Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Atazanavir sulfate (BMS-232632 sulfate) 是一种氮杂肽和 HIV 蛋白酶抑制剂,与其他抗 HIV 药物联合用于治疗 HIV 感染和艾滋病。它也是SARS-CoV 3CLpro 抑制剂,IC50为 3.49 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 137 | 现货 | ||
5 mg | ¥ 289 | 现货 | ||
10 mg | ¥ 463 | 现货 | ||
25 mg | ¥ 879 | 现货 | ||
50 mg | ¥ 1,450 | 现货 | ||
100 mg | ¥ 1,980 | 现货 | ||
200 mg | ¥ 2,960 | 现货 | ||
500 mg | ¥ 4,890 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 397 | 现货 |
产品描述 | Atazanavir sulfate (BMS-232632 sulfate) is an azapeptide and HIV-PROTEASE INHIBITOR that is used in the treatment of HIV INFECTIONS and AIDS in combination with other ANTI-HIV AGENTS. |
靶点活性 | HIV protease:2.66 nM(Ki) |
体内活性 | 30 mM Atazanavir作用于LS180V细胞,免疫反应的P-gp表达提高2.5倍,细胞内Rh123降低。Atazanavir抑制U251,T98 g和 LN229胶质母细胞瘤细胞系的细胞生长,显著地提高GRP78和CHOP蛋白水平。Atazanavir也抑制人类20S proteasome 蛋白酶体。Atazanavir作用于U251胶质瘤细胞,各种不同大小的多聚泛素化蛋白质明显增加。Atazanavir 作用于病毒感染的H9细胞,抑制病毒gag前体p55聚合蛋白的蛋白水解裂解,IC50为~47 nM。Atazanavir作用于RF/MT-2 株,具有有效的抗病毒活性,EC50 为3.89 nM。30 μM Atazanavir作用于HepG2细胞,改变内质网应激的幅度和UPR基因表达。 |
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 | To determine cytotoxicity, host cells are incubated in the presence of serially diluted Atazanavir for 6 days and cell viability is quantitated using an XTT[2,3-bis(2-methoxy-4-nitro-5-sulfophenyl-2H-tetrazolium-5-carboxanilide] assay to calculate the 50% cytotoxic concentrations (CC50s). To assess the effect of human serum proteins on antiviral activity, the 10% fetal calf serum normally used for assays is replaced with 40% adult human serum or 1 mg of α1-acid glycoprotein/mL.(Only for Reference) |
别名 | 阿扎那韦硫酸盐, BMS-232632, BMS-232632 sulfate, 硫酸阿扎那韦 |
分子量 | 802.93 |
分子式 | C38H52N6O7·H2SO4 |
CAS No. | 229975-97-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 96 mg/mL (119.6 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 |
DMSO | 1 mM | 1.2454 mL | 6.2272 mL | 12.4544 mL | 31.136 mL |
5 mM | 0.2491 mL | 1.2454 mL | 2.4909 mL | 6.2272 mL | |
10 mM | 0.1245 mL | 0.6227 mL | 1.2454 mL | 3.1136 mL | |
20 mM | 0.0623 mL | 0.3114 mL | 0.6227 mL | 1.5568 mL | |
50 mM | 0.0249 mL | 0.1245 mL | 0.2491 mL | 0.6227 mL | |
100 mM | 0.0125 mL | 0.0623 mL | 0.1245 mL | 0.3114 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 sulfate 229975-97-7 Membrane transporter/Ion channel Metabolism Microbiology/Virology Neuroscience Proteases/Proteasome P450 SARS-CoV HIV Protease P-gp 阿扎那韦硫酸盐 BMS-232632 Sulfate CYPs Human immunodeficiency virus BMS-232632 CD243 Inhibitor ABCB1 Atazanavir Sulfate Cytochrome P450 BMS-232632 sulfate BMS232632 Sulfate Multidrug resistance protein 1 BMS232632 BMS 232632 Sulfate Cluster of differentiation 243 SARS coronavirus 硫酸阿扎那韦 Atazanavir Pgp HIV BMS 232632 inhibit P-glycoprotein MDR1 inhibitor