| 名称 | Atazanavir |
| 描述 | Atazanavir (BMS-232632)(BMS-232632) is an highly effective HIV-1 protease inhibitor. |
| 细胞实验 | U251, T98 g, and LN229 glioblastoma cell lines are exposed to increasing concentrations of nelfinavir and atazanavir. Cells cultured in 96-well plates are treated with drugs for 48 h, and cell growth and survival are determined by conventional MTT assay.(Only for Reference) |
| 激酶实验 | Protease assays: To determine the inhibition constants (Ki) for each Prt inhibitor, purified HIV-1 RF wild-type Prt (2.5 nM) is incubated at 37 ℃ with 1 μM to 15 μM fluorogenic substrate in reaction buffer (1 M NaCl, 1 mM EDTA, 0.1 M sodium acetate [pH 5.5], 0.1% polyethylene glycol 8000) in the presence or absence of Atazanavir. Cleavage of the substrate is quantified by measuring an increase in fluorescent emission at 490 nM after excitation at 340 nM using a Cytofluor 4000. Reactions are carried out using 1.36 μM, 1.66 μM, 2.1 μM, 3.0 μM, 5.0 μM, or 15 μM substrate in the presence of five concentrations of Atazanavir (1.25 nM to 25 nM). Substrate cleavage is monitored at 5-min intervals for 30 min. Cleavage rates are then determined for each sample at early time points in the reaction, and Ki values are determined from the slopes of the resulting Michaelis-Menten plots. |
| 体外活性 | Atazanavir has potent in vitro activity with 50 and 90% effective concentrations(EC50) of 2-5 nM and 9-15 nM respectively against wild type virus[1]. Atazanavir is able to potently induce endoplasmic reticulum (ER) stress response in malignant glioma cells, as indicated by elevated levels of GRP78 and CHOP, and activation of caspase-4, which leads to cell death[3]. |
| 体内活性 | Atazanavir has excellent oral bioavailability in the range of 60-70%[1]. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | Ethanol : 32 mg/mL (45.4 mM)
DMSO : 55 mg/mL (78.03 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
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| 关键字 | CD243 | BMS 232632 | Pgp | Cluster of differentiation 243 | HIV Protease | HIV | inhibit | SARS coronavirus | Human immunodeficiency virus | Inhibitor | Atazanavir | P-glycoprotein | ABCB1 | Cytochrome P450 | CYPs | SARS-CoV | MDR1 | P-gp | BMS232632 | Multidrug resistance protein 1 |
| 相关产品 | Stavudine | 5-Fluorouracil | Emtricitabine | Kaempferol | Dextran sulfate sodium salt (MW 4500-5500) | Hydroxychloroquine | Lamivudine | Naringin | Naringenin | Decanedioic acid |
| 相关库 | 高选择性抑制剂库 | 经典已知活性库 | 神经退行性疾病化合物库 | 膜蛋白靶向化合物库 | EMA 上市药物库 | 抗癌临床化合物库 | 抗病毒库 | FDA 上市药物库 | 离子通道库 | 抗癌药物库 |
United States
