阿扎那韦 T0100L

Product Introduction
Bioactivity


英文名: Atazanavir

描述: 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。

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 具有很强的体外活性，对野生型病毒的EC50和EC90 分别为2-5 nM和9-15 nM[1]。Atazanavir 能有效诱导恶性胶质瘤细胞的内质网（ER）应激反应，促使 GRP78 和 CHOP 水平升高以及 caspase-4 激活，促进细胞死亡[3]。

体内活性: Atazanavir 的口服生物利用度非常高，在 60%-70% 之间[1]。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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)


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: Clopidogrel hydrogen sulfate | Linderane | Naringenin | 5,7-DIMETHOXYFLAVONE | Beta-Tetralone | α-​Terpinyl acetate | Germacrone | Avasimibe | CYP17-IN-1 | Clomethiazole

相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Approved Drug Library | Highly Selective Inhibitor Library | EMA Approved Drug Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途