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Elvitegravir Integrase inhibitor

Cat.No.S2001

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.
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Quality Control

Batch: Purity: 99.97%
99.97

Cell Culture, Treatment & Working Concentration

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
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
human MT4 cells Cytotoxicity assay Cytotoxicity against human MT4 cells by MTT assay, CC50=1.15 μM
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Solubility

In vitro
Batch:

DMSO : 89 mg/mL (198.71 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 35 mg/mL

Water : Insoluble

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Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Chemical Information, Storage & Stability

Molecular Weight 447.88 Formula

C23H23ClFNO5

Storage (From the date of receipt)
CAS No. 697761-98-1 Download SDF Storage of Stock Solutions

Synonyms GS-9137,JTK-303,D06677 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

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
HIV-1 IIIB
(Cell-free assay)
0.7 nM
HIV-2 ROD
(Cell-free assay)
1.4 nM
HIV-2 EHO
(Cell-free assay)
2.8 nM
In vitro

Elvitegravir inhibits PBMC and PA with IC50 of 0.89 and 20 nM, respectively. This compound prevents the integration of HIV-1 cDNA through the inhibition of DNA strand transfer. It 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. This inhibitor blocks the replication of HIV-1 clinical isolates carrying NRTI, NNRTI, and PI resistance-associated genotypes. It inhibits the HIV replication at a step that occurs after reverse transcription but before proteolytic cleavage, consistent with the integration step. This chemical inhibits the synthesis of strand transfer products with an IC50 of 54 nM. It blocks integration via the inhibition of IN-mediated strand transfer. This agent 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. It 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. This compound 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.

References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-07-25)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06274398 COMPLETED
Safety Issues
Eastern Virginia Medical School
2024-01-16 PHASE1
NCT06087913 COMPLETED
Safety Issues
Eastern Virginia Medical School
2023-11-08 PHASE1
NCT04040075 TERMINATED
HIV-1-infection
Southampton Healthcare, Inc.
2019-07-01 PHASE4
NCT03717129 COMPLETED
Healthy Volunteers
Johns Hopkins University
2019-04-15 PHASE4
NCT04047420 COMPLETED
HIV Infections
National Institute of Allergy and Infectious Diseases (NIAID)
2019-12-11 PHASE1
NCT02859558 COMPLETED
HIV-1 Infection
Advancing Clinical Therapeutics Globally for HIV/AIDS and Other Infections
2017-01-24 PHASE2

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