Atazanavir (BMS-232632) Sulfate - 10mM in DMSO , Human immunodeficiency virus type 1 protease inhibitor, CAS No.229975-97-7, Human immunodeficiency virus type 1 protease inhibitor

CAS: 229975-97-7 Cat. No.: A407846 Molecular Weight: 802.93 EC Number: 620-495-2 PubChem CID: 158550

GRADE & PURITY 10mM in DMSO

Synonyms

(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)

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

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%

Specifications

Synonyms

(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)

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

Atazanavir Sulfate (BMS-232632) is a HIV protease inhibitor with K_i of 2.66 nM in a cell-free assay.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Mechanism of action

Human immunodeficiency virus type 1 protease inhibitor

Names and Identifiers

• Isomeric SMILES: CC(C)(C)[C@@H](C(=O)N[C@@H](CC1=CC=CC=C1)[C@H](CN(CC2=CC=C(C=C2)C3=CC=CC=N3)NC(=O)[C@H](C(C)(C)C)NC(=O)OC)O)NC(=O)OC.OS(=O)(=O)O
• PubChem CID: 158550
• Molecular Weight: 802.93

Chemical and Physical Properties

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