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

Asunaprevir  (Synonyms: BMS-650032)

Cat. No.: HY-14434 Purity: 99.71%
COA Handling Instructions

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.

Asunaprevir Chemical Structure

Asunaprevir Chemical Structure

CAS No. : 630420-16-5

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 356 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 356 In-stock
Estimated Time of Arrival: December 31
Solid
2 mg USD 108 In-stock
Estimated Time of Arrival: December 31
5 mg USD 216 In-stock
Estimated Time of Arrival: December 31
10 mg USD 360 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1020 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 32 publication(s) in Google Scholar

Top Publications Citing Use of Products

32 Publications Citing Use of MCE Asunaprevir

  • 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)
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].

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

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

748.29

Appearance

Solid

Formula

C35H46ClN5O9S
CAS No.
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
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 : ≥ 100 mg/mL (133.64 mM)

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
10 mM 0.1336 mL 0.6682 mL 1.3364 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: ≥ 2.5 mg/mL (3.34 mM); Clear solution

  • 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

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (3.34 mM); Clear solution

  • 4.

    Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: 2.5 mg/mL (3.34 mM); Suspended solution; Need ultrasonic

  • 5.

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

    Solubility: 2 mg/mL (2.67 mM); Clear solution; Need ultrasonic

  • 6.

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

    Solubility: ≥ 2 mg/mL (2.67 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.71%

COA (260 KB) RP-HPLC (244 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
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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.

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Keywords:

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

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