Daclatasvir (BMS-790052)

Catalog No.S1482 Synonyms: EBP883

Daclatasvir (BMS-790052) Chemical Structure

Molecular Weight(MW): 738.88

Daclatasvir (BMS-790052) is a highly selective inhibitor of HCV NS5A with EC50 of 9-50 pM, for a broad range of HCV replicon genotypes and the JFH-1 genotype 2a infectious virus in cell culture. Phase 3.

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4 Customer Reviews

  • Sensitivity of PR63cc to the combinatory treatment with asunaprevir and daclatasvir. Huh7.5.1 cells infected with PR63cc or JFH1 at an MOI of 0.05 for 3 days were treated with either asunaprevir, daclatasvir or in combination for another 3 days. 40 nM asunaprevir and 0.05 nM daclatasvir, approximately the EC50 concentration of the each inhibitor for JFH1, were used. The antiviral efficiency of each compound was evaluated by quantifying the intracellular HCV RNA by RT-qPCR. Data were expressed as the percentage of mock treatment control. The error bars were calculated from two independent experiments. ns, P > 0.05. *, P < 0.05.

    Antiviral Res, 2017, 139:18-24. Daclatasvir (BMS-790052) purchased from Selleck.

    The toxicity of BMS-790052 (BMS) and Telaprevir (TPV) was measured by seeding 96-well plates to 70% confluence and exposing the cells to up to 50 μM of compound for 72 hours. MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] was added to each well at a final concentration of 500 μg/ml 4 h before dissolving crystals in 100 μl of DMSO and measuring at 550 nm UV wavelengths. The 50% cytotoxic concentration (CC50) was then calculation using the OD550 value and the following formula: log CC50=log concentration of HPP-[(HPP-50)/(HPP-LPP)×log d HPP: highest protective percentage closest to 50% LPP: Lowest protective percentage closest to 50% d: dilution factor

    2011 Dr. Julie Sheldon,Dr Esteban Domingo and Dr Celia Perales. Daclatasvir (BMS-790052) purchased from Selleck.

  • Huh7.5 cells were infected with JFH-1 (2a) strain. Once the cells reached 80% infectivity they were treated with pMconcentration of BMS790052 for two different time points. Cells were collected in SDS sample loading buffer and probed for NS5A and GAPDH. After 16hrs hyperphosphorylated NS5A disappeared with increasing concentration of the drug. 40hrs of treatment resulted complete disappearance of NS5A. GAPDH is internal control.



    2011 Dr. Anita Nag of Florida State University. Daclatasvir (BMS-790052) purchased from Selleck.

    80% infected HCV JFH-1 cells were treated with several concentrations of BMS790052 in pMrange. Cells were fixed after 16hrs and NS5A was probed.Cells treated with BMS790052 shows NS5A present in clusters compared to an even cytoplasmic distribution in untreated cells.

    2011 Dr. Anita Nag of Florida State University. Daclatasvir (BMS-790052) purchased from Selleck.

Purity & Quality Control

Choose Selective HCV Protease Inhibitors

Biological Activity

Description Daclatasvir (BMS-790052) is a highly selective inhibitor of HCV NS5A with EC50 of 9-50 pM, for a broad range of HCV replicon genotypes and the JFH-1 genotype 2a infectious virus in cell culture. Phase 3.
Features First-in-class, highly selective inhibitor of hepatitis C virus (HCV) NS5A with picomolar EC50 values.
HCV NS5A [1]
9 pM-50 pM(EC50)
In vitro

BMS-790052 is one of the most potent inhibitors of HCV replication reported so far. The mean EC50 valuses of BMS-790052 are 50 and 9 pM for HCV genotype 1a and 1b replicons, respectively. BMS-790052 displays a therapeutic index (CC50/EC50) of at least 105 and is inactive towards a panel of 10 RNA and DNA viruses, with EC50 higher than 10 μM. This confirms BMS-790052's specificity for HCV. [1] In Huh7 cells harboring the HCV genotype 1b replicons, BMS-790052 blocks both transient and stable HCV genome replication, with EC50 values raging from 1-15 pM. BMS-790052 (100 pM or 1 nM) has been shown to alter the subcellular localization and biochemical fractionation of NS5A. [2] BMS-790052 inhibits hybrid replicons containing HCV genotype-4 NS5A genes with EC50 of 7-13 pM. Residue 30 of NS5A is an important site for BMS-790052-mediated resistance in the hybrid replicons. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human Huh7 cells M3\XcWZ2dmO2aX;uJIF{e2G7 Mm\4N{Bl[Xm| MmiyRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGNXKGenbn;0fZBmKDGkIHnu[oVkfGWmIHnuJIh2dWGwIFj1bFch[2WubIOgZYZ1\XJiMzDkZZl{KGK7IHPlcIwu[mG|ZXSgdoVxdGmlb36gZZN{[XluIFXDOVA:O2VvME[g{txO NXj0[IlGOjVzNEixNFA>
human CEM cells NUPifJFQS3m2b4TvfIlkcXS7IHHzd4F6 Mon5N{Bl[Xm| M4fP[GN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGNGVSClZXzsd{Bi\nSncjCzJIRigXNuIFPDOVA:QS54IN88US=> NFXCWmYzPTF3NEexOC=>
african green monkey Vero cells MXTDfZRwfG:6aXPpeJkh[XO|YYm= NXrN[4o1S3m2b4TvfIlkcXS7IHHnZYlve3RiYX\ybYNidiCpcnXlckBud26tZYmgWoVzdyClZXzsd{whS0N3ME25MlYh|ryP M1LD[lI{PDZ4MkOz
human CEM cells M4rQU2N6fG:2b4jpZ4l1gSCjc4PhfS=> M2e4dGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGNGVSClZXzsd{whS0N3ME25MlYh|ryP MXKyNlcxPDh6Nx?=
human PBMC cells NITEdIlEgXSxdH;4bYNqfHliYYPzZZk> M1TFfmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBDVUNiY3XscJMtKEOFNUC9NVkh|ryP MnLsNlI4ODR6OEe=

... Click to View More Cell Line Experimental Data


Kinase Assay:[4]
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FRET assay for HCV NS5A inhibitors:

The peptide (Ac-Asp-Glu-Asp [EDANS]-Glu-Glu-Abu-[COO] Ala-Ser-Lys [DABCYL]-NH2) contains a fluorescence donor {EDANS, 5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid} near one end of the peptide and an acceptor {DABCYL, 4-[(4-dimethylamino)phenyl]azo)benzoic acid} near the other end. Intermolecular resonance energy transfer between the donor and the acceptor quenches the fluorescence of the peptide, but as the NS3 protease cleaves the peptide, the products are released from resonance energy transfer quenching. The fluorescence of the donor increases over time as more substrate is cleaved by the NS3 protease. The assay reagent is: 5× luciferase cell culture lysis reagent diluted to 1× with dH2O, NaCl (150 mM), the FRET peptide (20 μM). HCV-Huh-7 cells are placed in a 96-well plate, and allowed to attach overnight (1×104 cells per well). The next day, BMS-790052 is added to the wells and the plate is incubated for 72 hours. The plate is then rinsed with PBS and used for the FRET assay by the addition of 30 μL of the FRET peptide assay reagent (described above) per well. Signals are obtained using the Cytofluor 4000 instrument, which has been set to 340 nm (excitation)/490 nm (emission) automatic mode, for 20 cycles or less, with the plate being read in the kinetic mode. Following FRET, 40 μL of luciferase substrate is added to each well and the luciferase is measured.
Cell Research:[1]
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  • Cell lines: HCV replicon cells (Huh7)
  • Concentrations: 0.1 pM - 50 μM, dissolved in DMSO (the final concentration of DMSO is 0.5%)
  • Incubation Time: 72 hours
  • Method: BMS-790052 is added to 96-well plates containing HCV replicon cells seeded approximately 12 hours before in 200 µL media.The cell plates are tested for replication activity and cytotoxicity after 72 hours of incubation. Cytotoxicity is measured with CellTiter-Blue, after which the media and dye are removed, plates are inverted and the remaining liquid is blotted with paper towels. Replication activity of the HCV genotype 1a cell lines is quantified using Renilla luciferase. 1× Renilla luciferase lysis buffer (30 µL) is added to each well and plates are incubated with gentle shaking for 15 min. Renilla luciferase substrate (40 µL) is then added and the signals are detected using a Top Count luminometer set for light emission quantification. One hundred per cent activity is calculated for each cell line for the DMSO-only wells; percentage activity is calculated for each concentration of the inhibitor by dividing the average value for wells containing compound by the average value for wells containing DMSO.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 148 mg/mL (200.3 mM)
Ethanol 148 mg/mL (200.3 mM)
Water 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.

Chemical Information

Molecular Weight 738.88


CAS No. 1009119-64-5
Storage powder
in solvent
Synonyms EBP883

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03686722 Completed Diabetes Mellitus Type 2|Hepatitis C|Drug Interactions Mohamed Raslan|Ain Shams University|Drug Research Centre Cairo Egypt September 9 2017 Phase 1
NCT01492504 Completed Hepatitis C Bristol-Myers Squibb February 7 2012 --
NCT02262728 Completed Hepatitis C Chronic Janssen Research & Development LLC September 30 2014 Phase 2
NCT01455090 Completed Chronic Hepatitis C Bristol-Myers Squibb November 30 2011 Phase 2
NCT03247296 Active not recruiting Hepatitis C MTI University February 28 2017 --
NCT03485846 Active not recruiting Chronic Hepatitis C Genotype 1b R-Pharm|Almedis November 27 2017 Phase 2

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID