| Size | Price | Stock | Qty |
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| 1mg |
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| 10mg |
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| Targets |
DVR-01 targets the hepatitis B virus (HBV) capsid, a protein shell that encapsulates the viral pregenomic RNA (pgRNA) and polymerase. By binding to the capsid protein, DVR-01 disrupts the proper assembly of the capsid, preventing the encapsidation of pgRNA. This blocks the formation of new infectious viral particles. The compound's activity against drug-resistant mutants indicates it may bind to a conserved site on the capsid protein.
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| ln Vitro |
In human hepatoma cells, DVR-01 (0-10 μM; 4 d) suppresses HBV with EC50 values of 1.7 and 1.6 μM in AML12HBV10 and HepDES19 cells, respectively [1]. DVR-01 (0.156-10 μM; 2 d) specifically impedes the encapsidation of HBV pgRNA [1]. In human hepatoma cells, DVR-01 (3 d) has antiviral activity against hepatitis viruses, with EC50s of 2.899, >10, and >25 μM against HBV, WHV, and DHBV, respectively [1]. Against drug-resistant HBV mutations, DVR-01 (0.0097-10 μM; 2 d) demonstrated antiviral efficacy with EC50 values of 2.899, 3.273, 3.180, 2.752, and 2.567 for wt, rtL180 M/rtM204V, rtA181V, rtN236T, rtM2, and 2.403 μM 04I and rtL180 M/rtM204V/rtT184G/rtS202I, respectively[1].
In vitro, DVR-01 inhibits HBV replication in human hepatoma cells. It has EC50 values of 1.7 μM and 1.6 μM in AML12HBV10 and HepDES19 cells, respectively. It also shows antiviral activity against drug-resistant HBV mutants with EC50 values of 2.403-3.273 μM. DVR-01 (0.156-10 μM; 2 days) selectively disrupts the pgRNA encapsidation by HBV. |
| ln Vivo |
In vivo, DVR-01 can be used for the research of HBV infection and related diseases. As a capsid inhibitor, it has the potential to reduce viral load in animal models of chronic HBV infection. However, detailed in vivo efficacy data is limited in publicly available sources. The compound is primarily used as a research tool.
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| Enzyme Assay |
In vitro antiviral assays for DVR-01 are performed using human hepatoma cell lines (e.g., AML12HBV10, HepDES19) that stably replicate HBV. Cells are treated with various concentrations of DVR-01 for 4 days. HBV replication is assessed by measuring the levels of extracellular HBV DNA, HBeAg, or HBsAg in the culture supernatant by qPCR or ELISA. EC50 values are calculated from dose-response curves. Cytotoxicity is assessed using MTT or ATP-lite assays to determine CC50 values.
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| Cell Assay |
Cellular assays for DVR-01 involve studying its effect on HBV capsid assembly. Cells are treated with DVR-01, and the encapsidation of pgRNA is assessed by measuring the amount of pgRNA associated with capsids using native agarose gel electrophoresis or by qPCR after capsid immunoprecipitation. The selectivity of the compound for disrupting encapsidation over other steps of the viral life cycle can be determined.
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| Animal Protocol |
In vivo animal studies for DVR-01 would utilize mouse models of HBV infection, such as hydrodynamic injection models or humanized liver chimeric mice. The compound would be administered orally or intraperitoneally. Viral load in the serum would be measured by qPCR. Efficacy would be compared to vehicle and reference antivirals (e.g., entecavir, tenofovir).
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| ADME/Pharmacokinetics |
DVR-01 has a molecular weight of 406.11 g/mol and a molecular formula of C20H23ClN2O3S. It is a solid at room temperature. It is typically stored as a powder at -20°C. It is soluble in DMSO. Pharmacokinetic properties such as oral bioavailability and half-life would be determined in preclinical studies. The compound is a small molecule HBV capsid inhibitor.
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| Toxicity/Toxicokinetics |
Preclinical toxicity of DVR-01 would be evaluated in standard toxicology studies. As a capsid inhibitor targeting a viral protein, it is expected to have a favorable selectivity profile. However, comprehensive toxicity data is not available in public databases. The compound is for research use only and is not approved for clinical use.
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| References | |
| Additional Infomation |
DVR-01 is a potent HBV capsid inhibitor. It has EC50 values of 1.7 μM and 1.6 μM in AML12HBV10 and HepDES19 cells, respectively. It shows activity against drug-resistant HBV mutants. It is a research compound for studying HBV infection.
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| Molecular Formula |
C20H23CLN2O3S
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|---|---|
| Molecular Weight |
406.93
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| Exact Mass |
406.111
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| CAS # |
330461-34-2
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| PubChem CID |
1079083
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
3.7
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
579
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CCCN(CC1)S(=O)(=O)C2=C(C=CC(=C2)C(=O)NCC3=CC=CC=C3)Cl
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| InChi Key |
PBAWFYZFSXYUOS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H23ClN2O3S/c21-18-11-10-17(20(24)22-15-16-8-4-3-5-9-16)14-19(18)27(25,26)23-12-6-1-2-7-13-23/h3-5,8-11,14H,1-2,6-7,12-13,15H2,(H,22,24)
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| Chemical Name |
3-(azepan-1-ylsulfonyl)-N-benzyl-4-chlorobenzamide
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| Synonyms |
DVR01; DVR 01; DVR-01
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4574 mL | 12.2871 mL | 24.5743 mL | |
| 5 mM | 0.4915 mL | 2.4574 mL | 4.9149 mL | |
| 10 mM | 0.2457 mL | 1.2287 mL | 2.4574 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.
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