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

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

Cat. No.: HY-14740 Purity: 99.90%
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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
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 109 In-stock
Solution
10 mM * 1 mL in DMSO USD 109 In-stock
Solid
5 mg USD 63 In-stock
10 mg USD 99 In-stock
50 mg USD 383 In-stock
100 mg USD 686 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 12 publication(s) in Google Scholar

Other Forms of Elvitegravir:

Elvitegravir Related Antibodies

Top Publications Citing Use of Products

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

    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 MedChemExpress. Usage Cited in: Antimicrob Agents Chemother. 2015 Dec;59(12):7666-7670.  [Abstract]

    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.

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    HIV HIV-1 HIV-2

    • 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

    HIV-1

     

    HIV-2

     

    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].

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

    Elvitegravir Related Antibodies
    Clinical Trial
    Molecular Weight

    447.88

    Formula

    C23H23ClFNO5
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(O)C1=CN(C2=C(C1=O)C=C(C(OC)=C2)CC3=CC=CC(Cl)=C3F)[C@@H](C(C)C)CO
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 233.33 mg/mL (520.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 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

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    • Protocol 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

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.90%

    COA (253 KB) HNMR (254 KB) LCMS (92 KB) OR (170 KB)

    Handling Instructions (2659 KB)
    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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2327 mL 11.1637 mL 22.3274 mL 55.8185 mL
    5 mM 0.4465 mL 2.2327 mL 4.4655 mL 11.1637 mL
    10 mM 0.2233 mL 1.1164 mL 2.2327 mL 5.5819 mL
    15 mM 0.1488 mL 0.7442 mL 1.4885 mL 3.7212 mL
    20 mM 0.1116 mL 0.5582 mL 1.1164 mL 2.7909 mL
    25 mM 0.0893 mL 0.4465 mL 0.8931 mL 2.2327 mL
    30 mM 0.0744 mL 0.3721 mL 0.7442 mL 1.8606 mL
    40 mM 0.0558 mL 0.2791 mL 0.5582 mL 1.3955 mL
    50 mM 0.0447 mL 0.2233 mL 0.4465 mL 1.1164 mL
    60 mM 0.0372 mL 0.1861 mL 0.3721 mL 0.9303 mL
    80 mM 0.0279 mL 0.1395 mL 0.2791 mL 0.6977 mL
    100 mM 0.0223 mL 0.1116 mL 0.2233 mL 0.5582 mL
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    Elvitegravir Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Elvitegravir697761-98-1GS-9137 JTK-303 D06677GS9137GS 9137JTK303JTK 303JTK-303D06677D 06677D-06677HIV IntegraseHIVHuman immunodeficiency virusHIV-1IIIBHIV-2EHOHIV-2RODcDNAInhibitorinhibitorinhibit

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