| 產(chǎn)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. |
| 靶點(diǎn)： |
HIV Protease;P450;P-gp;SARS-CoV;P450;SARS-CoV;HIVProtease;P-gp |
| 體內(nèi)研究： |
30 mM Atazanavir作用于LS180V細(xì)胞,免疫反應(yīng)的P-gp表達(dá)提高2.5倍,細(xì)胞內(nèi)Rh123降低。Atazanavir抑制U251,T98 g和 LN229膠質(zhì)母細(xì)胞瘤細(xì)胞系的細(xì)胞生長,顯著地提高GRP78和CHOP蛋白水平。Atazanavir也抑制人類20S proteasome 蛋白酶體。Atazanavir作用于U251膠質(zhì)瘤細(xì)胞,各種不同大小的多聚泛素化蛋白質(zhì)明顯增加。Atazanavir 作用于病毒感染的H9細(xì)胞,抑制病毒gag前體p55聚合蛋白的蛋白水解裂解,IC50為~47 nM。Atazanavir作用于RF/MT-2 株,具有有效的抗病毒活性,EC50 為3.89 nM。30 μM Atazanavir作用于HepG2細(xì)胞,改變內(nèi)質(zhì)網(wǎng)應(yīng)激的幅度和UPR基因表達(dá) |
| 細(xì)胞實(shí)驗(yàn)： |
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) |
| 參考文獻(xiàn)： |
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 |
| 保存條件： |
2-8℃ |
| 配置溶液濃度參考： |
|
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 |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
上海工商
危險(xiǎn)品化學(xué)品經(jīng)營許可證（不帶存儲(chǔ)）
營業(yè)執(zhí)照(三證合一)
北京