1. Anti-infection
    Metabolic Enzyme/Protease
  2. HCV
    HCV Protease

Asunaprevir (Synonyms: BMS-650032)

Cat. No.: HY-14434 Purity: 99.27%
Handling Instructions

Asunaprevir is a potent hepatitis C virus (HCV) NS3 protease inhibitor, with the IC50 of 0.2 nM-3.5 nM.

For research use only. We do not sell to patients.
Asunaprevir Chemical Structure

Asunaprevir Chemical Structure

CAS No. : 630420-16-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 356 In-stock
2 mg USD 108 In-stock
5 mg USD 216 In-stock
10 mg USD 360 In-stock
50 mg USD 1020 In-stock
100 mg   Get quote  
200 mg   Get quote  

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    Asunaprevir purchased from MCE. Usage Cited in: Int J Radiat Oncol Biol Phys. 2016 Nov 15;96(4):867-876.

    Simeprevir inhibits DNA damage repair following irradiation. U251, BT474, and HepG2 cells are pretreated with Simeprevir or DMSO and irradiated at a dose of 6 Gy. After 6 hours, prolongation of γH2AX foci is detected in Simeprevir-treated cells along with decreased phosphorylation of DNA-PKcs, indicating impaired nonhomologous end-joining repair.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Asunaprevir is a potent hepatitis C virus (HCV) NS3 protease inhibitor, with the IC50 of 0.2 nM-3.5 nM.

    IC50 & Target

    IC50: 0.2 nM-3.5 nM (HCV NS3 protease)

    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]. Asunaprevir, administered at single or multiple doses of 200 to 600 mg twice daily, is generally well tolerated, achieving rapid and substantial decreases in HCV RNA levels in subjects chronically infected with genotype 1 HCV[4].

    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].

    Clinical Trial
    References
    Preparing Stock Solutions
    Concentration Volume 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
    10 mM 0.1336 mL 0.6682 mL 1.3364 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay
    [2]

    Asunaprevir is diluted in assay buffer in 10% DMSO.

    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]

    Asunaprevir is diluted in vehicle (PEG-400-ethanol, 9:1).

    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
    Molecular Weight

    748.29

    Formula

    C₃₅H₄₆ClN₅O₉S

    CAS No.

    630420-16-5

    SMILES

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

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 42.9 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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    Product Name:
    Asunaprevir
    Cat. No.:
    HY-14434
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