Daclatasvir (BMS-790052)

For research use only.

Catalog No.S1482 Synonyms: EBP883

42 publications

Daclatasvir (BMS-790052) Chemical Structure

CAS No. 1009119-64-5

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.

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Selleck's Daclatasvir (BMS-790052) has been cited by 42 publications

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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

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 NXzQfWlpTnWwY4Tpc44h[XO|YYm= NIX3NIw{KGSjeYO= MnuwRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGNXKGenbn;0fZBmKDGkIHnu[oVkfGWmIHnuJIh2dWGwIFj1bFch[2WubIOgZYZ1\XJiMzDkZZl{KGK7IHPlcIwu[mG|ZXSgdoVxdGmlb36gZZN{[XluIFXDOVA:O2VvME[g{txO NFHibpMzPTF2OEGwNC=>
human CEM cells NIrTNWxEgXSxdH;4bYNqfHliYYPzZZk> NGi1PWk{KGSjeYO= NYjnZWw4S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hS0WPIHPlcIx{KGGodHXyJFMh\GG7czygR2M2OD17Lk[g{txO M{jRPFI2OTV2N{G0
african green monkey Vero cells M3jhcWN6fG:2b4jpZ4l1gSCjc4PhfS=> M1\EPGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGGocnnjZY4h\3KnZX6gcY9vc2W7IG\ldo8h[2WubIOsJGNEPTB;OT62JO69VQ>? MXSyN|Q3PjJ|Mx?=
human CEM cells NEfmZYREgXSxdH;4bYNqfHliYYPzZZk> M2\JWmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGNGVSClZXzsd{whS0N3ME25MlYh|ryP NHXyNWwzOjdyNEi4Oy=>
human PBMC cells MVTDfZRwfG:6aXPpeJkh[XO|YYm= NIHkTGxEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSk2FIHPlcIx{NCCFQ{WwQVE6KM7:TR?= MlzyNlI4ODR6OEe=

... Click to View More Cell Line Experimental Data

Protocol

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)
Water Insoluble
Ethanol '148 mg/mL

* 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
Formula

C40H50N8O6

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

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03208322 Unknown status Other: Non-Interventional Hepatitis C Bristol-Myers Squibb November 30 2018 --
NCT03487848 Active not recruiting Drug: Daclatasvir|Drug: Sofosbuvir Hepatitis C|Chronic Hepatitis Bristol-Myers Squibb May 18 2018 Phase 2
NCT03540212 Recruiting Drug: Daclatasvir and sofosbuvir Chronic HCV Infection Ain Shams University December 10 2017 Phase 2|Phase 3
NCT03004625 Completed Drug: daclatasvir|Drug: asunaprevir|Drug: Ribavirin Hepatitis C Kaohsiung Medical University Chung-Ho Memorial Hospital|Chang Gung Memorial Hospital|National Taiwan University Hospital|Taipei Veterans General Hospital Taiwan|China Medical University Hospital|National Cheng-Kung University Hospital November 2016 Phase 3
NCT02865369 Not yet recruiting Drug: Daclatasvir and Asunaprevir Chronic Hepatitis C Sang Gyune Kim|Seoul National University Boramae Hospital|Severance Hospital|Inha University Hospital|Korea University|Gachon University Gil Medical Center|Hanyang University Seoul Hospital|Ewha Womans University Mokdong Hospital|Bristol-Myers Squibb|Soonchunhyang University Hospital September 2016 --

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID