Bersacapavir
Based on 3 publication(s) in Google Scholar
Bersacapavir (JNJ-6379) is an HBV capsid assembly modulator. Bersacapavir exerts a dual mechanism of action against both early and late stages of HBV infection by forming complete genome-free empty capsids and inhibiting de novo synthesis of cccDNA. Bersacapavir inhibits HBV replication. Bersacapavir can be used in the research of hepatitis B.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 98.90%
- CAS No.: 1638266-40-6
- Formule: C16H14F4N4O3S
- Masse moléculaire:418.37
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Bersacapavir
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Activité biologique
Description
In Vitro
Bersacapavir (0.625-10 μM) enhances the rate and extent of HBV capsid assembly in a dose-dependent manner in cell-free fluorescence quenching assays using the Cp*150 protein[1].
Bersacapavir potently inhibits HBV replication in HepG2.117 cells, with an EC50 of 54 nM and an EC90 of 226 nM[1].
Bersacapavir inhibits HBV replication in HepG2.2.15 cells, with an EC50 of 69 nM and an EC90 of 241 nM[1].
Bersacapavir (0.24-1000 nM) exhibits additive to synergistic antiviral activity in HepG2.2.15 cells when combined with TDF or ETV[1].
Bersacapavir (0-5000 nM; 11 days) dose-dependently reduces extracellular HBV DNA (EC50: 93 nM), intracellular HBV RNA (EC50: 876 nM), extracellular HBe/cAg (EC50: 960 nM), and extracellular HBsAg (EC50: 1608 nM), and inhibits cccDNA formation when added together with viral inoculum to HBV-infected PHHs[1].
Bersacapavir (2-10 μM; 30 min) disrupts pre-formed mature HBV capsids in HepG2.117 cells, rendering the DNA inside the capsids susceptible to DNase I digestion[1].
Bersacapavir (0.625-10 μM) dose-dependently inhibits de novo cccDNA formation in HBV-infected PHHs when co-administered with viral inoculum[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1638266-40-6
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Appearance Solid
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Masse moléculaire 418.37
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Formule C16H14F4N4O3S
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Color Light yellow to khaki
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SMILES
O=C(C1=CC(S(=O)(N[C@@H](C)C(F)(F)F)=O)=CN1C)NC2=CC=C(F)C(C#N)=C2
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Synonyms
JNJ-6379; JNJ-56136379
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Viruses
Canocapavir Is a Novel Capsid Assembly Modulator Inducing a Conformational Change of the Linker Region of HBV Core Protein. [Abstract]2023 May 18;15(5):1195. PMID: 37243280 -
Anal Methods
An automated microfluidic platform for the screening and characterization of novel hepatitis B virus capsid assembly modulators. [Abstract]2022 Jan 6;14(2):135-146. PMID: 34918017 -
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (239.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
Pureté et documentation
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Fiche technique (274 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.3902 mL | 11.9511 mL | 23.9023 mL | 59.7557 mL |
| 5 mM | 0.4780 mL | 2.3902 mL | 4.7805 mL | 11.9511 mL | |
| 10 mM | 0.2390 mL | 1.1951 mL | 2.3902 mL | 5.9756 mL | |
| 15 mM | 0.1593 mL | 0.7967 mL | 1.5935 mL | 3.9837 mL | |
| 20 mM | 0.1195 mL | 0.5976 mL | 1.1951 mL | 2.9878 mL | |
| 25 mM | 0.0956 mL | 0.4780 mL | 0.9561 mL | 2.3902 mL | |
| 30 mM | 0.0797 mL | 0.3984 mL | 0.7967 mL | 1.9919 mL | |
| 40 mM | 0.0598 mL | 0.2988 mL | 0.5976 mL | 1.4939 mL | |
| 50 mM | 0.0478 mL | 0.2390 mL | 0.4780 mL | 1.1951 mL | |
| 60 mM | 0.0398 mL | 0.1992 mL | 0.3984 mL | 0.9959 mL | |
| 80 mM | 0.0299 mL | 0.1494 mL | 0.2988 mL | 0.7469 mL | |
| 100 mM | 0.0239 mL | 0.1195 mL | 0.2390 mL | 0.5976 mL |
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