Daclatasvir (BMS-790052)
For research use only.
Catalog No.S1482 Synonyms: EBP883
45 publications

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.
Purity & Quality Control
Choose Selective HCV Protease Inhibitors
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. | ||||||||||||||||||||||||||||||||||||||||||||
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Features | First-in-class, highly selective inhibitor of hepatitis C virus (HCV) NS5A with picomolar EC50 values. | ||||||||||||||||||||||||||||||||||||||||||||
Targets |
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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] |
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Cell Data |
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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. |
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Cell Research:[1] |
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Solubility (25°C)
In vitro | DMSO | 148 mg/mL (200.3 mM) |
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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 |
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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 |
In vivo Formulation Calculator (Clear solution)
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: : mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL,)
Method for preparing in vivo formulation:Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80,mix and clarify, next add μL ddH2O,mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
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Clinical Trial Information
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
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NCT03208322 | Unknown status | Other: Non-Interventional | Hepatitis C | Bristol-Myers Squibb | November 30 2018 | -- |
NCT03487848 | Completed | Drug: Daclatasvir|Drug: Sofosbuvir | Hepatitis C|Chronic Hepatitis | Bristol-Myers Squibb | July 17 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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