Liarozole
(Synonyms: 利阿唑,R75251) 目录号 : GC61971
A CYP26A1 inhibitor
Cas No.:115575-11-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Liarozole is an inhibitor of the cytochrome P450 (CYP) isoform CYP26A1 (IC50 = 2.1 ?M), an enzyme involved in the metabolism of all-trans retinoic acid .1 It also inhibits the production of estradiol induced by follicle-stimulating hormone (FSH) in rat granulosa cells and testosterone and androstenedione production induced by human chorionic gonadotropin (hCG) in rat testicular cells (IC50s = 0.4, 2.3, and 0.7 ?M, respectively).2 Liarozole enhances the antiproliferative activity of all-trans retinoic acid in MCF-7 breast cancer cells.3 It decreases plasma levels of retinoic acid in rats in a dose-dependent manner.4 Liarozole (5 and 20 mg/kg) decreases estradiol undecylate-induced vaginal keratinization in ovariectomized rats.
1.Thatcher, J.E., Buttrick, B., Shaffer, S.A., et al.Substrate specificity and ligand interactions of CYP26A1, the human liver retinoic acid hydroxylaseMol. Pharmacol.80(2)228-239(2011) 2.Bruynseels, J., De Coster, R., Rooy, P.V., et al.R 75251, a new inhibitor of steroid biosynthesisProstate16(4)345-357(1990) 3.Wouters, W., van Dun, J., Dillen, A., et al.Effects of liarozole, a new antitumoral compound, on retinoic acid-induced inhibition of cell growth and on retinoic acid metabolism in MCF-7 human breast cancer cellsCancer Res.52(10)2841-2846(1992) 4.Van Wauwe, J., Van Nyen, G., Coene, M.C., et al.Liarozole, an inhibitor of retinoic acid metabolism, exerts retinoid-mimetic effects in vivoJ. Pharmacol. Exp. Ther.261(2)773-779(1992)
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.2388 mL | 16.1938 mL | 32.3876 mL |
| 5 mM | 0.6478 mL | 3.2388 mL | 6.4775 mL |
| 10 mM | 0.3239 mL | 1.6194 mL | 3.2388 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。