| 名稱 | Atazanavir sulfate |
| 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. |
| 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) |
| 激酶實(shí)驗(yàn) | 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. |
| 體內(nèi)活性 | 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(zhǎng),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)。 |
| 存儲(chǔ)條件 | Keep away from moisture,
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (2.49 mM), Sonication is recommended.
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 250 mg/mL (311.36 mM), Sonication is recommended.
10% DMSO+90% Saline : 10 mg/mL (12.45 mM), Solution.
H2O : < 1 mg/mL (insoluble or slightly soluble)
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| 關(guān)鍵字 | SARS-CoV | SARSCoV | P-gp?(P-glycoprotein) | P-gp | Pgp | P-glycoprotein | Multidrug resistance protein 1 | MDR1 | HIVProtease | HIV protease | HIV | Cytochrome P450 | Cluster of differentiation 243 | CD243 | BMS232632 Sulfate | BMS232632 | BMS 232632 Sulfate | BMS 232632 | Atazanavir | ABCB1 |
| 相關(guān)產(chǎn)品 | Guanidine hydrochloride | glycine | Glycerol | Aceglutamide | Malic acid | Sucrose | Dextran sulfate sodium salt (MW 5000) | Guanidine thiocyanate | Gluconate Calcium | Thymidine | L-Cysteine | D(+)-Raffinose pentahydrate |
| 相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | 抗癌上市藥物庫(kù) | 已知活性化合物庫(kù) | 臨床失敗化合物庫(kù) | 抗衰老化合物庫(kù) | 抗病毒庫(kù) | 膜蛋白靶向化合物庫(kù) | 神經(jīng)退行性疾病化合物庫(kù) | 免疫/炎癥分子化合物庫(kù) | 藥物功能重定位化合物庫(kù) | 抗癌臨床化合物庫(kù) | 抗癌藥物庫(kù) |