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Liarozole (R75251 dihydrochloride) 是一种咪唑衍生物,是一种具有口服活性的维甲酸 (RA) 代谢阻断剂(RAMBA),具有抗肿瘤作用。它能够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 (R75251 dihydrochloride) 是一种咪唑衍生物,是一种具有口服活性的维甲酸 (RA) 代谢阻断剂(RAMBA),具有抗肿瘤作用。它能够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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 497 | 现货 | |
5 mg | ¥ 1,230 | 现货 | |
10 mg | ¥ 1,990 | 现货 | |
25 mg | ¥ 3,890 | 现货 | |
50 mg | ¥ 6,230 | 现货 | |
100 mg | ¥ 8,390 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,370 | 现货 |
产品描述 | Liarozole (R75251 dihydrochloride) is a cytochrome P450 (CYP450) dependent inhibitor, orally active, it also a potent inhibitor of estrogen (via inhibition of aromatase) and testicular androgen synthesis (inhibition of 17 ,20-lyase).Liarozole dihydrochloride is an imidazole derivative; it is being investigated as a non-hormonal agent in prostate cancer and in the treatment of various other cancers and skin disorders. |
靶点活性 | CYP26:7 μM (IC50) |
体外活性 | Liarozole 在牛肾上腺微粒体中抑制17α-羟化酶活性(IC50=0.15 μM)[1]。在人肝癌细胞中对胆固醇合成具有适度抑制作用(IC50=5 μM)[1]。同时,Liarozole 抑制仓鼠肝微粒体(IC50=2.2 μM)、大鼠肝同源物(IC50=0.14 μM)、Dunning 前列腺癌同源物(IC50=0.26 μM)以及MCF-7人乳腺癌细胞中维甲酸代谢成更极性代谢产物的过程(10μM时几乎完全阻断)[1]。 |
别名 | 利阿唑, R75251 dihydrochloride |
分子量 | 308.76 |
分子式 | C17H13ClN4 |
CAS No. | 115575-11-6 |
Smiles | Clc1cccc(c1)C(c1ccc2nc[nH]c2c1)n1ccnc1 |
密度 | 1.36g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 55 mg/mL (178.13 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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