[CAS NO. 229975-97-7] Atazanavir (BMS-232632) Sulfate

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PRODUCTS SPECIFICATIONS [229975-97-7]

Catalog

SLK-S1457

Brand

Selleck

CAS

229975-97-7

DESCRIPTION [229975-97-7]

Overview

MDL	MFCD08067748
Molecular Weight	802.93
Molecular Formula	C38H52N6O7.H2SO4
SMILES	S(=O)(=O)(O)O.N(CC1=CC=C(C=C1)C2=CC=CC=N2)(C[C@@H]([C@H](CC3=CC=CC=C3)NC([C@@H](NC(OC)=O)[C@](C)(C)C)=O)O)NC([C@@H](NC(OC)=O)[C@](C)(C)C)=O

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.2454 mL	6.2272 mL	12.4544 mL
5 mM	0.2491 mL	1.2454 mL	2.4909 mL
10 mM	0.1245 mL	0.6227 mL	1.2454 mL
50 mM	0.0249 mL	0.1245 mL	0.2491 mL

Description

Atazanavir Sulfate (BMS-232632-05, Reyataz) is a inhibitor with of 2.66 nM in a cell-free assay.

Features

Atazanavir is generally more potent than other HIV-1 Prt inhibitors, including IDV, SQV, RTV, NFV, and APV.

Targets

HIV protease ^[1]
(Cell-free assay)

2.66 nM(Ki)

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.

References

[1] Robinson BS, et al. Antimicrob Agents Chemother, 2000, 44(8), 2093-2099.
[2] Zhang D, et al. Drug Metab Dispos, 2005, 33(11), 1729-1739.
[3] Pyrko P, et al. Cancer Res, 2007, 67(22), 10920-10928.
[4] Parker RA, et al. Mol Pharmacol, 2005, 67(6), 1909-1919.
[5] Perloff ES, et al. Drug Metab Dispos, 2005, 33(6), 764-770.

Synonyms

2,5,6,10,13-Pentaazatetradecanedioic acid, 3,12-bis(1,1-dimethylethyl)-8-hydroxy-4,11-dioxo-9-(phenylmethyl)-6-[[4-(2-pyridinyl)phenyl]methyl]-, 1,14-dimethyl ester, (3S,8S,9S,12S)-, sulfate (1:1)

2,5,6,10,13-Pentaazatetradecanedioic acid, 3,12-bis(1,1-dimethylethyl)-8-hydroxy-4,11-dioxo-9-(phenylmethyl)-6-[[4-(2-pyridinyl)phenyl]methyl]-, dimethyl ester, (3S,8S,9S,12S)-, sulfate (1:1) (salt)

Atazanavir sulfate

Atazor

Reyataz