HBV-IN-4
Based on 1 publication(s) in Google Scholar
HBV-IN-4, a phthalazinone derivative, is a potent and orally active HBV DNA replication inhibitor with an IC50 of 14 nM. HBV-IN-4 induces the formation of genome-free capsids and has potent anti-HBV potencies.
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- Pureza : 99.37%
- No. CAS: 2305897-84-9
- Fòrmula: C24H19ClFN5O3
- Peso molecular:479.89
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) HBV-IN-4
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Actividad biológica
Descripciòn
IC50 & Target
IC50: 14 nM (HBV DNA replication)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 2.2.15 | CC50 |
>100 μM
Compound: 19f
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Cytotoxicity in human HepG2.2.15 cells assessed as reduction in cell viability incubated for 8 days by MTT assay
Cytotoxicity in human HepG2.2.15 cells assessed as reduction in cell viability incubated for 8 days by MTT assay
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[PMID: 32692159] |
| HepG2 2.2.15 | IC50 |
0.014 μM
Compound: 19f
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Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as reduction in cytoplasmic HBV-DNA replication incubated for 8 days by real-time PCR analysis
Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as reduction in cytoplasmic HBV-DNA replication incubated for 8 days by real-time PCR analysis
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[PMID: 32692159] |
In Vitro
HBV-IN-4 (compound 19f; 0-1 μM; 8 days) treatment inhibits the various forms (relaxed circular [rc] and single-stranded [ss] HBV DNA) in a dose-dependent manner in HepG2.2.15 cells. HBV-IN-4 treatment could also reduce capsidassociated DNAs dose-dependently. HBV-IN-4 could induce the formation of genome-free capsids, including a phenotype of faster-migrating ones[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
HBV-IN-4 (compound 19f) exhibits favorable drug characteristics with low plasma clearance (CL=4.1 mL/min/kg), excellent drug exposure (AUC0-t=49 744 h?ng/L), T1/2 (2.15 hours) and oral bioavailability (F=60.4%) using 20 mg/kg oral administration in mice. HBV-IN-4 also shows good distribution in liver exposure[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c male mice (8-week-old) injected with a recombinant adenoassociated virus (AAV[1]
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Dosage:50 mg/kg, 150 mg/kg
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Administration:Oral administration; twice a day; for 4 weeks
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Result:Resulted in a 2.67 log reduction of the HBV DNA viral load during a 4-week treatment.
Chemical Information
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No. CAS 2305897-84-9
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Appearance Solid
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Peso molecular 479.89
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Fòrmula C24H19ClFN5O3
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Color White to off-white
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SMILES
N#CC1=CC=C(CN(N=C(C2=CC(Cl)=C(NCC(O)CO)N=C2F)C3=C4C=CC=C3)C4=O)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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J Med Virol
Drug Repurposing: In Vitro Evaluation of Simeprevir as a Novel Antiviral Drug Against Severe Fever With Thrombocytopenia Syndrome Virus. [Abstract]2025 Oct;97(10):e70655. PMID: 41117261
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (208.38 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.21 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.21 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0838 mL | 10.4191 mL | 20.8381 mL | 52.0953 mL |
| 5 mM | 0.4168 mL | 2.0838 mL | 4.1676 mL | 10.4191 mL | |
| 10 mM | 0.2084 mL | 1.0419 mL | 2.0838 mL | 5.2095 mL | |
| 15 mM | 0.1389 mL | 0.6946 mL | 1.3892 mL | 3.4730 mL | |
| 20 mM | 0.1042 mL | 0.5210 mL | 1.0419 mL | 2.6048 mL | |
| 25 mM | 0.0834 mL | 0.4168 mL | 0.8335 mL | 2.0838 mL | |
| 30 mM | 0.0695 mL | 0.3473 mL | 0.6946 mL | 1.7365 mL | |
| 40 mM | 0.0521 mL | 0.2605 mL | 0.5210 mL | 1.3024 mL | |
| 50 mM | 0.0417 mL | 0.2084 mL | 0.4168 mL | 1.0419 mL | |
| 60 mM | 0.0347 mL | 0.1737 mL | 0.3473 mL | 0.8683 mL | |
| 80 mM | 0.0260 mL | 0.1302 mL | 0.2605 mL | 0.6512 mL | |
| 100 mM | 0.0208 mL | 0.1042 mL | 0.2084 mL | 0.5210 mL |
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