2. Anti-infection Metabolic Enzyme/Protease
  3. HCV HCV Protease SARS-CoV
  4. Grazoprevir potassium salt

Grazoprevir potassium salt  (Synonyms: MK-5172 potassium salt)

Cat. No.: HY-15298A Purity: 99.79%
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Grazoprevir potassium salt (MK-5172 potassium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively. Grazoprevir potassium salt inhibits SARS-CoV-2 3CLpro activity.

For research use only. We do not sell to patients.

CAS No. : 1206524-86-8

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10 mM * 1 mL in DMSO
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Customer Review

Based on 29 publication(s) in Google Scholar

Other Forms of Grazoprevir potassium salt:

Grazoprevir potassium salt Related Antibodies

Top Publications Citing Use of Products

29 Publications Citing Use of MCE Grazoprevir potassium salt

ELISA
Cell Proliferation/Viability Assay
In Vivo Imaging
In Vivo Efficacy Study

    Grazoprevir potassium salt purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2022 Nov 14;40(11):1294-1305.e4.  [Abstract]

    Primary T cell lines were treated with or without Grazoprevir (all in the presence of target cells), and cytokine levels quantified.

    Grazoprevir potassium salt purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2022 Nov 14;40(11):1294-1305.e4.  [Abstract]

    Cytotoxicity response of OFF VIPER CAR T cells to Grazoprevir being added, washed out, and re-introduced after two days.

    Grazoprevir potassium salt purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2022 Nov 14;40(11):1294-1305.e4.  [Abstract]

    Grazoprevir dose-response profile of various cells, as measured in cytokine levels and cell killing.

    Grazoprevir potassium salt purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2022 Nov 14;40(11):1294-1305.e4.  [Abstract]

    IVIS imaging of groups treated with (1) no T cells, (2) non-transduced T cell (NT-WT), (3) ON VIPER CAR T cells, (4) ON VIPER CAR T cells with Grazoprevir (5) OFF VIPER CAR T cells, (6) OFF VIPER CAR T cells with Grazoprevir, or (7) Traditional CAR T cells by day 21.

    Grazoprevir potassium salt purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2022 Nov 14;40(11):1294-1305.e4.  [Abstract]

    Illustration of the dual-tumor model generated by systemically growing Nalm6 cells via i.v. and regional growth of MSTO-211H cells via s.c (left). Timeline for the in vivo experiment (right). Inducers (Grazoprevir or POM) were injected daily through i.p.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Grazoprevir potassium salt (MK-5172 potassium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively[1][2]. Grazoprevir potassium salt inhibits SARS-CoV-2 3CLpro activity[3].

    IC50 & Target

    Ki: 0.01±<0.01 nM (gt1b), 0.01±0.01 nM (gt1a), 0.08±0.02 nM (gt2a), 0.15±0.06 nM (gt2b), 0.90±0.2 nM (gt3a)[1]
    In Vitro

    In biochemical assays, Grazoprevir (MK-5172) is effective against a panel of major genotypes and variants engineered with common resistant mutations, with Ki of 0.01±<0.01 nM (gt1b), 0.01±0.01 nM (gt1a), 0.08±0.02 nM (gt2a), 0.15±0.06 nM (gt2b), 0.90±0.2 nM (gt3a), 0.07±0.01 nM (gt1bR155K), 0.14±0.03 nM (gt1bD168V), 0.30±0.04 nM (gt1bD168Y), 5.3±0.9 nM (gt1bA156T), and 12±2 nM (gt1bA156V), respectively. In the replicon assay, Grazoprevir demonstrates subnanomolar to low-nanomolar EC50s against genotypes 1a, 1b, and 2a, with EC50s of 0.5±0.1 nM, 2±1 nM, and 2±1 nM for gt1bcon1, gt1a, and gt2a, respectively. Grazoprevir is potent against a panel of HCV replication mutants NS5A (Y93H) (EC50=0.7±0.3 nM), NS5B nucleosides (S282T) (EC50=0.3±0.1 nM), and NS5B (C316Y) (EC50=0.4±0.2)[1]. Grazoprevir (MK-5172) maintains the excellent potency against the gt 3a enzyme as well as a broad panel of mutant enzymes, has excellent potency in the replicon system [gt1b IC50(50% NHS)=7.4 nM; gt1a IC50(40% NHS)=7 nM], and shows excellent rat liver exposure[2].

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

    Grazoprevir potassium salt Related Antibodies
    In Vivo

    Grazoprevir (MK-5172) demonstrates efficacy in vivo against chronic-HCV-infected chimpanzees[1]. When dosed to dogs, Grazoprevir (MK-5172) shows low clearance of 5 mL/min/kg and a 3 h half-life after iv dosing and has good plasma exposure (AUC=0.4 μM h) after a 1 mg/kg oral dose. Dog liver biopsy studies showed that the liver concentration of Grazoprevir after the 1 mg/kg oral dose is 1.4 μM at the 24 h time point. Similar to its behavior in rats, Grazoprevir demonstrates effective partitioning into liver tissue and maintains high liver concentration, relative to potency, 24 h after oral dosing in dogs[2].

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

    804.99

    Formula

    C38H49KN6O9S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    COC1=CC2=C(N=C(CCCCC[C@@H]3C[C@H]3OC4=O)C(O[C@H]5CN(C([C@H](C(C)(C)C)N4)=O)[C@H](C(N[C@@]([C@@H]6C=C)(C6)C([N-]S(C7CC7)(=O)=O)=O)=O)C5)=N2)C=C1.[K+]
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (124.23 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.2423 mL 6.2113 mL 12.4225 mL
    5 mM 0.2485 mL 1.2423 mL 2.4845 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (3.11 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (3.11 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    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: 99.79%

    SDS (252 KB)

    COA (261 KB) HNMR (150 KB) RP-HPLC (235 KB) LCMS (235 KB)

    Handling Instructions (2659 KB)
    References
    Animal Administration
    [1]

    Rats and Dogs[1]
    Studies are performed in both rats and dogs. For studies in which Grazoprevir is dosed intravenously to rats or dogs, the compound is formulated in polyethylene glycol 200 (PEG200) and administered as a bolus at either 2 mg/kg of body weight (Rats) or 0.5 mg/kg (dog). For oral studies, the crystalline potassium salt of the compound is dosed as a solution in PEG400 at 5 mg/kg (Rats) or 1 mg/kg (dog). For all studies, blood samples are collected in EDTA-containing tubes at appropriate times and plasma is separated by centrifugation and stored at −70°C until analysis. Quantitation of Grazoprevir levels is conducted by high-performance liquid chromatography/mass spectroscopy (LC/MS/MS) following protein precipitation. Liver samples are obtained from rat studies at the termination of the experiment. For dog, liver biopsy samples (20 μL) are collected following sedation. Tissue samples are homogenized in four volumes of deionized water, and drug concentrations are determined by LC/MS/MS after protein precipitation.

    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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.2423 mL 6.2113 mL 12.4225 mL 31.0563 mL
    5 mM 0.2485 mL 1.2423 mL 2.4845 mL 6.2113 mL
    10 mM 0.1242 mL 0.6211 mL 1.2423 mL 3.1056 mL
    15 mM 0.0828 mL 0.4141 mL 0.8282 mL 2.0704 mL
    20 mM 0.0621 mL 0.3106 mL 0.6211 mL 1.5528 mL
    25 mM 0.0497 mL 0.2485 mL 0.4969 mL 1.2423 mL
    30 mM 0.0414 mL 0.2070 mL 0.4141 mL 1.0352 mL
    40 mM 0.0311 mL 0.1553 mL 0.3106 mL 0.7764 mL
    50 mM 0.0248 mL 0.1242 mL 0.2485 mL 0.6211 mL
    60 mM 0.0207 mL 0.1035 mL 0.2070 mL 0.5176 mL
    80 mM 0.0155 mL 0.0776 mL 0.1553 mL 0.3882 mL
    100 mM 0.0124 mL 0.0621 mL 0.1242 mL 0.3106 mL
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    Grazoprevir potassium salt 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:

    Grazoprevir1206524-86-8MK-5172MK5172MK 5172HCVHCV ProteaseSARS-CoVHepatitis C virusSARS coronavirusInhibitorinhibitorinhibit

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