货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
T29277-1ml	10mM in DMSO	￥840.00 T29277-1ml ￥840.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

T29277-1ml

10mM in DMSO

￥840.00

货期：3-5天

产品描述：

Liarozole (R75251; R85246) is an imidazole derivative and orally active 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

靶点：

CYP26:7 μM (IC50)

体外研究：

Liarozole (0.01~10 μM; 9 days; MCF-7 cells) inhibits cells proliferation.

Liarozole (1 μM; 4 days; mesenchymal cells) completely inhibits chondrogenesis.

体内研究：

Liarozole (5-20 mg/kg; p.o.; 3 days) reverses the vaginal keratosis caused by estrogen stimulation. Liarozole (40 mg/kg; p.o.; 21 days) reduces tumor burden substantially. Animal Model: Ovariectomized rats Dosage: 5~20 mg/kg Administration: P.o.; 3 days Result: Reversed the vaginal keratosis caused by estrogen stimulation. Animal Model: SCID mice Dosage: 40 mg/kg Administration: P.o.; 21 daysResult: Inhibited tumor growth and survival.

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] 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.

溶解性：

Soluble in DMSO

保存条件：

-80℃（运输条件：冰袋低温运输）

备注：

Liarozole (R75251; R85246) 是一种咪唑衍生物和具有口服活性的维甲酸 (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。

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	3.239 ml	16.194 ml	32.388 ml
5 mM	0.648 ml	3.239 ml	6.478 ml
10 mM	0.324 ml	1.619 ml	3.239 ml
50 mM	0.065 ml	0.324 ml	0.648 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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