Elvitegravir (JTK-303)

Catalog No.S2001 Synonyms: GS-9137

For research use only.

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.

Elvitegravir (JTK-303) Chemical Structure

CAS No. 697761-98-1

Selleck's Elvitegravir (JTK-303) has been cited by 26 publications

Purity & Quality Control

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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)
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human C8166 cells NH3kbHBHfW6ldHnvckBie3OjeR?= NGnyOG5CdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJUVZzIFzBTUA{SiCrbn\lZ5Rm\CCrbjDoeY1idiCFOEG2OkBk\WyuczDhd5Nme3OnZDDhd{Bxem:2ZXP0bY9vKGGpYXnud5Qhfmm{dYOtbY5lfWOnZDDjfZRweGG2aHnjJIVn\mWldDDifUBOXFRiYYPzZZktKEWFNUC9NE4zOSCwTR?= MUiyNVc3OzF2OR?=
MT4 cells M3y1fWZ2dmO2aX;uJIF{e2G7 MnmxRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGlXOSB|QjDpckBOXDRiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB3cXK3cz3pcoR2[2WmIHP5eI9x[XSqaXOg[YZn\WO2IHL5JG1VXCCjc4PhfUwhTUN3ME2wMlM4KG6P NV\yRW17OTh4NkW1PFA>
human MT4 cells NYjzbYd6S3m2b4TvfIlkcXS7IHHzd4F6 MULDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNWFQh[2WubIOgZpkhVVSWIHHzd4F6NCCFQ{WwQVEvOTVizszN MXqxPFY3PTV6MB?=

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 89 mg/mL
(198.71 mM)
Ethanol 35 mg/mL
(78.14 mM)
Water 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 Information

Molecular Weight 447.88
Formula

C23H23ClFNO5

CAS No. 697761-98-1
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

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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.

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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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03976752 Completed Drug: Genvoya HIV/AIDS Emory University|Centers for Disease Control and Prevention March 13 2019 Phase 1
NCT02985996 Completed Drug: Truvada|Drug: Genvoya HIV Infections Emory University|Centers for Disease Control and Prevention February 6 2017 Phase 1
NCT02251236 Completed Drug: Stribild|Drug: Genvoya HIV University of California San Diego|Gilead Sciences|University at Buffalo January 2016 Not Applicable
NCT02600819 Completed Drug: E/C/F/TAF|Drug: B/F/TAF HIV-1 Infection Gilead Sciences December 14 2015 Phase 3
NCT02295384 Completed Other: Retrospective Audit HIV Holdsworth House Medical Practice|Gilead Sciences November 2014 --
NCT02219217 Completed Drug: Dolutegravir Elvitegravir and Cobicistat HIV St Stephens Aids Trust|ViiV Healthcare October 2014 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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