Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Atazanavir (BMS-232632) 是一种高选择性的HIV-1蛋白酶抑制剂,可研究艾滋病毒感染。它也是SARS-CoV 3CLpro 的抑制剂,IC50为 3.49 μM。它是CYP3A4的底物和抑制剂,也是P-糖蛋白的抑制剂和诱导剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 289 | 现货 | ||
10 mg | ¥ 463 | 现货 | ||
25 mg | ¥ 847 | 现货 | ||
50 mg | ¥ 1,450 | 现货 | ||
100 mg | ¥ 1,980 | 现货 | ||
200 mg | ¥ 2,970 | 现货 | ||
500 mg | ¥ 4,890 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 468 | 现货 |
产品描述 | Atazanavir (BMS-232632)(BMS-232632) is an highly effective HIV-1 protease inhibitor. |
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]. |
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. |
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) |
别名 | Zrivada, Reyataz, Latazanavir, 阿扎那韦, BMS-232632 |
分子量 | 704.86 |
分子式 | C38H52N6O7 |
CAS No. | 198904-31-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 32 mg/mL (45.4 mM)
DMSO: 65 mg/mL (92.2 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 1.4187 mL | 7.0936 mL | 14.1872 mL | 35.468 mL |
5 mM | 0.2837 mL | 1.4187 mL | 2.8374 mL | 7.0936 mL | |
10 mM | 0.1419 mL | 0.7094 mL | 1.4187 mL | 3.5468 mL | |
20 mM | 0.0709 mL | 0.3547 mL | 0.7094 mL | 1.7734 mL | |
DMSO | 50 mM | 0.0284 mL | 0.1419 mL | 0.2837 mL | 0.7094 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Atazanavir 198904-31-3 Membrane transporter/Ion channel Metabolism Microbiology/Virology Neuroscience Proteases/Proteasome P450 SARS-CoV HIV Protease P-gp CD243 BMS 232632 Pgp Zrivada Cluster of differentiation 243 Reyataz HIV inhibit SARS coronavirus Latazanavir Human immunodeficiency virus Inhibitor P-glycoprotein ABCB1 Cytochrome P450 CYPs MDR1 阿扎那韦 BMS232632 Multidrug resistance protein 1 BMS-232632 inhibitor