Product Name :
Oltipraz
Description:
Oltipraz has an inhibitory effect on HIF-1α activation 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. Oltipraz is a potent Nrf2 activator.
CAS:
64224-21-1
Molecular Weight:
226.34
Formula:
C8H6N2S3
Chemical Name:
4-methyl-5-(pyrazin-2-yl)-3H-1,2-dithiole-3-thione
Smiles :
CC1C(=S)SSC=1C1C=NC=CN=1
InChiKey:
CKNAQFVBEHDJQV-UHFFFAOYSA-N
InChi :
InChI=1S/C8H6N2S3/c1-5-7(12-13-8(5)11)6-4-9-2-3-10-6/h2-4H,1H3
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
Oltipraz has an inhibitory effect on HIF-1α activation 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. Oltipraz is a potent Nrf2 activator.|Product information|CAS Number: 64224-21-1|Molecular Weight: 226.34|Formula: C8H6N2S3|Synonym:|RP 35972|NSC 347901|Chemical Name: 4-methyl-5-(pyrazin-2-yl)-3H-1,2-dithiole-3-thione|Smiles: CC1C(=S)SSC=1C1C=NC=CN=1|InChiKey: CKNAQFVBEHDJQV-UHFFFAOYSA-N|InChi: InChI=1S/C8H6N2S3/c1-5-7(12-13-8(5)11)6-4-9-2-3-10-6/h2-4H,1H3|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 6 mg/mL (26.51 mM; Need ultrasonic and warming).|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In 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.Deferoxamine In stock Oltipraz treatment also inhibits HIF-1α activation stimulated by either hypoxia or CoCl2.Alvelestat supplier Oltipraz is a cancer chemopreventive agent and has an inhibitory effect on angiogenesis and tumor growth.PMID:32806950 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.|References:|Lee WH, et al. Oltipraz and dithiolethione congeners inhibit hypoxia-inducible factor-1alpha activity through p70 ribosomal S6 kinase-1 inhibition and H2O2-scavenging effect. Mol Cancer Ther. 2009 Oct;8(10):2791-802.Lv S, et al. Glucagon-induced extracellular cAMP regulates hepatic lipid metabolism. J Endocrinol. 2017 Aug;234(2):73-87.Ramos-Gomez M, et al. Sensitivity to carcinogenesis is increased and chemoprotective efficacy of enzyme inducers is lost in nrf2 transcription factor-deficient mice. Proc Natl Acad Sci U S A. 2001 Mar 13;98(6):3410-5.Products are for research use only. Not for human use.|
