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

Boceprevir (Synonyms: EBP 520; SCH 503034)

Cat. No.: HY-10237 Purity: 98.83%
Handling Instructions

Boceprevir is a novel, potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with Ki of 14 nM in both enzyme assay and EC90 of 350 nM in cell-based replicon assay.

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

Boceprevir Chemical Structure

Boceprevir Chemical Structure

CAS No. : 394730-60-0

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 82 In-stock
Estimated Time of Arrival: December 31
5 mg USD 72 In-stock
Estimated Time of Arrival: December 31
10 mg USD 108 In-stock
Estimated Time of Arrival: December 31
50 mg USD 228 In-stock
Estimated Time of Arrival: December 31
100 mg USD 348 In-stock
Estimated Time of Arrival: December 31
200 mg USD 540 In-stock
Estimated Time of Arrival: December 31
500 mg   Get quote  
1 g   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 22 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Boceprevir purchased from MCE. Usage Cited in: Virology. 2014 May;456-457:300-9.

    Jurkat cells are transfected with plasmids expressing (A) HCV NS3/4A or (B) HPgV NS3/4AB-HA. Telaprevir, Boceprevir, and Danoprevir are added at concentrations of 100 µM, 16.6 µM, 2.7 µM, or 0 µM in 0.1% DMSO. Lysates are harvested after 24 h and resolved by immunoblots probed with anti-HCV NS3 (A) or anti-HA (B). The position of HCV NS3/4A (~75kDa), HCV NS3 (~73kDa), NS3/4AB-HA, and NS4B-HA (~30kDa) are indicated. Molecular markers are on the right.

    Boceprevir purchased from MCE. Usage Cited in: Antimicrob Agents Chemother. 2015 Dec;59(12):7666-7670.

    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.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Boceprevir is a novel, potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with Ki of 14 nM in both enzyme assay and EC90 of 350 nM in cell-based replicon assay.

    IC50 & Target

    Ki: 14 nM (HCV NS3 protease)[1]

    In Vitro

    In the HCV NS3 protease continuous assay, Boceprevir (SCH 503034) has a potency of 14 nM (Ki) average over a large number of runs. In the 72-h bicistronic subgenomic cell-based replicon assay in HuH-7 cells, the EC50 and EC90 values are determined to be 0.20 µM and 0.35 µM, respectively. Boceprevir is also found to be a very weak inhibitor of HNE (Ki=26 µM) representing a selectivity of 2200[1].

    In Vivo

    Boceprevir, an HCV Protease Inhibitor for the Treatment of Hepatitis C Virus Infection. The pharmacokinetic profile of Boceprevir is evaluated in several animal species. Following oral administration, Boceprevir is moderately absorbed in rats (10 mg/kg), dogs (3 mg/kg), and monkeys (3 mg/kg). Absorption is relatively rapid in dogs but slower in mice (10 mg/kg), rats, and monkeys, as evidenced by mean absorption times (MAT) ranging from 0.5 to 1.4 h. The AUC is good in dogs and rats, moderate in mouse, and low in monkeys. The absolute oral bioavailability is modest in mouse, rats, and dogs (26-34%) but low in monkeys (4%)[1]. Boceprevir (100 mg/kg, orally) inhibit HCV NS3/4A protease activity in triple-transgenic mice[2].

    Clinical Trial
    Molecular Weight

    519.68

    Formula

    C₂₇H₄₅N₅O₅

    CAS No.

    394730-60-0

    SMILES

    O=C(N1[[email protected]@H]([[email protected]@]2([H])C(C)([[email protected]]2(C1)[H])C)C(NC(C(C(N)=O)=O)CC3CCC3)=O)[[email protected]@H](NC(NC(C)(C)C)=O)C(C)(C)C

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 10 mg/mL (19.24 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9243 mL 9.6213 mL 19.2426 mL
    5 mM 0.3849 mL 1.9243 mL 3.8485 mL
    10 mM 0.1924 mL 0.9621 mL 1.9243 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 1.67 mg/mL (3.21 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 1.67 mg/mL (3.21 mM); Suspended solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 1.67 mg/mL (3.21 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Animal Administration
    [2]

    Mice[2]
    Boceprevir is purchased from MedChem Express. To evaluate the effect of Boceprevir, triple-transgenic mice are induced with Doxycycline (Dox) for 10 days (n=5 per group). On the third day after Dox induction, when plasma Gluc activity reaches its peak, the mice are administered either Boceprevir (100 mg/kg) or DMSO via oral gavage twice daily for 7 days. During this period, blood is collected from the caudal vein daily to detect plasma Gluc activity.

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

    References

    Purity: 98.83%

    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    BoceprevirEBP 520SCH 503034EBP520EBP-520SCH503034SCH-503034HCV ProteaseHCVHepatitis C virusInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product name

     

    Salutation

    Applicant name *

     

    Email address *

    Phone number *

     

    Organization name *

    Country or Region *

     

    Requested quantity *

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product name:
    Boceprevir
    Cat. No.:
    HY-10237
    Quantity:
    MCE Japan Authorized Agent: