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Atazanavir sulfate

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。

CAS号

229975-97-7

分子式

C38H52N6O7·H2SO4

主要靶点

HIV Protease|P-gp|P450|SARS-CoV

仅限科研使用

Cat No : CM04619

Print datasheet

Synonyms

BMS-232632 sulfate|BMS-232632|阿扎那韦硫酸盐|硫酸阿扎那韦

验证数据展示

  • CAS No.: 229975-97-7

    Atazanavir sulfate
    CAS#: 229975-97-7

产品信息

Atazanavir 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.

CAS号 229975-97-7
分子式 C38H52N6O7·H2SO4
主要靶点 HIV Protease|P-gp|P450|SARS-CoV
主要通路 蛋白酶体|代谢|离子通道|神经科学|微生物学
分子量 802.93
纯度 99.67%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 BMS-232632 sulfate|BMS-232632|阿扎那韦硫酸盐|硫酸阿扎那韦

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。

溶解度

H2O:<1 mg/mL,Ethanol:<1 mg/mL,DMSO:96 mg/mL (119.6 mM)

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)

参考文献

1.Robinson BS, et al. Antimicrob Agents Chemother, 2000, 44(8), 2093-2099.
2.Zhang D, et al. Drug Metab Dispos, 2005, 33(11), 1729-1739.
3.Pyrko P, et al. Cancer Res, 2007, 67(22), 10920-10928.
4.Parker RA, et al. Mol Pharmacol, 2005, 67(6), 1909-1919.
5.Perloff ES, et al. Drug Metab Dispos, 2005, 33(6), 764-770.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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=
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C1   V1   C2   V2