Oltipraz
(Synonyms: 奥替普拉; RP 35972; NSC 347901) 目录号 : GC12821
A Nrf2 and CAR activator
Cas No.:64224-21-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- 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.
| Cas No. | 64224-21-1 | SDF | |
| 别名 | 奥替普拉; RP 35972; NSC 347901 | ||
| 化学名 | 4-methyl-5-(pyrazin-2-yl)-3H-1,2-dithiole-3-thione | ||
| Canonical SMILES | CC(C1=S)=C(SS1)C2=CN=CC=N2 | ||
| 分子式 | C8H6N2S3 | 分子量 | 226.34 |
| 溶解度 | ≥ 22.6mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。