Asunaprevir

Catalog No.S4935 Batch:S493501

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Technical Data

Formula

C35H46ClN5O9S
Molecular Weight 748.29 CAS No. 630420-16-5
Solubility (25°C)* In vitro DMSO 100 mg/mL (133.63 mM)
Ethanol 100 mg/mL (133.63 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Asunaprevir is an orally bioavailable inhibitor of the hepatitis C virus enzyme serine protease NS3 that is necessary for protein processing required for viral replication.
Targets
1b (J4L6S) [1] 1a (H77) [1] 6a (HK-6A) [1] 4a (ED43) [1] 5a (SA13) [1] View More
0.3 nM 0.7 nM 0.9 nM 1.6 nM 1.7 nM
In vitro Asunaprevir (ASV) competitively binds to the NS3/4A protease complex, with Ki values of 0.4 and 0.24 nM against recombinant enzymes representing genotypes 1a (H77) and 1b (J4L6S), respectively. Asunaprevir is high selective without any significant activity against the closely related GB virus-B NS3 protease and a panel of human serine or cysteine proteases. In cell culture, ASV inhibits replication of HCV replicons representing genotypes 1 and 4, with 50% effective concentrations (EC50s) ranging from 1 to 4 nM, and has weaker activity against genotypes 2 and 3 (EC50, 67-1162 nM). Selectivity is again demonstrated by the absence of activity (EC50, >12 μM) against a panel of other RNA viruses[1].
In vivo Plasma and tissue exposures in vivo in several animal species indicate that ASV displays a hepatotropic disposition (liver-to-plasma ratios ranging from 40- to 359-fold across species). Twenty-four hours postdose, liver exposures across all species tested are ≥110-fold above the inhibitor EC50s observed with HCV genotype-1 replicons[1].

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    Huh 7.5.1 cells

  • Concentrations

    1 or 10 nM

  • Incubation Time

    3, 6, 24, and 48 h

  • Method

    --
Animal Study:

[1]
  • Animal Models

    male FVB mice, Sprague-Dawley rats, male beagles, male cynomolgus monkeys

  • Dosages

    5 mg/kg (mice); 3, 5, 10, and 15 mg/kg (rats); 3 or 6 mg/kg (Dogs); 3 mg/kg (Monkeys)

  • Administration

    by oral gavage

Selleck's Asunaprevir has been cited by 7 publications

METTL3-Dependent N6-Methyladenosine Modification Programs Human Neural Progenitor Cell Proliferation [ Int J Mol Sci, 2023, 10.3390/ijms242115535] PubMed: 37958523
Genetic instability from a single S phase after whole-genome duplication [ Nature, 2022, 604(7904):146-151] PubMed: 35355016
Going Viral: An Investigation into the Chameleonic Behaviour of Antiviral Compounds [ Chemistry, 2022, e202202798.] PubMed: 36286339
Hepatitis C virus drugs that inhibit SARS-CoV-2 papain-like protease synergize with remdesivir to suppress viral replication in cell culture [ Cell Rep, 2021, 35(7):109133] PubMed: 33984267
Development of a Cell-Based Luciferase Complementation Assay for Identification of SARS-CoV-2 3CLpro Inhibitors [ Viruses, 2021, 13(2)173] PubMed: 33498923
Mechanisms of genetic instability in a single S-phase following whole genome doubling [ bioRxiv, 2021, 10.1101/2021.07.16.452672] PubMed: None
Hepatitis C Virus Drugs Simeprevir And Grazoprevir Synergize with Remdesivir to Suppress SARS-CoV2 Replication [ BioRxiv, 2020, 10.1101/2020.12.13.422511] PubMed: none

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.