S44802 |
Atazanavir Sulfate |
| MedMol | ≥98% |
- 产品描述： 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.
- 靶点： HIV Protease;P450;P-gp;SARS-CoV
- 体内研究： 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
- 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. Zhang D, et al.In vitro inhibition of UDP glucuronosyltransferases by atazanavir and other HIV protease inhibitors and the relationship of this property to in vivo bilirubin glucuronidation.Drug Metab Dispos, 2005, 33(11), 1729-1739. 2. Perloff ES, et al.Atazanavir: effects on P-glycoprotein transport and CYP3A metabolism in vitro.Drug Metab Dispos, 2005, 33(6), 764-770. 3. Parker RA, et al.Endoplasmic reticulum stress links dyslipidemia to inhibition of proteasome activity and glucose transport by HIV protease inhibitors.Mol Pharmacol, 2005, 67(6), 1909-1919. 4. Pyrko P, et al.HIV-1 protease inhibitors nelfinavir and atazanavir induce malignant glioma death by triggering endoplasmic reticulum stress.Cancer Res, 2007, 67(22), 10920-10928. 5.Robinson BS, et al.BMS-232632, a highly potent human immunodeficiency virus protease inhibitor that can be used in combination with other available antiretroviral agents.Antimicrob Agents Chemother, 2000, 44(8), 2093-2099.
- 溶解性： Soluble in DMSO
- 保存条件： 2-8℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 1.245 ml 6.227 ml 12.454 ml 5 mM 0.249 ml 1.245 ml 2.491 ml 10 mM 0.125 ml 0.623 ml 1.245 ml 50 mM 0.025 ml 0.125 ml 0.249 ml
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输入产品批号：
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
