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  3. Daclatasvir dihydrochloride

Daclatasvir dihydrochloride (Synonyms: BMS-790052 dihydrochloride; EBP 883 dihydrochloride)

Cat. No.: HY-10465 Purity: 99.62%
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Daclatasvir dihydrochloride (BMS-790052 dihydrochloride) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir dihydrochloride is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively.

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

Daclatasvir dihydrochloride Chemical Structure

Daclatasvir dihydrochloride Chemical Structure

CAS No. : 1009119-65-6

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Customer Review

Based on 44 publication(s) in Google Scholar

Other Forms of Daclatasvir dihydrochloride:

Top Publications Citing Use of Products

Publications Citing Use of MCE Daclatasvir dihydrochloride

    Daclatasvir dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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.
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    Description

    Daclatasvir dihydrochloride (BMS-790052 dihydrochloride) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir dihydrochloride is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively[1][2][3].

    IC50 & Target

    EC50: 50 pM (HCV replicon genotype 1a), 9 pM (HCV replicon genotype 1b), 71 pM (HCV replicon genotype 2a), 146 pM (HCV replicon genotype 3a), 12 pM (HCV replicon genotype 4a) and 33 pM (HCV replicon genotype 5a)[1]
    Kd: 8 nM (NS5A33-202) and 210 nM (NS5A26-202)[2]
    IC50: 1.5 µM (OATP1B) and 3.27 µM (OATP1B3)[3]

    In Vitro

    Daclatasvir (BMS-790052) demonstrates potent inhibitory activity towards all genotypes tested, with EC50 values ranging from 9 pM to 146 pM. Daclatasvir inhibits HCV replicon genotype 1a, 1b, 2a, 3a, 4a and 5a with EC50 values of 50 pM, 9 pM, 71 pM, 146 pM, 12 pM and 33 pM, respectively. Daclatasvir is a potent inhibitor of the JFH-1 genotype 2a infectious virus that replicates in cell culture (EC50=28 pM)[1]. Daclatasvir (BMS-790052) binds tightly to NS5A33-202 and NS5A26-202 with Kds of 8 nM and 210 nM, respectively[2].

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

    In Vivo

    Daclatasvir (BMS-790052; 30 mg/kg; oral administration; daily; for 27 days) treatment reduces serum HCV RNA titers very rapidly by ~1.5 log10 at day 3[4].

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

    Animal Model: NOD/SCID male mice (5 weeks of age, 18-20 g) bearing HCV RNA-transfected cells[4]
    Dosage: 30 mg/kg
    Administration: Oral administration; daily; for 27 days
    Result: Reduced serum HCV RNA titers very rapidly by ~1.5 log10 at day 3.
    Clinical Trial
    Molecular Weight

    811.80

    Formula

    C₄₀H₅₂Cl₂N₈O₆

    CAS No.

    1009119-65-6

    SMILES

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

    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 : ≥ 56 mg/mL (68.98 mM)

    H2O : 50 mg/mL (61.59 mM; Need ultrasonic)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.2318 mL 6.1592 mL 12.3183 mL
    5 mM 0.2464 mL 1.2318 mL 2.4637 mL
    10 mM 0.1232 mL 0.6159 mL 1.2318 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 mg/mL (1.23 mM); Clear solution

    • 2.

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

      Solubility: ≥ 1 mg/mL (1.23 mM); Clear solution

    • 3.

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

      Solubility: ≥ 1 mg/mL (1.23 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.62%

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    Keywords:

    DaclatasvirBMS-790052EBP 883BMS790052BMS 790052EBP883EBP-883HCVHepatitis C virusNS5AreplicongenotypesantiviralJFH-1OATP1B1OATP1B3Inhibitorinhibitorinhibit

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    Product Name:
    Daclatasvir dihydrochloride
    Cat. No.:
    HY-10465
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