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

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

Cat. No.: HY-14740 Purity: 99.90%
SDS COA 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
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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Customer Review

Based on 12 publication(s) in Google Scholar

Other Forms of Elvitegravir:

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.

    View All HIV Isoform Specific Products:

    • 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

     

    Cellular Effect
    Cell Line Type Value Description References
    C8166 EC50
    0.00021 μM
    Compound: 1
    Antiviral activity against wild type HIV1 LAI-3B infected in human C8166 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    Antiviral activity against wild type HIV1 LAI-3B infected in human C8166 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    [PMID: 21862337]
    C8166 EC50
    0.00021 μM
    Compound: Elvitegravir
    Antiviral activity against HIV1 LAI 3B infected in human C8166 cells assessed as protection against virus-induced cytopathic effect by MTT assay
    Antiviral activity against HIV1 LAI 3B infected in human C8166 cells assessed as protection against virus-induced cytopathic effect by MTT assay
    [PMID: 21763149]
    C8166 EC50
    0.001 μM
    Compound: 1
    Antiviral activity against HIV1 A17 harboring reverse transcriptase Y181C mutant infected in human C8166 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    Antiviral activity against HIV1 A17 harboring reverse transcriptase Y181C mutant infected in human C8166 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    [PMID: 21862337]
    C8166 CC50
    17.2 μM
    Compound: 1
    Cytotoxicity against human C8166 cells by MTT assay
    Cytotoxicity against human C8166 cells by MTT assay
    [PMID: 21862337]
    C8166 CC50
    17.2 μM
    Compound: Elvitegravir
    Cytotoxicity against human C8166 cells by MTT assay
    Cytotoxicity against human C8166 cells by MTT assay
    [PMID: 21763149]
    HEK-293T CC50
    > 250 μM
    Compound: Elvitegravir
    Cytotoxicity against human HEK293T cells assessed as cell growth inhibition by MTT assay
    Cytotoxicity against human HEK293T cells assessed as cell growth inhibition by MTT assay
    [PMID: 36898139]
    HeLa CC50
    > 50 μM
    Compound: EVG
    Cytotoxicity against human HeLa-CD4-LTR-beta-gal cells after 24 hrs by ATPlite reagent based luminescence analysis
    Cytotoxicity against human HeLa-CD4-LTR-beta-gal cells after 24 hrs by ATPlite reagent based luminescence analysis
    [PMID: 25961960]
    HeLa CC50
    > 50 μM
    Compound: 1, EVG
    Cytotoxicity against human HeLa cells expressing CD4-LTR-beta-gal after 24 hrs by ATPlite assay
    Cytotoxicity against human HeLa cells expressing CD4-LTR-beta-gal after 24 hrs by ATPlite assay
    [PMID: 24684270]
    HeLa EC50
    0.0142 μM
    Compound: 1, EVG
    Antiviral activity against HIV1 3B infected in human HeLa cells expressing CD4-LTR-beta-gal assessed as inhibition of viral replication after 3 days by reporter gene assay
    Antiviral activity against HIV1 3B infected in human HeLa cells expressing CD4-LTR-beta-gal assessed as inhibition of viral replication after 3 days by reporter gene assay
    [PMID: 24684270]
    MT4 EC50
    0.00037 μM
    Compound: 2, elvitegravir, GS-9137
    Antiviral activity against HIV1 3B in MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    Antiviral activity against HIV1 3B in MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    [PMID: 18665580]
    MT4 EC50
    0.0006 μM
    Compound: GS-9137
    Antiviral activity against HIV 1 NL4.3 harboring integrase L74M mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    Antiviral activity against HIV 1 NL4.3 harboring integrase L74M mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    [PMID: 18378713]
    MT4 EC50
    0.0007 μM
    Compound: GS-9137
    Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    [PMID: 18378713]
    MT4 EC50
    0.0008 μM
    Compound: 1, GS-9137
    Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    [PMID: 21227550]
    MT4 EC50
    0.0009 μM
    Compound: GS-9137
    Antiviral activity against HIV 1 NL4.3 integrase S230N mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    Antiviral activity against HIV 1 NL4.3 integrase S230N mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    [PMID: 18378713]
    MT4 EC50
    0.001 μM
    Compound: GS-9137
    Antiviral activity against HIV 1 3B infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    Antiviral activity against HIV 1 3B infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    [PMID: 18378713]
    MT4 EC50
    0.0022 μM
    Compound: 3, EVG
    Antiviral activity against HIV1 harboring K103N/Y181C double mutant infected in human MT4 cells assessed as protection of cells from virus-induced cytopathic after 5 days by MTT assay
    Antiviral activity against HIV1 harboring K103N/Y181C double mutant infected in human MT4 cells assessed as protection of cells from virus-induced cytopathic after 5 days by MTT assay
    [PMID: 25907370]
    MT4 EC50
    0.0031 μM
    Compound: 3, EVG
    Antiviral activity against wild-type HIV1 3B infected in human MT4 cells assessed as protection of cells from virus-induced cytopathic after 5 days by MTT assay
    Antiviral activity against wild-type HIV1 3B infected in human MT4 cells assessed as protection of cells from virus-induced cytopathic after 5 days by MTT assay
    [PMID: 25907370]
    MT4 EC50
    0.012 μM
    Compound: GS-9137
    Antiviral activity against HIV 1 NL4.3 integrase E92Q mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    Antiviral activity against HIV 1 NL4.3 integrase E92Q mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    [PMID: 18378713]
    MT4 EC50
    0.015 μM
    Compound: GS-9137
    Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 20 passages selected in presence of compound
    Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 20 passages selected in presence of compound
    [PMID: 18378713]
    MT4 EC50
    0.018 μM
    Compound: GS-9137
    Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 40 passages selected in presence of compound
    Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 40 passages selected in presence of compound
    [PMID: 18378713]
    MT4 EC50
    0.033 μM
    Compound: GS-9137
    Antiviral activity against HIV 1 3B harboring integrase E92Q S230N double mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 20 passages in presence of compound
    Antiviral activity against HIV 1 3B harboring integrase E92Q S230N double mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 20 passages in presence of compound
    [PMID: 18378713]
    MT4 EC50
    0.05 μM
    Compound: GS-9137
    Antiviral activity against HIV 1 3B harboring integrase L34M mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 40 passages in presence of compound
    Antiviral activity against HIV 1 3B harboring integrase L34M mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 40 passages in presence of compound
    [PMID: 18378713]
    MT4 EC50
    0.059 μM
    Compound: GS-9137
    Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 60 passages selected in presence of compound
    Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 60 passages selected in presence of compound
    [PMID: 18378713]
    MT4 EC50
    0.077 μM
    Compound: GS-9137
    Antiviral activity against HIV 1 3B harboring integrase E92Q, S230N and L34M triple mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 60 passages in presence of compound
    Antiviral activity against HIV 1 3B harboring integrase E92Q, S230N and L34M triple mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 60 passages in presence of compound
    [PMID: 18378713]
    MT4 EC50
    0.9 μM
    Compound: 49
    Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay
    Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay
    [PMID: 19719237]
    MT4 CC50
    1.15 μM
    Compound: 2, elvitegravir, GS-9137
    Cytotoxicity against human MT4 cells by MTT assay
    Cytotoxicity against human MT4 cells by MTT assay
    [PMID: 18665580]
    MT4 IC50
    1.3 nM
    Compound: EVG
    Inhibition of wild type HIV1 3B infected in human MT4 cells using cells pre-incubated with compound for 1 hr measured 4 days post viral infection by MTT assay
    Inhibition of wild type HIV1 3B infected in human MT4 cells using cells pre-incubated with compound for 1 hr measured 4 days post viral infection by MTT assay
    [PMID: 22963135]
    MT4 CC50
    2.12 μM
    Compound: 1, GS-9137
    Cytotoxicity against human MT4 cells by MTT assay
    Cytotoxicity against human MT4 cells by MTT assay
    [PMID: 21227550]
    MT4 EC50
    2.12 μM
    Compound: 2, GS-9137
    Cytotoxicity against human MT4 cells by MTT assay
    Cytotoxicity against human MT4 cells by MTT assay
    [PMID: 20630765]
    MT4 CC50
    2.12 μM
    Compound: GS-9137
    Cytotoxicity against human MT4 cells by MTT assay
    Cytotoxicity against human MT4 cells by MTT assay
    [PMID: 18541726]
    MT4 IC50
    29 nM
    Compound: EVG
    Inhibition of wild type HIV1 3B infected in human MT4 cells using cells pre-incubated with compound for 1 hr measured 4 days post viral infection in presence of 20 mg/ml HSA by MTT assay
    Inhibition of wild type HIV1 3B infected in human MT4 cells using cells pre-incubated with compound for 1 hr measured 4 days post viral infection in presence of 20 mg/ml HSA by MTT assay
    [PMID: 22963135]
    MT4 CC50
    4 μM
    Compound: 49
    Cytotoxicity against human MT4 cells after 5 days by MTT assay
    Cytotoxicity against human MT4 cells after 5 days by MTT assay
    [PMID: 19719237]
    MT4 CC50
    4.6 μM
    Compound: 3, EVG
    Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay
    Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay
    [PMID: 25907370]
    MT4 CC50
    6.3 μM
    Compound: EVG
    Cytotoxic activity against mock-infected human MT4 cellls assessed as reduction in cell viability by MTT assay
    Cytotoxic activity against mock-infected human MT4 cellls assessed as reduction in cell viability by MTT assay
    [PMID: 28951095]
    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.

    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
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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

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    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%

    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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      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.

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