2. Anti-infection Metabolic Enzyme/Protease
  3. HCV HCV Protease SARS-CoV
  4. Asunaprevir

Asunaprevir (BMS-650032) is a potent and orally bioavailable hepatitis C virus (HCV) NS3 protease inhibitor, with IC50 of 0.2 nM-3.5 nM. Asunaprevir inhibits SARS-CoV-2 3CLpro activity.

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

CAS No. : 630420-16-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
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Customer Review

Based on 41 publication(s) in Google Scholar

Other Forms of Asunaprevir:

Asunaprevir Related Antibodies

Top Publications Citing Use of Products

41 Publications Citing Use of MCE Asunaprevir

In Vivo Efficacy Study
Bio/Physico-chemical Assay
WB

    Asunaprevir purchased from MedChemExpress. Usage Cited in: Nature. 2020 Oct;586(7829):407-411.  [Abstract]

    Compared to vehicle controls, Asunaprevir (10 mM, 0.5 μL) infusion in the central amygdala of SOM.iPKR.TRAP animals significantly increased phosphorylation of eIF2α in SOM neurons.

    Asunaprevir purchased from MedChemExpress. Usage Cited in: Nature. 2020 Oct;586(7829):407-411.  [Abstract]

    Representative LTM motion traces for WT + Asunaprevir (10 mM, 0.5 μL), SOM.iPKR + Asunaprevir and PKCδ.iPKR + Asunaprevir animals.

    Asunaprevir purchased from MedChemExpress. Usage Cited in: Nat Neurosci. 2020 Feb;23(2):281-292.  [Abstract]

    De novo translation labeled at the N-terminus using BONCAT in Nes.iPKR amygdala slices showed a robust decrease in translation in mutant amygdala treated with 1 μM Asunaprevir (ASV) compared to vehicle (VEH)-treated mutant amygdala as well as ASV-treated wild-type amygdala.

    Asunaprevir purchased from MedChemExpress. Usage Cited in: Nat Neurosci. 2020 Feb;23(2):281-292.  [Abstract]

    In vivo SUnSET assay: Asunaprevir treated CamK2α.iPKR mice have significantly reduced translation in LA principal neurons compared to VEH treatment and Asunaprevir-treated WT mice. One-way ANOVA followed by Bonferroni's post-hoc test. n [CamK2α WT + Asunaprevir] = 36 (GFP-) neurons, n [CamK2α.iPKR +VEH] = 22 (GFP-) neurons, 78 (GFP+) neurons, and n[CamK2α.iPKR + Asunaprevir] = 31 (GFP-) neurons, 58 (GFP+) neurons from 3 mice/group.

    Asunaprevir purchased from MedChemExpress. Usage Cited in: Cell. 2019 Aug 22;178(5):1145-1158.e20.  [Abstract]

    Transcriptome analysis of Asunaprevir (3 μM, 60 h)-treated Med14SMASh vs. control cells. Red dots represent mRNA spike-ins used to normalize signals on a per cell basis.

    Asunaprevir purchased from MedChemExpress. Usage Cited in: Cell. 2019 Aug 22;178(5):1145-1158.e20.  [Abstract]

    Med26, PolII, PolII-S5, PolII-S2, H3K4me3, H3K4me1, and H3K27Ac ChIP-Seq profiles at the Xbp1 locus in Asunaprevir (3 μM, 60 h)-treated WT (left) or Med14SMASh (right) cells. The orientation of genes is denoted with red arrows.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Asunaprevir (BMS-650032) is a potent and orally bioavailable hepatitis C virus (HCV) NS3 protease inhibitor, with IC50 of 0.2 nM-3.5 nM[1]. Asunaprevir inhibits SARS-CoV-2 3CLpro activity[5].

    IC50 & Target

    IC50: 0.2 nM-3.5 nM (HCV NS3 protease)
    Cellular Effect
    Cell Line Type Value Description References
    Huh-7 EC50
    3 nM
    Compound: 2
    Antiviral activity against HCV genotype 1b Con1 expressing NS3 protease infected in human Huh7.5 cells assessed as reduction in viral RNA replication by luciferase reporter gene assay
    Antiviral activity against HCV genotype 1b Con1 expressing NS3 protease infected in human Huh7.5 cells assessed as reduction in viral RNA replication by luciferase reporter gene assay
    		[PMID: 27564532]
    In Vitro

    In multiple experiments, populations of resistant colonies are markedly reduced when cells are treated with a combination of DCV and Asunaprevir[1].
    Asunaprevir (ASV) inhibits the NS3 proteolytic activity of genotype 1a (H77 strain) and genotype 1b (J4L6S strain), with IC50s of 0.7 and 0.3 nM, respectively. The EC50s of ASV against replicons encoding the NS3 protease domains representing genotypes 1a, 1b, and 4a, range from 1.2 to 4.0 nM[2].
    Replicon cells are maintained under selective pressure with asunaprevir at concentrations of 10 and 30 times the EC50 values (50 or 150 nM final concentrations, respectively). For genotype 1b resistance selection, replicon cells are maintained in the presence of asunaprevir at 10 or 30 times the EC50 values (30 or 90 nM final concentrations, respectively)[3].

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

    Asunaprevir Related Antibodies
    In Vivo

    Asunaprevir (ASV, 3-15 mg/kg, p.o.) displays a hepatotropic disposition (liver-to-plasma ratios ranging from 40- to 359-fold across species) in several animal species. Twenty-four hours postdose, liver exposures across all species tested are ≥110-fold above the inhibitor EC50 observed with HCV genotype-1 replicons[2].

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

    748.29

    Formula

    C35H46ClN5O9S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    ClC1=CC=C2C(C(O[C@H]3CN(C([C@@H](NC(OC(C)(C)C)=O)C(C)(C)C)=O)[C@H](C(N[C@@]4(C(NS(C5CC5)(=O)=O)=O)[C@H](C=C)C4)=O)C3)=NC=C2OC)=C1
    Shipping

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

    DMSO : ≥ 100 mg/mL (133.64 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : 20 mg/mL (26.73 mM; Need ultrasonic)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.3364 mL 6.6819 mL 13.3638 mL
    5 mM 0.2673 mL 1.3364 mL 2.6728 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (3.34 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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (3.34 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 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.
    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: 99.84%

    SDS (419 KB)

    COA (260 KB) RP-HPLC (252 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [2]

    Cytotoxicity is determined by incubating cells (3,000 to 10,000 cells/well) with serially diluted test compounds or DMSO for 5 days (MT-2 cells) or 4 days (all other cell types). Cell viability is quantitated using an MTS assay for MT-2 or a Cell-Titer Blue reagent assay for HEK-293, HuH-7, HepG2, and MRC5 cells, and 50% cytotoxic concentrations (CC50s) are calculated. For the HCV and BVDV replicon assays, CC50s are determined from the same wells that are later used to determine EC50s.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Mice (n=9 per group; overnight fast) receive Asunaprevir (ASV) by oral gavage (5 mg/kg; vehicle of PEG-400-ethanol, 9:1). Blood samples (-0.2 mL) are obtained by retro-orbital bleeding at 0.25, 0.5, 1, 3, 6, 8, and 24 h after dosing. Within each group, three animals are bled at 0.25, 3, and 24 h, three at 0.5 and 6 h, and three at 1 and 8 h, resulting in a composite pharmacokinetic profile. Livers and brains are also removed from mice at the terminal sampling points. Rats (n=3 per group; overnight fast) receive ASV (amorphous free acid) by oral gavage (3, 5, 10, and 15 mg/kg) in PEG-400-ethanol (9:1). Serial blood samples (-0.3 mL) are obtained from the jugular vein predosing (0 h) and at 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 24, and 48 h postdosing. To assess tissue exposure, rats are orally administered ASV (5 or 15 mg/kg, same vehicle as above), and blood, liver, and heart samples from two rats/group are obtained at 0.17, 0.5, 1, 2, 4, 6, 8, 24, 48, and 72 h after dosing.

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    Ethanol / DMSO 1 mM 1.3364 mL 6.6819 mL 13.3638 mL 33.4095 mL
    5 mM 0.2673 mL 1.3364 mL 2.6728 mL 6.6819 mL
    10 mM 0.1336 mL 0.6682 mL 1.3364 mL 3.3410 mL
    15 mM 0.0891 mL 0.4455 mL 0.8909 mL 2.2273 mL
    20 mM 0.0668 mL 0.3341 mL 0.6682 mL 1.6705 mL
    25 mM 0.0535 mL 0.2673 mL 0.5346 mL 1.3364 mL
    DMSO 30 mM 0.0445 mL 0.2227 mL 0.4455 mL 1.1137 mL
    40 mM 0.0334 mL 0.1670 mL 0.3341 mL 0.8352 mL
    50 mM 0.0267 mL 0.1336 mL 0.2673 mL 0.6682 mL
    60 mM 0.0223 mL 0.1114 mL 0.2227 mL 0.5568 mL
    80 mM 0.0167 mL 0.0835 mL 0.1670 mL 0.4176 mL
    100 mM 0.0134 mL 0.0668 mL 0.1336 mL 0.3341 mL
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    Asunaprevir 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:

    Asunaprevir630420-16-5BMS-650032BMS650032BMS 650032HCVHCV ProteaseSARS-CoVHepatitis C virusSARS coronavirusInhibitorinhibitorinhibit

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