2. Anti-infection
  3. HCV
  4. Daclatasvir dihydrochloride

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

Cat. No.: HY-10465 Purity: 99.68%
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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 an 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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10 mM * 1 mL in DMSO
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Based on 50 publication(s) in Google Scholar

Other Forms of Daclatasvir dihydrochloride:

Daclatasvir dihydrochloride Related Antibodies

Top Publications Citing Use of Products

46 Publications Citing Use of MCE Daclatasvir dihydrochloride

WB

    Daclatasvir dihydrochloride purchased from MedChemExpress. Usage Cited in: PLoS Pathog. 2018 Sep 18;14(9):e1007284.  [Abstract]

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

    Daclatasvir dihydrochloride purchased from MedChemExpress. Usage Cited in: Eur J Med Chem. 2018 Jan 1;143:1053-1065.  [Abstract]

    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 MedChemExpress. Usage Cited in: Eur J Med Chem. 2018 Jan 1;143:1053-1065.  [Abstract]

    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 MedChemExpress. Usage Cited in: Open Virol J. 2014 Mar 7;8:1-8.  [Abstract]

    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.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    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 an 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].

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

    Daclatasvir dihydrochloride Related Antibodies
    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].

    MedChemExpress (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.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 56 mg/mL (68.98 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 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

      This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 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

      This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.68%

    COA (257 KB) LCMS (95 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 1.2318 mL 6.1592 mL 12.3183 mL 30.7958 mL
    5 mM 0.2464 mL 1.2318 mL 2.4637 mL 6.1592 mL
    10 mM 0.1232 mL 0.6159 mL 1.2318 mL 3.0796 mL
    15 mM 0.0821 mL 0.4106 mL 0.8212 mL 2.0531 mL
    20 mM 0.0616 mL 0.3080 mL 0.6159 mL 1.5398 mL
    25 mM 0.0493 mL 0.2464 mL 0.4927 mL 1.2318 mL
    30 mM 0.0411 mL 0.2053 mL 0.4106 mL 1.0265 mL
    40 mM 0.0308 mL 0.1540 mL 0.3080 mL 0.7699 mL
    50 mM 0.0246 mL 0.1232 mL 0.2464 mL 0.6159 mL
    60 mM 0.0205 mL 0.1027 mL 0.2053 mL 0.5133 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Daclatasvir dihydrochloride Related Classifications

    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.

    Keywords:

    Daclatasvir1009119-65-6BMS-790052EBP 883BMS790052BMS 790052EBP883EBP-883HCVHepatitis C virusNS5AreplicongenotypesantiviralJFH-1OATP1B1OATP1B3Inhibitorinhibitorinhibit

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