Elvitegravir

Synonyms: GS-9137,JTK-303,D06677

Elvitegravir 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.

Elvitegravir Chemical Structure

Elvitegravir Chemical Structure

CAS: 697761-98-1

Selleck's Elvitegravir has been cited by 32 publications

Purity & Quality Control

Batch: Purity: 99.97%
99.97

Elvitegravir Related Products

Choose Selective Integrase Inhibitors

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human C8166 cells Function assay Antiviral activity against HIV1 LAI 3B infected in human C8166 cells assessed as protection against virus-induced cytopathic effect by MTT assay, EC50=0.21 nM 21763149
MT4 cells Function assay Antiviral activity against HIV1 3B in MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.37 nM 18665580
human MT4 cells Cytotoxicity assay Cytotoxicity against human MT4 cells by MTT assay, CC50=1.15 μM 18665580
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Biological Activity

Description Elvitegravir 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.
Targets
HIV-1 IIIB [1]
(Cell-free assay)
HIV-2 ROD [1]
(Cell-free assay)
HIV-2 EHO [1]
(Cell-free assay)
0.7 nM 1.4 nM 2.8 nM
In vitro
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. [1] 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. [2]

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04047420 Completed
HIV Infections
National Institute of Allergy and Infectious Diseases (NIAID)|CONRAD
December 11 2019 Phase 1
NCT03976752 Completed
HIV/AIDS
Emory University|Centers for Disease Control and Prevention
March 13 2019 Phase 1
NCT02985996 Completed
HIV Infections
Emory University|Centers for Disease Control and Prevention
February 6 2017 Phase 1
NCT02251236 Completed
HIV
University of California San Diego|Gilead Sciences|University at Buffalo
January 2016 Not Applicable
NCT02600819 Completed
HIV-1 Infection
Gilead Sciences
December 14 2015 Phase 3
NCT02295384 Completed
HIV
Holdsworth House Medical Practice|Gilead Sciences
November 2014 --

Chemical Information & Solubility

Molecular Weight 447.88 Formula

C23H23ClFNO5

CAS No. 697761-98-1 SDF Download Elvitegravir SDF
Smiles CC(C)C(CO)N1C=C(C(=O)C2=C1C=C(C(=C2)CC3=C(C(=CC=C3)Cl)F)OC)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 89 mg/mL ( (198.71 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 35 mg/mL

Water : Insoluble


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In vivo
Batch:

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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