| 名称 | Doxazosin |
| 描述 | Doxazosin (UK 33274) is a long-lasting inhibitor of α1-adrenoceptors that is widely used to treat benign prostatic hyperplasia and lower urinary tract symptoms. |
| 体外活性 | Doxazosin, at concentrations of 5-20 mumol/L, increased LDL binding to hepatic cells in a dose-related manner. Also, in these hepatic cells, doxazosin produced dose-related decreases in both newly synthesized cholesterol and cholesterol ester. In rabbit fibroblasts that were LDL receptor negative, de novo cholesterol synthesis was markedly reduced by increasing concentrations of doxazosin. Taken together, these results suggest that doxazosin may have a direct inhibitory effect on cholesterol synthesis independent of the LDL receptor[2]. |
| 体内活性 | Both the enantiomers were highly bound to the plasma proteins of rats, dogs and humans [(-)doxazosin: 89.4%-94.3%; (+)doxazosin: 90.9%-95.4%]. (+)Doxazosin exhibited significantly higher protein binding capacities than (-)doxazosin in all the three species, and the difference in the bound concentration (Cb) between the two enantiomers was enhanced as their concentrations were increased. Although the percentage of the plasma protein binding in the dog plasma was significantly lower than that in the human plasma at 400 and 800 ng/mL, the corrected percentage of plasma protein binding was dog>human>rat[3]. |
| 存储条件 | keep away from direct sunlight,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 30 mg/mL (66.45 mM), Sonication is recommended.
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| 关键字 | α1-adrenergic receptor | UK-33274 | UK33274 | Inhibitor | inhibit | Doxazosin | Beta Receptor | AdrenergicReceptor | Adrenergic Receptor |
| 相关产品 | Amitraz | Trifluoperazine dihydrochloride | Buflomedil hydrochloride | Mirtazapine | Mianserin hydrochloride | Trazodone hydrochloride | Gemfibrozil | D-Mannitol | Octopamine hydrochloride | Tolazoline hydrochloride | Isoprenaline hydrochloride | Dexmedetomidine hydrochloride |
| 相关库 | 抑制剂库 | 经典已知活性库 | 抗癌上市药物库 | 已知活性化合物库 | 神经信号分子库 | FDA 上市药物库 | GPCR靶点分子库 | 神经退行性疾病化合物库 | 膜蛋白靶向化合物库 | 药物功能重定位化合物库 | 抗癌临床化合物库 | 抗癌药物库 |
