Liarozole-dihydrochloride-R75251-dihydrochloride-DataSheet-生命科學試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELiarozole dihydrochlorideCat. No.: HY-106019CCAS No.: 1883548-96-6Synonyms: R75251 dihydrochloride分式: CHClN分量: 381.69作靶點: Cytochrome P450作通路: Metabolic Enzyme/Protease儲存式: Please store the product under the recommended condition

2、s inthe COA.溶解性數(shù)據(jù)體外實驗 H2O : 50 mg/mL (131.00 mM)DMSO : 50 mg/mL (131.00 mM; Need ultrasonic)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.6199 mL 13.0996 mL 26.1993 mL5 mM 0.5240 mL 2.6199 mL 5.2399 mL10 mM 0.2620 mL 1.3100 mL 2.6199 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選

3、擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Liarozole dihydrochloride (R75251; R85246)種細胞素 P450 (CYP450) 依賴性抑制劑，具有服活性，也雌激素 (estrogen) 和丸雄激素合成的有效抑制劑。Liarozole dihydrochloride 通過抑制 4-羥化酶 (4-hydroxylase) 來防視酸的分解代謝，并在體內(nèi)顯出類視醇保留和類視醇模擬作。Liarozoledihydrochloride咪唑衍物; 它被作為前列腺癌和和膚病的激素藥物進研究。體外研究Liarozole

4、 inhibits the metabolism of retinoic acid to more polar metabolites in hamster liver microsomes1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE(IC50=2.2 M), rat liver homogenate (IC50=0.14 M), dunning prostate cancer homogenate (IC50=0.26 M)and MCF-7 human breast cancer cells (almost complete block

5、 at 10M) 1.Liarozole inhibits 17a-hydroxylase activity in bovine adrenal microsomes (IC50=0.15 M) 1.Liarozole has modest inhibitory activityon cholesterol synthesis in human hepatoma cells(IC50=5 M) 1.REFERENCES1. Bryson HM, et al. Liarozole. Drugs Aging. 1996 Dec;9(6):478-84; discussion 485.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-3792; 021