Oltipraz (Synonyms: NSC 347901, RP 35972) |
| رقم الكتالوجGC12821 |
Oltipraz له تأثير مثبط على تنشيط HIF-1α بطريقة تعتمد على الوقت ، مما يلغي تمامًا تحريض HIF-1α عند تركيزات 10 ميكرومتر ، ويكون IC50 من Oltipraz لتثبيط HIF-1α هو 10 ميكرومترOltipraz هو منشط فعال Nrf2
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 64224-21-1
Sample solution is provided at 25 µL, 10mM.
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Oltipraz is a synthetic, substituted 1,2-dithiole-3-thione originally 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).
In vitro: Oltipraz has been classified as a monofunctional inducer since it advantageously elevates Phase II detoxification enzymes, while only slightly altering the expression of the Phase I “activating” enzymes. Oltipraz effectively induced quinone reductase in Hepa 1c1c7 cells defective in the aryl hydrocarbon receptor function required by bifunctional inducers [1].
In vivo: Dietary concentrations of oltipraz produce great inhibition of aflatoxin B1-induced hepatic tumorigenesis in rats. Levels of hepatic aflatoxin-DNA adducts and serum aflatoxin-albumin adducts decreased when biliary elimination of aflatoxin-glutathione conjugants increased, therefore providing predictive biomarkers that measured a chemopreventive effect. In other animal studies, oltipraz was found to inhibit chemically induced carcinogenesis in bladder, colon, breast, stomach, and skin cancer models [2].
Clinical trial: In a Phase I study, a single oral dose of oltipraz was given to normal volunteers at dose levels of 125, 250, 375, and 500 mg. There was no significant difference in half-life between the four dose levels nor in clearance at the 125 and 250 mg levels. A series of small trials evaluating single oral doses of oltipraz for up to 28 days also showed a short t1/2 (4.1-5.3 hours), a sustained steady state without variation after a loading dose, and increased serum and urine concentrations with consumption of a high-fat diet [2].
Reference:
[1] Clapper ML. Chemopreventive activity of oltipraz. Pharmacol Ther. 1998 Apr;78(1):17-27.
[2] Benson AB 3rd. Oltipraz: a laboratory and clinical review. J Cell Biochem Suppl. 1993;17F:278-91.
| Cas No. | 64224-21-1 | SDF | |
| المرادفات | NSC 347901, RP 35972 | ||
| Chemical Name | 4-methyl-5-(pyrazin-2-yl)-3H-1,2-dithiole-3-thione | ||
| Canonical SMILES | CC(C1=S)=C(SS1)C2=CN=CC=N2 | ||
| Formula | C8H6N2S3 | M.Wt | 226.34 |
| الذوبان | ≥ 22.6mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.4181 mL | 22.0907 mL | 44.1813 mL |
| 5 mM | 0.8836 mL | 4.4181 mL | 8.8363 mL |
| 10 mM | 0.4418 mL | 2.2091 mL | 4.4181 mL |
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)
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