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Oltipraz Catalog No.GC12821

Nrf2 activator;An antischistosomal agent

Size Price Stock Qty
10mM (in 1mL DMSO)
$34.00
In stock
10mg
$34.00
In stock
50mg
$63.00
In stock
200mg
$139.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

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Chemical Properties

Cas No. 64224-21-1 SDF
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
Solubility ≥22.6mg/mL in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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Background

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.