Atazanavir (BMS-232632) Sulfate, 人体免疫缺陷病毒 1 型蛋白酶抑制剂

艾滋病毒蛋白酶抑制剂
  • 10mM in DMSO
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A407846-1ml
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Compound libraries (12326)

基本描述

别名 阿扎那韦 (BMS-232632) 硫酸盐
英文别名 (3S,​8S,​9S,​12S)​-3,​12-​bis(1,​1-​dimethylethyl)​-​8-​hydroxy-​4,​11-​dioxo-​9-​(phenylmethyl)​-​6-​[[4-​(2-​pyridinyl)​phenyl]​methyl]​-​2,​5,​6,​10,​13-​pentaazatetradecaned​ioic acid 1,​14-​dimethyl ester, sulfate (1:1)
规格或纯度 10mM in DMSO
英文名称 Atazanavir (BMS-232632) Sulfate
生化机理 硫酸阿扎那韦(BMS-232632)是一种 HIV 蛋白酶抑制剂,在无细胞试验中的Ki值为 2.66 nM。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 抑制剂
作用机制 人体免疫缺陷病毒 1 型蛋白酶抑制剂
产品介绍

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%

名称和识别符

Canonical SMILES COC(=O)NC(C(=O)NC(CC1=CC=CC=C1)C(O)CN(CC2=CC=C(C=C2)C3=NC=CC=C3)NC(=O)C(NC(=O)OC)C(C)(C)C)C(C)(C)C.O[S](O)(=O)=O
分子量 802.93

化学和物理性质

溶解性 Solubility (25°C) In vitro DMSO: 100 mg/mL (116.01 mM); Ethanol: 100 mg/mL (116.01 mM); Water: Insoluble;

安全和危险性(GHS)

质量标准

Concentration(Compounding value) 9-11(mmol/L)
Appearance(A407846) Colorless Transparent Liquid
Record the entire process by video Conform

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

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