1. Metabolic Enzyme/Protease
    Anti-infection
  2. HIV Integrase
    HIV

Elvitegravir (Synonyms: GS-9137; JTK-303; EVG; D06677)

Cat. No.: HY-14740 Purity: 99.78%
Data Sheet SDS Handling Instructions

Elvitegravir is an HIV integrase inhibitor for HIV-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.

For research use only. We do not sell to patients.
Elvitegravir Chemical Structure

Elvitegravir Chemical Structure

CAS No. : 697761-98-1

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $83 In-stock
10 mg $75 In-stock
50 mg $290 In-stock
100 mg $520 In-stock
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500 mg   Get quote  

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    Elvitegravir purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2016;38:1111-1120.

    Arithmetic means±SEM (n=10) of erythrocyte annexin-V-binding following incubation for 48 hours to Ringer solution without (white bar) or with (black bars) Elvitegravir (0.5-2.5 µg/mL).

    Elvitegravir purchased from MCE. Usage Cited in: Antimicrob Agents Chemother. 2015 Dec;59(12):7666-7670.

    Effects of antiviral drugs on cellular uptake of fluorescein by BeWo cells. The cells are incubated with 1 μM fluorescein in the presence of 100 μM compounds for 10 min at 37°C.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Elvitegravir is an HIV integrase inhibitor for HIV-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.

    IC50 & Target

    IC50: 0.7 nM (HIV-1IIIB), 2.8 nM (HIV-2EHO), 1.4 nM(HIV-2ROD)[1]

    In Vitro

    Elvitegravir (EVG) blocks the integration of HIV-1 cDNA through the inhibition of DNA strand transfer. Elvitegravir exerts potent anti-HIV activity against not only wild-type strains but also drug-resistant clinical isolates. Interestingly, Elvitegravir also shows antiviral activity against murine leukemia virus (MLV) and simian immunodeficiency virus (SIV). Elvitegravir shows potent antiviral activity against three laboratory strains of HIV, with EC50 values in the subnanomolar to nanomolar range. Next, the activity of Elvitegravir is evaluated against wild-type clinical isolates representing various subtypes of HIV-1. Elvitegravir suppresses the replication of all HIV-1 subtypes tested, with an antiviral EC50 ranging from 0.1 to 1.26 nM. Moreover, Elvitegravir suppresses the replication of HIV-1 clinical isolates carrying NRTI, NNRTI, and PI resistance-associated genotypes, as did a control IN inhibitor, the compound L-870,810. The cytotoxicities of these inhibitors are also determined using an MTT colorimetric assay. Mean values for the concentration that suppresses the viability of target cells by 50% for Elvitegravir and L-870,810 in PBMC obtained from three independent donors are 4.6±0.5 μM and 2.7±0.6 μM, respectively. Thus, Elvitegravir can suppress various HIV strains, including diverse HIV-1 subtypes and clinical isolates carrying multiple mutations associated with resistance to currently approved antiretroviral drugs[1].

    Clinical Trial
    NCT Number Sponsor Condition Start Date Phase
    NCT00708162 Gilead Sciences HIV Infection July 2008 Phase 3
    NCT01929759 Massachusetts General Hospital|Brigham and Women's Hospital|Gilead Sciences HIV Disease January 2014
    NCT02219217 St Stephens Aids Trust|ViiV Healthcare HIV October 2014 Phase 1
    NCT02198443 Fundacion Clinic per a la Recerca Biomédica HIV June 6, 2015 Phase 4
    NCT02882230 Fondation Ophtalmologique Adolphe de Rothschild HIV September 2016
    NCT02180438 University of Washington|Clinique des Maladies Infectieuses Ibrahima DIOP Mar/CRCF, Centre Hospitalier Universitaire de Fann|Gilead Sciences HIV-2 Infection September 2014 Phase 4
    NCT02351908 St Stephens Aids Trust|Merck Sharp & Dohme Corp. HIV March 2015 Phase 4
    NCT02859558 AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) HIV-1 Infection January 2017 Phase 2
    NCT02475135 Janssen Sciences Ireland UC Healthy June 2015 Phase 1
    NCT02470650 Juan A. Arnaiz|Hospital Clinic of Barcelona Patient Compliance|Antiretroviral Therapy Intolerance June 2015 Phase 4
    NCT02203461 Technische Universität München|Gilead Sciences|MUC Research GmbH Insulin Resistance July 2014 Phase 1
    NCT02397096 Merck Sharp & Dohme Corp. HIV-1 Infection June 9, 2015 Phase 3
    NCT00042289 National Institute of Allergy and Infectious Diseases (NIAID)|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) HIV Infections March 2003 Phase 4
    NCT00537966 University of Zurich HIV Infections January 2002
    NCT00445146 Gilead Sciences HIV Infections February 2007 Phase 2
    NCT01923311 Gilead Sciences Acquired Immune Deficiency Syndrome (AIDS)|HIV Infections August 26, 2013 Phase 2|Phase 3
    NCT01721109 Gilead Sciences Acquired Immunodeficiency Syndrome|HIV Infections December 6, 2012 Phase 2|Phase 3
    NCT02383108 PENTA Foundation HIV Infection June 2016 Phase 2|Phase 3
    NCT02284035 Juan A. Arnaiz|Hospital Clinic of Barcelona AIDS January 2015 Phase 3
    NCT00298350 Gilead Sciences HIV|HIV-1|Human Immunodeficiency Virus February 2006 Phase 2
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    References
    Preparing Stock Solutions
    Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
    1 mM 2.2327 mL 11.1637 mL 22.3274 mL
    5 mM 0.4465 mL 2.2327 mL 4.4655 mL
    10 mM 0.2233 mL 1.1164 mL 2.2327 mL
    Cell Assay
    [1]

    Elvitegravir (EVG) is prepared in DMSO and stored, and then diluted with appropriate medium before use[1].

    MT-2 cells (2×105 cells) are infected with HIV-1 IIIB and then cultured in the presence of 0.5 nM or 0.1 nM Elvitegravir. Cultures are incubated at 37°C until an extensive cytopathic effect (CPE) is observed, and the culture supernatant is then harvested for further passage in fresh MT-2 cells. The concentration of Elvitegravir is increased when a significant CPE is observed. At the indicated passages, proviral DNA is extracted from infected MT-2 cells and then subjected to PCR, followed by direct population-based sequencing. Susceptibility to Elvitegravir at the indicated passages is determined using the MAGI assay or p24 production[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    447.88

    Formula

    C₂₃H₂₃ClFNO₅

    CAS No.

    697761-98-1

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 99.78%

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    Elvitegravir
    Cat. No.:
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