Liarozole (R75251; R85246) 是一种咪唑衍生物，是一种维甲酸 (RA) 代谢阻断剂 (RAMBA)。Liarozole 抑制维甲酸依赖的细胞色素 P450 (CYP26) 4-羟基化 (IC50=7 μM)，导致组织维甲酸水平增加。Liarozole 具有抗肿瘤特性。
货号:ajcx32810
CAS:115575-11-6
分子式:C17H13ClN4
分子量：308.76
溶解度:>20mg/ml in DMSO
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Liarozole (R75251; R85246) is an imidazole derivative and a retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of retinoic acid (IC50=7 μM), resulting in increased tissue levels of retinoic acid. Liarozole shows antitumoral properties[1][2][3].

Liarozole (0.01~10 μM; 9 days; MCF-7 cells) inhibits cells proliferation[3].Liarozole (1 μM; 4 days; mesenchymal cells) completely inhibits chondrogenesis[4].

Liarozole (5-20 mg/kg; p.o.; once daily for 3 days) reverses the vaginal keratosis caused by estrogen stimulation[5].Liarozole (40 mg/kg; guvage; 21 days) reduces tumor burden substantially[6].

[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] benzoic acid. Toxicol Appl Pharmacol. 2002; 178(3):186-194.
[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.