Elvitegravir (GS-9137, JTK-303)

Catalog No.S2001

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

Molecular Weight(MW): 447.88

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.

Size Price Stock Quantity  
In DMSO USD 160 In stock
USD 120 In stock
USD 470 In stock
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6 Customer Reviews

  • PhA efflux in MDCKII-BCRP cells. Concentration-dependent inhibition of BCRP/ABCG2 by elvitegravir and vicriviroc. Each curve depicts one representative experiment of a series of three or four; each concentration was tested in 30000 cells.

     

     

    J Antimicrob Chemother 2011 66, 802-812. Elvitegravir (GS-9137, JTK-303) purchased from Selleck.

    mdr1a/b and ABCB1 inhibition measured by calcein assay. Concentration-dependent effects of elvitegravir and vicriviroc on calcein accumulation in P388/dx cells (a) and L-MDR1 cells (b). Each curve depicts one representative experiment of a series of three or four. Data are expressed as means+SEM.

    J Antimicrob Chemother 2011 66, 802-812. Elvitegravir (GS-9137, JTK-303) purchased from Selleck.

  • Effect of antiretrovirals and positive control rifampicin (at 10 μmol/L) on ABCB1 function in LS180 cells after 3 and 7 days (d) of treatment. ABCB1 function was normalized to the medium control. Data are expressed as means+SEM for n¼4. **P<0.01.

    J Antimicrob Chemother 2011 66, 802-812. Elvitegravir (GS-9137, JTK-303) purchased from Selleck.

    Functional windows of antiviral drug action. (A) At the indicated times, 10-fold EC95 adjusted levels of RAL, EVG, AZT, or NVP were added to HIV-Luc-infected cultures. Cells were lysed at 48 h postinfection, and luciferase activities are expressed as the percentage of the response in non-drug-treated cells. (B) Results of an experiment similar to that in panel A, except cells were treated with 10 the EC95 of RAL, 100 the EC95 of RAL, 10 the EC95 of EVG, or 100 the EC95 of EVG at the indicated times. Numbers indicate the time (in h) required for 50% inhibition compared to the no-drug control (dashed lines).

     

     

    Antim Ag Ch 2011 55, 42-49. Elvitegravir (GS-9137, JTK-303) purchased from Selleck.

  • HIV-Luc was preincubated with the indicated level of drug for 1 h prior to 2 min of MNP-mediated infection. Extensively washed cultures were incubated in the absence of drug for 2 days prior to cell lysis and luciferase assays. The NN-luc control virus was omitted from the virucidal activity assays.

     

     

    Antim Ag Ch 2011 55, 42-49. Elvitegravir (GS-9137, JTK-303) purchased from Selleck.

    Cells were treated with the indicated concentrations of Elvitegravir.

    2010 Dr. Johanna Weiss of University Hospital Heidelberg. Elvitegravir (GS-9137, JTK-303) purchased from Selleck.

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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]

Protocol

Solubility (25°C)

In vitro DMSO 90 mg/mL (200.94 mM)
Ethanol 35 mg/mL (78.14 mM)
Water slightly soluble or insoluble
In vivo Add solvents individually and in order:

* 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 powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02882230 Not yet recruiting HIV Fondation Ophtalmologique Adolphe de Rothschild September 2016 --
NCT02859558 Not yet recruiting HIV-1 Infection AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) August 2016 Phase 2
NCT02475135 Completed Healthy Janssen Sciences Ireland UC June 2015 Phase 1
NCT02470650 Recruiting Patient Compliance|Antiretroviral Therapy Intolerance Juan A. Arnaiz|Hospital Clinic of Barcelona June 2015 Phase 4
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

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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Integrase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID