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

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1831
    CAS #: 697761-98-1Purity ≥98%

    Description: Elvitegravir (also known as GS-9137, JTK-303, D06677 or EVG) is a potent 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 is a monoketo acid modified from the distinct diketo acid moiety (DKA) motif and is used for the treatment of HIV infection. The drug received FDA approval on August 27, 2012 for use in adult patients starting HIV treatment for the first time as part of the fixed dose combination known as Stribild.

    References: J Virol. 2008 Jan;82(2):764-74; Expert Rev Anti Infect Ther. 2012 Jan;10(1):13-20. 

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    Molecular Weight (MW)447.88
    FormulaC23H23ClFNO5 
    CAS No.697761-98-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 90 mg/mL (200.9 mM)
    Water:<1 mg/mL 
    Ethanol: 35 mg/mL (78.1 mM)
    Other info

    Chemical Name: 6-[(3-Chloro-2-fluorophenyl)methyl]-1-[(2S)-1-hydroxy-3-methylbutan-2-yl]-7-methoxy-4-oxoquinoline-3-carboxylic acid

    InChi Key: JUZYLCPPVHEVSV-LJQANCHMSA-N

    InChi Code: InChI=1S/C23H23ClFNO5/c1-12(2)19(11-27)26-10-16(23(29)30)22(28)15-8-14(20(31-3)9-18(15)26)7-13-5-4-6-17(24)21(13)25/h4-6,8-10,12,19,27H,7,11H2,1-3H3,(H,29,30)/t19-/m1/s1

    SMILES Code: O=C(C1=CN([[email protected]@H](C(C)C)CO)C2=C(C=C(CC3=CC=CC(Cl)=C3F)C(OC)=C2)C1=O)O

    SynonymsD06677; D-06677; D 06677; EVG, GS-9137; GS-9137; GS9137; GS 9137; JTK 303; JTK-303; JTK303; EVG; Stribild


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    In Vitro

    In vitro activity: 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. 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.

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    References

    J Virol. 2008 Jan;82(2):764-74; Expert Rev Anti Infect Ther. 2012 Jan;10(1):13-20. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Elvitegravir (GS-9137, JTK-303)

    Mechanism of action of EVG. (A) Quantification of HIV-1 DNA species. J Virol. 2008 Jan;82(2):764-74.
     

    Elvitegravir (GS-9137, JTK-303)

    Induction of EVG-resistant HIV-1. Data from MT-2 cells are shown. J Virol. 2008 Jan;82(2):764-74.
     

    Elvitegravir (GS-9137, JTK-303)

    Effect of EVG-selected mutations on IN strand transfer activity and on the inhibition of strand transfer by IN inhibitors. J Virol. 2008 Jan;82(2):764-74.


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