1. Metabolic Enzyme/Protease
  2. Cytochrome P450
  3. Liarozole dihydrochloride

Liarozole dihydrochloride (Synonyms: R75251 dihydrochloride)

目录号: HY-106019C
产品使用指南

Liarozole dihydrochloride (R75251; R85246) 是一种细胞色素 P450 (CYP450) 依赖性抑制剂,具有口服活性,也是雌激素 (estrogen) 和睾丸雄激素合成的有效抑制剂。Liarozole dihydrochloride 通过抑制 4-羟化酶 (4-hydroxylase) 来防止视黄酸的分解代谢,并在体内显示出类视黄醇保留和类视黄醇模拟作用。Liarozole dihydrochloride 是咪唑衍生物; 它被作为前列腺癌和和皮肤病的非激素药物进行研究。

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Liarozole dihydrochloride Chemical Structure

Liarozole dihydrochloride Chemical Structure

CAS No. : 1883548-96-6

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Description

Liarozole dihydrochloride (R75251; R85246) 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 prevents the catabolism of retinoic acid via inhibition of 4-hydroxylase and exhibits retinoid sparing and retinoid-mimetic effects in vivo. 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[1].

In Vitro

Liarozole inhibits the metabolism of retinoic acid to more polar metabolites in hamster liver microsomes (IC50=2.2 μM), rat liver homogenate (IC50=0.14 μM), dunning prostate cancer homogenate (IC50=0.26 μM) and MCF-7 human breast cancer cells (almost complete block at 10μM) [1].
Liarozole inhibits 17a-hydroxylase activity in bovine adrenal microsomes (IC50=0.15 μM) [1].
Liarozole has modest inhibitory activity on cholesterol synthesis in human hepatoma cells(IC50=5 μM)[1].

Molecular Weight

381.69

Formula

C₁₇H₁₅Cl₃N₄

CAS No.

1883548-96-6

SMILES

ClC1=CC(C(C2=CC=C3N=CNC3=C2)N4C=CN=C4)=CC=C1.[H]Cl.[H]Cl

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Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

H2O : ≥ 50 mg/mL (131.00 mM)

DMSO : 50 mg/mL (131.00 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6199 mL 13.0996 mL 26.1993 mL
5 mM 0.5240 mL 2.6199 mL 5.2399 mL
10 mM 0.2620 mL 1.3100 mL 2.6199 mL
* 请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液,并请注意储备液的保存方式和期限。
References
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产品名称:
Liarozole dihydrochloride
目录号:
HY-106019C
需求量:

Liarozole dihydrochloride

Cat. No.: HY-106019C