产品说明书

Liarozole

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Chemical Structure| 115575-11-6 同义名 : R75251
CAS号 : 115575-11-6
货号 : A161291
分子式 : C17H13ClN4
纯度 : 98%+
分子量 : 308.765
MDL号 : MFCD00864664
存储条件：

粉末 Keep in dark place,Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(340.06 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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].In MCF-7 cells, Liarozole inhibits cell proliferation at concentrations ranging from 0.01-10 μM for 9 days of treatment[3].In mesenchymal cells, Liarozole completely inhibited chondrogenesis at a concentration of 1 μM for 4 days of treatment[4].
实验方案
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
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.