1. Anti-infection
  2. HCV
  3. Daclatasvir

Daclatasvir (Synonyms: BMS-790052; EBP 883)

Cat. No.: HY-10466 Purity: 99.24%
Handling Instructions

Daclatasvir is a potent HCV NS5A protein inhibitor, with mean EC50 values of 50 and 9 pM against genotype 1a and 1b replicons, respectively.

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

Daclatasvir Chemical Structure

Daclatasvir Chemical Structure

CAS No. : 1009119-64-5

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Customer Review

Based on 39 publication(s) in Google Scholar

Other Forms of Daclatasvir:

Top Publications Citing Use of Products

Publications Citing Use of MCE Daclatasvir

    Daclatasvir purchased from MCE. Usage Cited in: Open Virol J. 2014 Mar 7;8:1-8.

    The PKR activation block is not unique to CypI, DAAs also prevent the IFN-induced PKR activation in HCV-infected cells. JFH-1-infected Huh7.5.1 cells are treated with or without CypI (cyclosporine A and alisporivir), DAAs (the HCV NS5A inhibitor daclatasvir and the HCV protease inhibitor telaprevir) and an HIV-1 inhibitor (reverse transcriptase inhibitor emtricitabine). Results are representative of 4 independent experiments.

    Daclatasvir purchased from MCE. Usage Cited in: Eur J Med Chem. 2018 Jan 1;143:1053-1065.

    GS4.3 cells are treated with 7f (20 μM), or Telaprevir (0.5μM), Sofosbuvir (0.8 μM), Daclatasvir (0.15 μM) or solvent control for 6 days.

    Daclatasvir purchased from MCE. Usage Cited in: Eur J Med Chem. 2018 Jan 1;143:1053-1065.

    Huh7.5 cells are infected with HCV and simultaneously treated with 7f (10 μM) or DAA (0.04 μM Simeprevir, 0.08 μM Sofosbuvir, or 16 pM Daclatasvir) or 7f plus DAA.

    Daclatasvir purchased from MCE. Usage Cited in: PLoS Pathog. 2018 Sep 18;14(9):e1007284.

    Polyprotein expression efficiency is determined by Western-Blot using an antibody against NS3 and beta actin as loading control.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Daclatasvir is a potent HCV NS5A protein inhibitor, with mean EC50 values of 50 and 9 pM against genotype 1a and 1b replicons, respectively.

    IC50 & Target

    EC50: 9±4 pM (HCV replicon genotype 1b, in Con1 cells), 50 ± 13 pM (HCV replicon genotype 1a, in H77 cells)[1]

    In Vitro

    Daclatasvir (BMS-790052) is a small molecule inhibitor of the HCV NS5A protein that exhibits picomolar half-maximum effective concentrations (EC50) towards replicons expressing a broad range of HCV genotypes and the JFH-1 genotype 2a infectious virus in cell culture. Daclatasvir is a potent inhibitor of the JFH-1 genotype 2a infectious virus that replicates in cell culture (EC50=28 pM), an assay considered to be a more biologically relevant in vitro cell culture system. In addition, Daclatasvir displays similar potency in Huh-7, HeLa and HEK293T cells, demonstrating that the function(s) of NS5A inhibited by Daclatasvir is (are) highly conserved in different cellular environments[1].

    In Vivo

    In a randomized, double-blind, placebo-controlled, single ascending-dose study, Daclatasvir (BMS-790052) is administered at six dose levels to healthy, non-HCV-infected subjects over a range of 1 to 200 mg as an oral solution. Daclatasvir is safe and well tolerated up to 200 mg with no clinically relevant adverse effects. After oral administration, Daclatasvir is readily absorbed, with dose-proportional exposures over the studied dose range, and all subjects have drug concentrations greater than the protein-binding-adjusted EC90 for genotypes 1a and 1b, as measured in the replicon assay, at and beyond 24 h post-dose. (The protein binding-adjusted EC90 figures are derived from an analysis of the effect of the addition of human serum on antiviral activity in replicons. In the presence of 40% human serum, the EC90 for Daclatasvir is 383 pM (0.28 ng/mL) for the genotype 1a replicon and 49 pM (0.04 ng/mL) for the genotyope 1b replicon)[1]. Mice in each group that developed persistent HCV infection are divided into two treatment groups. One group receive 4 weeks of Asunaprevir/Daclatasvir treatment and the other group received 4 weeks of Ledipasvir/GS-558093 treatment. Asunaprevir/Daclatasvir therapy and Ledipasvir/GS-558093 therapy rapidly decease serum HCV RNA levels to below the sensitivity, and they are not detected after completion of the therapy except for two mice in the Ledipasvir/GS-558093 group[2].

    Molecular Weight

    738.88

    Formula

    C₄₀H₅₀N₈O₆

    CAS No.

    1009119-64-5

    SMILES

    O=C([[email protected]@H](NC(OC)=O)C(C)C)N1CCC[[email protected]]1C2=NC=C(N2)C3=CC=C(C=C3)C4=CC=C(C5=CN=C([[email protected]@H]6CCCN6C([[email protected]@H](NC(OC)=O)C(C)C)=O)N5)C=C4

    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 : ≥ 40 mg/mL (54.14 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.3534 mL 6.7670 mL 13.5340 mL
    5 mM 0.2707 mL 1.3534 mL 2.7068 mL
    10 mM 0.1353 mL 0.6767 mL 1.3534 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 (3.38 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.5 mg/mL (3.38 mM); Clear solution

    • 3.

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

      Solubility: ≥ 2.5 mg/mL (3.38 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [1]

    HCV genotype 1a and 1b replicon cells are maintained in media containing Daclatasvir at a concentration of 5- to 20-fold above EC50 and 0.5 mg/mL G418. Replicon cells similarly treated with DMSO are maintained as controls. After approximately 4-5 weeks when cell growth is similar to DMSO-treated control cells, selected cells are expanded for resistance testing and analysis by PCR with reverse transcription[1].

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

    Animal Administration
    [2]

    Mice[2]
    Humanized liver chimeric mice, whose chimeric rate of the liver is estimated as over 40 %, are injected intravenously with 100 µL of HCV-positive human serum samples. After inoculation, their blood is collected from an external jugular vein every 1-4 weeks. The HCV RNA levels are measured by the COBAS TaqMan HCV test in 100-fold diluted serum with a lower measurement range of 3.2 log IU/mL serum. After serum levels of HCV RNA reach plateau levels, mice are administered orally once a day for 4 weeks with one of the following: 40 mg/kg of Asunaprevir plus 30 mg/kg of Daclatasvir, 15 mg/kg of Ledipasvir plus 50 mg/kg of GS-558093 and 50 mg/kg of GS-558093 plus 400 mg/kg of Telaprevir.

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

    References

    Purity: 99.24%

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    Product Name:
    Daclatasvir
    Cat. No.:
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