| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Daclatasvir (formerly BMS-790052; EBP-883; trade name Daklinza), a direct-acting antiviral agent, is a selective inhibitor of HCV NS5A (nonstructural protein) with an EC50 of 9-50 pM. In order to treat hepatitis C (HCV), daclatasvir has been used in conjunction with sofosbuvir, another antiviral medication, to lower the levels of HCV RNA in the serum. 2014 saw the EU approve it after it was developed by BMS. The HCV nonstructural protein NS5A is inhibited by daclatasvir. According to a recent study, it targets two stages of the viral replication process, allowing HCV RNA to rapidly decline. Daclatasvir has been tested in combination regimens with ribavirin and pegylated interferon, as well as with other direct-acting antiviral medications like sofosbuvir and asunaprevir.
| Targets |
HCV NS5A (EC50 = 9 pM-50 pM)
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| ln Vitro |
BMS-790052 is among the strongest HCV replication inhibitors found to date. For HCV genotype 1a and 1b replicons, the mean EC50 values of BMS-790052 are 50 and 9 pM, respectively. BMS-790052 is inactive against a panel of 10 RNA and DNA viruses, with an EC50 greater than 10 μM, and exhibits a therapeutic index (CC50/EC50) of at least 105. This validates the HCV specificity of BMS-790052.[1] BMS-790052, with EC50 values ranging from 1 to 15 pM, inhibits both transient and stable HCV genome replication in Huh7 cells expressing the HCV genotype 1b replicons. It has been demonstrated that BMS-790052 (100 pM or 1 nM) modifies the subcellular localization and biochemical fractionation of NS5A.[2] With an EC50 of 7–13 pM, BMS-790052 suppresses hybrid replicons carrying HCV genotype–4 NS5A genes. In the hybrid replicons, residue 30 of NS5A plays a crucial role in BMS-790052-mediated resistance.[3]
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| ln Vivo |
Humanized liver chimeric mice, with an estimated 40% chimeric liver, receive intravenous injections of 100 µL of human serum samples positive for HCV. Every one to four weeks following the vaccination, their blood is drawn from an external jugular vein. With a lower measurement range of 3.2 log IU/mL serum, the COBAS TaqMan HCV test measures the HCV RNA levels in 100-fold diluted serum. Once serum HCV RNA levels plateau, mice are given 40 mg/kg of Asunaprevir plus 30 mg/kg of Daclatasvir, 15 mg/kg of Ledipasvir plus 50 mg/kg of GS-558093, or 50 mg/kg of GS-558093 plus 400 mg/kg of Telaprevir orally once a day for four weeks.
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| Enzyme Assay |
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 consists of 20 μM FRET peptide, 150 mM NaCl, and 5× luciferase cell culture lysis reagent diluted to 1× with dH2O. In a 96-well plate, HCV-Huh-7 cells are added and left to attach for the entire night (1×104 cells per well). The plate is incubated for 72 hours after BMS-790052 is added to the wells the following day. After that, the plate is cleaned with PBS and prepared for the FRET test by adding 30 μL of the previously mentioned FRET peptide assay reagent to each well.
Signals are acquired by reading the plate in the kinetic mode with the Cytofluor 4000 instrument, which is programmed to operate in the automatic mode at 340 nm (excitation)/490 nm (emission) for 20 cycles or less. Once FRET is completed, each well is filled with 40 μL of luciferase substrate, and the amount of luciferase is evaluated.
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| Cell Assay |
BMS-790052 is added to 96-well plates that have HCV replicon cells seeded in 200 µL media about 12 hours earlier.After being incubated for 72 hours, the cell plates are examined for cytotoxicity and replication activity. Following the measurement of cytotoxicity using CellTiter-Blue, the media and dye are removed, the plates are inverted, and the liquid that remains is blotted with paper towels. Renilla luciferase is used to measure the HCV genotype 1a cell lines' replication activity. After adding 1× Renilla luciferase lysis buffer (30 µL) to each well, the plates are incubated for 15 minutes with light shaking. The signals are then detected using a Top Count luminometer that is configured for light emission quantification after adding 40 µL of renilla luciferase substrate. The DMSO-only wells calculate 100% activity for each cell line; the average value for compound-containing wells is divided by the average value for DMSO-containing wells to determine the percentage activity for each inhibitor concentration.
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| Animal Protocol |
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| References |
| Molecular Formula |
C40H50N8O6
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| Molecular Weight |
738.890
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| Exact Mass |
738.39
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| Elemental Analysis |
C, 65.02; H, 6.82; N, 15.17; O, 12.99
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| CAS # |
1009119-64-5
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| Related CAS # |
Daclatasvir dihydrochloride;1009119-65-6;Daclatasvir-d6;1801709-41-0;Daclatasvir-d16
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| Appearance |
Solid powder
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| SMILES |
CC(C)[C@@H](C(=O)N1CCC[C@H]1C2=NC=C(N2)C3=CC=C(C=C3)C4=CC=C(C=C4)C5=CN=C(N5)[C@@H]6CCCN6C(=O)[C@H](C(C)C)NC(=O)OC)NC(=O)OC
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| InChi Key |
FKRSSPOQAMALKA-CUPIEXAXSA-N
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| InChi Code |
InChI=1S/C40H50N8O6/c1-23(2)33(45-39(51)53-5)37(49)47-19-7-9-31(47)35-41-21-29(43-35)27-15-11-25(12-16-27)26-13-17-28(18-14-26)30-22-42-36(44-30)32-10-8-20-48(32)38(50)34(24(3)4)46-40(52)54-6/h11-18,21-24,31-34H,7-10,19-20H2,1-6H3,(H,41,43)(H,42,44)(H,45,51)(H,46,52)/t31-,32-,33-,34-/m0/s1
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| Chemical Name |
methyl N-[(2S)-1-[(2S)-2-[5-[4-[4-[2-[(2S)-1-[(2S)-2-(methoxycarbonylamino)-3-methylbutanoyl]pyrrolidin-2-yl]-1H-imidazol-5-yl]phenyl]phenyl]-1H-imidazol-2-yl]pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]carbamate dihydrochloride
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| Synonyms |
BMS-790052; Daclatasvir; BMS790052; BMS 790052; EBP883; EBP 883; EBP-883; Daklinza (trade name)
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3534 mL | 6.7669 mL | 13.5338 mL | |
| 5 mM | 0.2707 mL | 1.3534 mL | 2.7068 mL | |
| 10 mM | 0.1353 mL | 0.6767 mL | 1.3534 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03882307 | Recruiting | Drug: sofosbuvir and daclatasvir | Hepatitis C, Chronic | Assiut University | October 2022 | Early Phase 1 |
| NCT05992077 | Recruiting | Drug: Sofosbuvir/Daclatasvir | HCV Infection | ANRS, Emerging Infectious Diseases |
August 7, 2023 | Not Applicable |
| NCT03646396 | Recruiting | Drug: Sofosbuvir-daclatasvir | HCV Coinfection | Sherief Abd-Elsalam | August 1, 2018 | Not Applicable |
| NCT03540212 | Recruiting | Drug: Daclatasvir and sofosbuvir | Chronic HCV Infection | Ain Shams University | December 10, 2017 | Phase 2 Phase 3 |
| NCT04468087 | Active Recruiting |
Drug: Atazanavir Drug: Daclatasvir 60 mg |
COVID-19 | Hospital do Coracao | February 15, 2021 | Phase 2 Phase 3 |
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