Oltipraz
(Synonyms: 奥替普拉; RP 35972; NSC 347901) 目录号 : GC12821A Nrf2 and CAR activator
Cas No.:64224-21-1
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
制备储备液 | |||
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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