Elvitegravir (GS-9137, JTK-303)

Catalog No.S2001

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.

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Elvitegravir (GS-9137, JTK-303) Chemical Structure

Elvitegravir (GS-9137, JTK-303) Chemical Structure
Molecular Weight: 447.88

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Elvitegravir (GS-9137, JTK-303) is available in the following compound libraries:

Product Information

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  • Elvitegravir (GS-9137, JTK-303) Mechanism

Product Description

Biological Activity

Description 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.
Targets HIV-1 IIIB [1]
(Cell-free assay)
HIV-2 ROD [1]
(Cell-free assay)
HIV-2 EHO [1]
(Cell-free assay)
IC50 0.7 nM 1.4 nM 2.8 nM
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]
In vivo

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Shimura K, et al. J Virol. 2008, 82(2), 764-774.

[2] Lampiris HW. Expert Rev Anti Infect Ther. 2012, 10(1), 13-20.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT02470650 Recruiting Patient Compliance|Antiretroviral Therapy Intolerance Juan A. Arnaiz|Hospital Clinic of Barcelona June 2015 Phase 4
NCT02475135 Completed Healthy Janssen Sciences Ireland UC June 2015 Phase 1
NCT02397096 Recruiting HIV-1 Infection Merck Sharp & Dohme Corp. June 2015 Phase 3
NCT02351908 Active, not recruiting HIV St Stephens Aids Trust|Merck Sharp & Dohme Corp. March 2015 Phase 4
NCT02477527 Completed HIV|AIDS|Sleep Disorders Midtown Medical Center, Tampa, FL|Gilead Sciences February 2015 Phase 4

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Chemical Information

Download Elvitegravir (GS-9137, JTK-303) SDF
Molecular Weight (MW) 447.88


CAS No. 697761-98-1
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 90 mg/mL (200.94 mM)
Ethanol 35 mg/mL (78.14 mM)
Water <1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name (S)-6-(3-chloro-2-fluorobenzyl)-1-(1-hydroxy-3-methylbutan-2-yl)-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid

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.

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