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Atazanavir Sulfate是一种HIV protease(HIV蛋白酶)抑制剂,抑制HIV Atazanavir,Ki值为2.66 nM。A sulfate salt form of atazanavir that is an highly potent HIV-1 protease inhibitor.
Information
Atazanavir (BMS-232632) Sulfate Atazanavir Sulfate (BMS-232632) is a HIV protease inhibitor with K i of 2.66 nM in a cell-free assay.
In vitro
Atazanavir inhibits the proteolytic cleavage of the viral gag precursor p55 polyprotein with IC50 of ~47 nM in virus-infected H9 cells. Atazanavir exhibits potent antiviral activity with EC50 of 3.89 nM in RF/MT-2 strains. . Atazanavir is shown to be an inhibitor of bilirubin glucuronidation with IC50 of 2.4 μM. Atazanavir inhibits recombinant UGT1A1 with Ki of 1.9 μM. Atazanavir inhibits cell growth in U251, T98G, and LN229 glioblastoma cell lines, with strikingly increased GRP78 and CHOP protein levels. Atazanavir causes a prominent increase of polyubiquitinated proteins of various different sizes in U251 glioblastoma cells. Atazanavir also inhibits human 20S proteasome with IC50 of 26 μM. Atazanavir (30 μM) changes the magnitudes of ER stress and UPR gene expression in HepG2 cells. Atazanavir (30 mM) causes a 2.5-fold increase in immunoreactive P-gp expression with decreased intracellular Rh123 in LS180V cells.
In vivo
Cell Data
cell lines:OPM-2, RPMI-8226, U-266, and INA-6
Concentrations:15 nM
Incubation Time:6 days
Powder Purity:≥97%
H318: 造成严重的眼睛损伤
H372: 通过长时间或反复暴露对器官造成损害