Liarozole
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货号：A161291
同义名：
R75251
Liarozole (R75251; R85246)是一种咪唑衍生物，作为口服有效的维甲酸 (RA) 代谢阻断剂 (RAMBA)，它抑制维甲酸依赖的细胞色素P450 (CYP26) 4-羟基化，IC50 为7 μM，从而增加组织维甲酸水平，并具有抗肿瘤 特性。
Liarozole 化学结构
Liarozole 3D分子结构
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Liarozole 纯度/质量文件 产品仅供科研
货号：A161291
标准纯度：
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Liarozole 质控信息
Liarozole 生物活性
描述
Liarozole is an imidazole derivative and metabolic blocker of retinoic acid with oral activity. Liarozole inhibits CYP26-dependent 4-hydroxylation of retinoic acid with an IC50 value of 7 μM, leading to an increase in tissue levels of retinoic acid. Liarozole possesses antitumour properties[1] [2] [3] [3] [4]
Liarozole 动物研究
Animal study
At a dose of 5-20 mg/kg administered orally for 3 days, Liarozole reversed vaginal keratosis induced by estrogen stimulation[5] [6]
Liarozole 参考文献
[1] Kuijpers AL, et al. The effects of oral liarozole on epidermal proliferation and differentiation in severe plaque psoriasis are comparable with those of acitretin. Br J Dermatol. 1998;139(3):380-389.
[2] Lucker GP, et al. Oral treatment of ichthyosis by the cytochrome P-450 inhibitor liarozole. Br J Dermatol. 1997;136(1):71-75.
[3] Wouters W, 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 cells. Cancer Res. 1992;52(10):2841-2846.
[4] Pignatello MA, et al. Liarozole markedly increases all trans-retinoic acid toxicity in mouse limb bud cell cultures: a model to explain the potency of the aromatic retinoid (E)-4-[2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthylenyl)-1-propenyl] benzo
[5] Van Wauwe J, et al. Liarozole, an inhibitor of retinoic acid metabolism, exerts retinoid-mimetic effects in vivo. J Pharmacol Exp Ther. 1992;261(2):773-779.
[6] Stearns ME, et al. Liarozole and 13-cis-retinoic acid anti-prostatic tumor activity [published correction appears in Cancer Res 1993 Dec 1;53(23):5831]. Cancer Res. 1993;53(13):3073-3077.
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Liarozole 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
3.24mL
0.65mL
0.32mL
16.19mL
3.24mL
1.62mL
32.39mL
6.48mL
3.24mL
Liarozole 技术信息
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