Home Proteases HCV Protease inhibitor Daclatasvir (BMS-790052) For research use only.

Daclatasvir (BMS-790052)

Synonyms: EBP883

Daclatasvir (BMS-790052, EBP883) 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.

Daclatasvir (BMS-790052) Chemical Structure

Daclatasvir (BMS-790052) Chemical Structure

CAS No. 1009119-64-5

Purity & Quality Control

Daclatasvir (BMS-790052) Related Products

Signaling Pathway

HCV Protease Signaling Pathways

HCV Protease Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human CEM cells Cytotoxicity assay 3 days Cytotoxicity against human CEM cells after 3 days, CC50=9.6 μM 25154714
Huh7 Antiviral assay 3 days Antiviral activity against HCV genotype 1b infected in human Huh7 cells after 3 days by cell-based replicon assay, EC50=0.000003μM 25148100
Huh-luc/neo-ET replicon Antiviral assay 48 hrs Antiviral activity against Hepatitis C virus genotype 1b harboring NS5A L28V mutant gene in Huh-luc/neo-ET replicon cells after 48 hrs by transient replicon mutant-based luciferase assay, EC50=0.000004μM 24568313
HuH7 Antiviral assay Antiviral activity against HCV genotype 1b infected in human HuH7 cells assessed as reduction in viral RNA replication, EC50=0.000004μM 26099532
HuH7 Antiviral assay Antiviral activity against HCV1b infected in human HuH7 cells assessed as inhibition of viral replication by RT-PCR analysis, EC50=0.0000066μM 22507961
HuH-Lcu-Neo Function assay 48 hrs Inhibition of NS5A in HCV genotype 1b infected in HuH-Lcu-Neo cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter gene assay, EC50=0.0000081μM 32202782
Huh-5.2 Antiviral assay 4 days Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh-5.2 cells assessed as decrease in HCV replicon RNA replication after 4 days by luciferase assay, EC50=0.000009μM 24900811
HuH7 Antiviral assay 3 days Antiviral activity against HCV genotype 1b Con1 infected in human HuH7 cells assessed as inhibition of viral RNA replication after 3 days by renilla luciferase reporter gene assay, EC50=0.000009μM 24320933
HuH7 Antiviral assay 72 hrs Antiviral activity against HCV1b infected in human HuH7 cells assessed as inhibition of viral replication after 72 hrs by FRET assay, EC50=0.000009μM 24521299
HuH7 Antiviral assay Antiviral activity against HCV genotype 1b Con1 infected in human HuH7 cells assessed as inhibition of viral replication, EC50=0.000009μM 26077493
Huh7.5/J6/JFH1/EMCVIRES/hRlucNeo Function assay 72 hrs Inhibition of NS5A in HCV genotype 2a infected in human Huh7.5/J6/JFH1/EMCVIRES/hRlucNeo cells assessed as inhibition of replicon levels incubated for 72 hrs by luciferase reporter gene assay, IC50=0.000009μM 31710479
HuH7 replicon Function assay 2 days Inhibition of NS5A in HCV genotype 1b infected in human HuH7 replicon cells assessed as reduction in subgenomic viral RNA replication treated for 2 days followed by compound washout and subsequent compound dosing measured after 1 day by SEAP reporter gene, EC50=0.000009μM 30772607
HuH7 Antiviral assay Antiviral activity against HCV 1b infected in human HuH7 cells by in vitro replicon assay, EC50=0.00001μM 23466233
Huh-luc/neo-ET replicon Antiviral assay 48 hrs Antiviral activity against Hepatitis C virus genotype 1b in Huh-luc/neo-ET replicon cells after 48 hrs by replicon-based luciferase assay, EC50=0.00001μM 24568313
HuH7 Function assay Inhibition of NS5A in HCV genotype-1b infected in human HuH7 cells by luciferase reporter gene assay, EC50=0.000023μM 25453810
HuH7.5/Con1/SG-Neo(I)-hRluc2aUb Function assay 72 hrs Inhibition of NS5A in HCV genotype 1b infected in human HuH7.5/Con1/SG-Neo(I)-hRluc2aUb cells assessed as inhibition of replicon levels incubated for 72 hrs by luciferase reporter gene assay, IC50=0.000023μM 31710479
HuH7 Antiviral assay Antiviral activity against HCV genotype 1b JFH-1 infected in human HuH7 cells assessed as inhibition of viral replication, EC50=0.000028μM 26077493
HuH7 Antiviral assay Antiviral activity against HCV 1b infected in human HuH7 cells by in vitro replicon assay, EC90=0.00003μM 23466233
HuH-Lcu-Neo Function assay 48 hrs Inhibition of NS5A in HCV genotype 1a infected in HuH-Lcu-Neo cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter gene assay, EC50=0.0000324μM 32202782
HuH7 Antiviral assay Antiviral activity against HCV genotype 1b expressing NS5A L31V mutant infected in human HuH7 cells assessed as reduction in viral RNA replication, EC50=0.000035μM 26099532
Huh-luc/neo-ET replicon Antiviral assay 48 hrs Antiviral activity against Hepatitis C virus genotype 1a in Huh-luc/neo-ET replicon cells after 48 hrs by replicon-based luciferase assay, EC50=0.0000398μM 24568313
HuH7 Antiviral assay Antiviral activity against wild type HCV genotype 1b infected in human HuH7 cells assessed as reduction in viral RNA replication, EC50=0.000048μM 26099532
W11.8 Antiviral assay 4 days Antiviral activity against Hepatitis C virus genotype 1a infected in W11.8 cells assessed as decrease in NS5A expression in replicon cell after 4 days by luminescence based ELISA, EC50=0.00005μM 24900811
HuH7 Antiviral assay 3 days Antiviral activity against HCV genotype 1a H77 infected in human HuH7 cells assessed as inhibition of viral RNA replication after 3 days by renilla luciferase reporter gene assay, EC50=0.00005μM 24320933
HuH7 Antiviral assay 72 hrs Antiviral activity against HCV1a infected in human HuH7 cells assessed as inhibition of viral replication after 72 hrs by FRET assay, EC50=0.00005μM 24521299
HuH7 Antiviral assay Antiviral activity against HCV genotype 5a infected in human HuH7 cells by luciferase reporter gene assay, EC50=0.000051μM 25453811
HuH7 Antiviral assay Antiviral activity against HCV genotype 1b infected in human HuH7 cells by luciferase reporter gene assay, EC50=0.000073μM 25453811
HuH-Lcu-Neo Function assay 48 hrs Inhibition of NS5A in patient-derived HCV genotype 3a infected in HuH-Lcu-Neo cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter gene assay, EC50=0.0001145μM 32202782
Huh-luc/neo-ET replicon Antiviral assay 48 hrs Antiviral activity against Hepatitis C virus genotype 1b harboring NS5A L31V mutant gene in Huh-luc/neo-ET replicon cells after 48 hrs by transient replicon mutant-based luciferase assay, EC50=0.0001259μM 24568313
HuH7 Function assay Inhibition of NS5A in HCV genotype-1a infected in human HuH7 cells by luciferase reporter gene assay, EC50=0.00014μM 25453810
HuH7 Antiviral assay Antiviral activity against HCV genotype 1a infected in human HuH7 cells by luciferase reporter gene assay, EC50=0.00014μM 25453811
HuH7 Antiviral assay Antiviral activity against HCV genotype 1b expressing NS5A Y93H mutant infected in human HuH7 cells assessed as reduction in viral RNA replication, EC50=0.00018μM 26099532
Huh-luc/neo-ET replicon Antiviral assay 48 hrs Antiviral activity against Hepatitis C virus genotype 1b harboring NS5A Y93H mutant gene in Huh-luc/neo-ET replicon cells after 48 hrs by transient replicon mutant-based luciferase assay, EC50=0.0003162μM 24568313
HuH7 Antiviral assay 72 hrs Antiviral activity against HCV1a infected in human HuH7 cells assessed as inhibition of viral replication after 72 hrs by FRET assay, EC90=0.00038μM 24521299
HuH7 Antiviral assay Antiviral activity against HCV genotype 4a infected in human HuH7 cells by luciferase reporter gene assay, EC50=0.00041μM 25453811
HuH-Lcu-Neo Function assay 48 hrs Inhibition of NS5A in HCV genotype 3a con infected in HuH-Lcu-Neo cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter gene assay, EC50=0.0004115μM 32202782
HuH7 Antiviral assay Antiviral activity against HCV genotype 6a infected in human HuH7 cells by luciferase reporter gene assay, EC50=0.00045μM 25453811
HuH7 Antiviral assay Antiviral activity against HCV genotype 3a infected in human HuH7 cells by luciferase reporter gene assay, EC50=0.00067μM 25453811
HuH7 Antiviral assay Antiviral activity against HCV genotype 2a infected in human HuH7 cells by luciferase reporter gene assay, EC50=0.00067μM 25453811
HuH-Lcu-Neo Function assay 48 hrs Inhibition of NS5A in patient-derived HCV genotype 2a infected in HuH-Lcu-Neo cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter gene assay, EC50=0.0494μM 32202782
HuH-Lcu-Neo Function assay 48 hrs Inhibition of NS5A in HCV genotype 2a con infected in HuH-Lcu-Neo cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter gene assay, EC50=0.05285μM 32202782
CEM Cytotoxicity assay 3 days Cytotoxicity against human CEM cells after 3 days, CC50=9.6μM 22507961
CEM Cytotoxicity assay Cytotoxicity against human CEM cells, CC50=9.6μM 22704887
Vero Cytotoxicity assay Cytotoxicity against african green monkey Vero cells, CC50=9.6μM 23466233
CEM Cytotoxicity assay Cytotoxicity against human CEM cells, CC50=10μM 26099532
PBMC Cytotoxicity assay Cytotoxicity against human PBMC cells, CC50=19μM 22704887
Vero Cytotoxicity assay 3 days Cytotoxicity against african green monkey Vero cells after 3 days, CC50=21μM 22507961
Vero Cytotoxicity assay Cytotoxicity against african green monkey Vero cells, CC50=21μM 22704887
CEM Cytotoxicity assay Cytotoxicity against human CEM cells, CC50=21μM 23466233
Vero Cytotoxicity assay Cytotoxicity against african green monkey Vero cells, CC50=21μM 26099532
Huh7.5.1 Antiviral assay 100 pM to 1 uM Antiviral activity against HCV genotype 1b NK/R2AN infected in human Huh7.5.1 cells expressing NS5A L31V mutant assessed as reduction in virus replication at 100 pM to 1 uM by luciferase reporter gene assay 26134551
Huh7.5.1 Antiviral assay 100 pM to 1 uM Antiviral activity against HCV genotype 1b NK/R2AN infected in human Huh7.5.1 cells expressing NS5A Y93H mutant assessed as reduction in virus replication at 100 pM to 1 uM by luciferase reporter gene assay 26134551
GS4.3 Antiviral assay 0.15 uM 6 days Antiviral activity against HCV infected in human GS4.3 cells assessed as inhibition of NS3/4A levels at 0.15 uM treated with fresh media containing compound every 2 days measured after 6 days by Western blot method 29232582
GS4.3 Antiviral assay 0.15 uM 6 days Antiviral activity against HCV infected in human GS4.3 cells assessed as inhibition of viral core protein levels at 0.15 uM treated with fresh media containing compound every 2 days measured after 6 days by Western blot method 29232582
HuH7 Antiviral assay 3 days Antiviral activity against HCV genotype 1b infected in human HuH7 cells at >= 10 times antiviral EC50 after 3 days by luciferase reporter assay 28430437
HuH7 Antiviral assay 3 days Antiviral activity against HCV genotype 1b infected in human HuH7 cells co-treated with asunaprevir after 3 days by luciferase reporter assay 28430437
Click to View More Cell Line Experimental Data

Biological Activity

Description Daclatasvir (BMS-790052, EBP883) 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.
Targets
HCV NS5A [1]
9 pM-50 pM(EC50)
In vitro
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]
Kinase Assay 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 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.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05992077 Recruiting
HCV Infection
ANRS Emerging Infectious Diseases
 August 7 2023 Not Applicable
NCT04852614 Recruiting
Hepatitis C Virus Infection
Ain Shams University
 December 1 2020 --
NCT04773756 Completed
Covid19
Alexandria University
 November 1 2020 Phase 4
NCT03208322 Withdrawn
Hepatitis C
Bristol-Myers Squibb
 November 30 2018 --

Chemical Information & Solubility

Molecular Weight 738.88 Formula

C40H50N8O6
CAS No. 1009119-64-5 SDF Download Daclatasvir (BMS-790052) SDF
Smiles CC(C)C(C(=O)N1CCCC1C2=NC=C(N2)C3=CC=C(C=C3)C4=CC=C(C=C4)C5=CN=C(N5)C6CCCN6C(=O)C(C(C)C)NC(=O)OC)NC(=O)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 148 mg/mL ( (200.3 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 148 mg/mL

Water : Insoluble


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