| 产品描述: | 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. |
| 靶点: |
IC50: 10 μM (HIF-1α) Nrf2;HIF/HIFProlyl-Hydroxylase;HIVProtease;ReverseTranscriptase;Nrf2;HIF |
| 体内研究: |
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. |
| 参考文献: |
1. 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. 2. Lv S, et al. Glucagon-induced extracellular cAMP regulates hepatic lipid metabolism. J Endocrinol. 2017 Aug;234(2):73-87. 3. 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. 4. Eba S, et al.The nuclear factor erythroid 2-related factor 2 activator oltipraz attenuates chronic hypoxia-induced cardiopulmonary alterations in mice.Am J Respir Cell Mol Biol. 2013 Aug;49(2):324-33. |
| 溶解性: |
DMSO : 6 mg/mL (26.51 mM; Need ultrasonic and warming) |
| 保存条件: |
2-8℃ |
| 配置溶液浓度参考: |
|
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 |
| 50 mM |
0.088 ml |
0.442 ml |
0.884 ml |
|
| 注意: |
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