 |
In vitro study | Oltipraz, as a chemoprotectant, induced 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, significantly accelerating the degradation of HIF-1α protein. |
In vivo study | Oltipraz (500 mg/kg, p.o.) significantly reduced gastric tumor diversity by 55% in wild-type mice, but had no effect on tumor burden in nrf2-null mice. In BALB/c nude mice transplanted with HCT116 cells, Oltipraz (200 mg/kg, p.o.) inhibited tumor growth and angiogenesis by inhibiting HIF-1α. In rats fed the CDAA diet, Oltipraz attenuates the progression of nonalcoholic steatohepatitis-associated fibrosis. |
Hazard Symbols | Xi - Irritant |
Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. S36/37 - Wear suitable protective clothing and gloves. |
WGK Germany | 3 |
RTECS | JP1293000 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 4.418 ml | 22.091 ml | 44.181 ml |
5 mM | 0.884 ml | 4.418 ml | 8.836 ml |
10 mM | 0.442 ml | 2.209 ml | 4.418 ml |
5 mM | 0.088 ml | 0.442 ml | 0.884 ml |
Use | pirthiothione, also known as oltipraz, is a new anti-schistosome drug synthesized by French factory in the mid Rhone-Poulenc, foreign trade name Oltipraz. The animal experiments and clinical application have proved that it has a significant killing effect on Schistosoma mansoni, Schistosoma Haemophilus, and Schistosoma japonicum. |
pharmacological action | for mice infected with blood stem cell of mansoni, The ED50 is 50 mg/kg per day, even served for 5 days, the activity was 2 times higher than that of imidazole. The ED50 of monkey was 20mg/kg. Mouse LD50 for 5g/kg (oral). In rats and monkeys, no mutagenic factors and immunosuppressive effects. Another dose of 45mg/rats, 3 days of gavage, worm reduction rate was 71%, female reduction rate of 88%. The clinical treatment of Egypt, mansoni and 321 cases of schistosomiasis, the dose of 15 mg/kg and 25 mg/kg per day for 2 days, the low dose group Recovery Rate was 86%, the high dose group Recovery Rate was 94%. If the dose is increased and the course of treatment is prolonged, the curative effect is better. |
biological activity | Oltipraz is a potent activator of Nrf2 and a potent inducer of Phase II detoxification enzymes, significant effect on glutathione-S-transferase (GST). Phase 3. |
Target | Value |