Elvitegravir (JTK-303) - Moligand™, 10mM in DMSO , Human immunodeficiency virus type 1 integrase inhibitor, CAS No.697761-98-1, Human immunodeficiency virus type 1 integrase inhibitor

CAS: 697761-98-1 Cat. No.: E408975 Molecular Weight: 447.88 EC Number: 691-248-4

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

GS-9137 | (S)-6-(3-chloro-2-fluorobenzyl)-1-(1-hydroxy-3-methylbutan-2-yl)-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Elvitegravir (JTK-303) Elvitegravir (GS-9137, JTK-303) is an HIV integrase inhibitor for HIV-1 IIIB , HIV-2 EHO and HIV-2 ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM in cell-free assays, respectively.
In vitro

Elvitegravir inhibits PBMC and PA with IC50 of 0.89 and 20 nM, respectively. Elvitegravir prevents the integration of HIV-1 cDNA through the inhibition of DNA strand transfer. Elvitegravir suppresses the replication of HIV-1, including various subtypes and multiple-drug-resistant clinical isolates, and HIV-2 strains with a 50% effective concentration in the subnanomolar to nanomolar range. Elvitegravir inhibits the replication of HIV-1 clinical isolates carrying NRTI, NNRTI, and PI resistance-associated genotypes. Elvitegravir inhibits the HIV replication at a step that occurs after reverse transcription but before proteolytic cleavage, consistent with the integration step. Elvitegravir inhibits the synthesis of strand transfer products with an IC50 of 54 nM. Elvitegravir blocks integration via the inhibition of IN-mediated strand transfer. Elvitegravir inhibits the integration of the HIV-based vector used as a positive control for the luciferase assay with an EC50 of 0.8 nM, as observed in the MAGI assay with HIV-1IIIB. Elvitegravir suppresses the replication of MLV infection with IC50 of 5.8 nM as well as that of the primate retrovirus SIV (IC50 = 0.5 nM), revealing that IN inhibitors have antiviral activity against a broad range of retroviruses. EVG is active against HIV-1 and HIV-2 and has a serum-free antiviral IC50 of 0.3-0.9 nM in peripheral blood mononuclear cells.

In vivo

Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonyms

GS-9137 | (S)-6-(3-chloro-2-fluorobenzyl)-1-(1-hydroxy-3-methylbutan-2-yl)-7-methoxy-4-oxo-1, 4-dihydroquinoline-3-carboxylic acid

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Elvitegravir (GS-9137, JTK-303) is an HIV integrase inhibitor for HIV-1 IIIB, HIV-2 EHO and HIV-2 ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM in cell-free assays, respectively.

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.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Human immunodeficiency virus type 1 integrase inhibitor

Product Properties

• ALogP: 5.3

Names and Identifiers

• Isomeric SMILES: CC(C)[C@@H](CO)N1C=C(C(=O)C2=C1C=C(C(=C2)CC3=C(C(=CC=C3)Cl)F)OC)C(=O)O
• Molecular Weight: 447.88
• Reaxy-Rn: 25499207
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=25499207&ln=

References

1. Zhaohong Su, Shiyu Hu, Yanqun Xu, Ju Liu, Pengcheng Liang, Jiaqi Wang, Qinyi Cao, Yi Peng, Wei Zhang, Duoqing Fan.  (2024)  A smart portable electrochemical sensor based on electrodeposited ferrocene-functionalized multiwalled carbon nanotubes for in vitro and in vivo detection of nicotine in tobacco samples.  NEW JOURNAL OF CHEMISTRY,  48  (8): (3370-3380).  [PMID:] [10.1039/D3NJ05035A]