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

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

Cat. No.: HY-14740 Purity: 99.85%
Handling Instructions

Elvitegravir (GS-9137; JTK-303; D06677) 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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 99 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 99 In-stock
Estimated Time of Arrival: December 31
Solid
10 mg USD 90 In-stock
Estimated Time of Arrival: December 31
50 mg USD 348 In-stock
Estimated Time of Arrival: December 31
100 mg USD 624 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 10 publication(s) in Google Scholar

Top Publications Citing Use of Products

    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.

    Elvitegravir purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2016;38(3):1111-20.

    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).
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Elvitegravir (GS-9137; JTK-303; D06677) 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 (GS-9137; JTK-303; D06677) 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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    Molecular Weight

    447.88

    Formula

    C₂₃H₂₃ClFNO₅

    CAS No.
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 250 mg/mL (558.19 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent 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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.5 mg/mL (5.58 mM); Suspended solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.08 mg/mL (4.64 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (4.64 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [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

    Purity: 99.85%

    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

     

    Salutation

    Applicant Name *

     

    Email address *

    Phone number *

     

    Organization name *

    Department *

     

    Requested quantity *

    Country or Region *

         

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Elvitegravir
    Cat. No.:
    HY-14740
    Quantity:
    MCE Japan Authorized Agent: