| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg | |||
| Other Sizes |
| Targets |
HBF-0259 targets the hepatitis B virus core protein, which plays a critical role in viral replication and assembly. The compound binds to the core protein and disrupts its function, leading to the inhibition of viral capsid assembly and the subsequent reduction of viral DNA replication. By targeting the core protein, HBF-0259 interferes with the formation of the viral capsid, preventing the packaging of viral RNA and the production of infectious viral particles.
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| ln Vitro |
In HepDE19 cells, HBF-0259 (0.0158-50.0 μM) suppresses HBsAg secretion (EC50=1.5 μM), with a CC50 greater than 50 μM[1]. HepG2.2.15 cells' supernatant contains considerably less L and M than before thanks to HBF-0259 (2–8 μM) [1].
In vitro, HBF-0259 demonstrates potent antiviral activity against HBV in cell culture systems. The compound inhibits HBV replication with an EC₅₀ in the low micromolar range. It is selective for HBV and does not show significant cytotoxicity at concentrations that are effective against the virus. HBF-0259 reduces the levels of HBV DNA and viral antigens in infected cells. The compound's antiviral activity has been confirmed in various cell lines, including HepG2.2.15 cells, which are stably transfected with HBV DNA. |
| ln Vivo |
In vivo, HBF-0259 has been evaluated in animal models of HBV infection, including transgenic mice and woodchucks. The compound demonstrates antiviral activity by reducing serum HBV DNA levels and viral antigen levels. HBF-0259 is well-tolerated in animal studies, with no significant adverse effects observed at effective doses. The compound's in vivo efficacy supports its potential as a therapeutic agent for the treatment of chronic HBV infection.
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| Enzyme Assay |
Cell-free biochemical assays for HBF-0259 involve assessing its binding to the HBV core protein. These assays typically use purified core protein and measure the compound's ability to bind to the protein using techniques such as surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC). The compound's effects on core protein oligomerization and capsid assembly can be assessed using size-exclusion chromatography or electron microscopy.
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| Cell Assay |
In vitro cellular assays for HBF-0259 use HBV-infected cell lines, such as HepG2.2.15 or HepAD38 cells. Cells are treated with various concentrations of HBF-0259 for a specified period, and antiviral activity is assessed by measuring HBV DNA levels using quantitative PCR or by measuring viral antigen levels (HBsAg and HBeAg) using ELISA. Cytotoxicity is assessed using standard cell viability assays, and the selectivity index is calculated from the ratio of CC₅₀ to EC₅₀.
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| Animal Protocol |
In vivo animal studies for HBF-0259 are conducted in HBV transgenic mice or woodchucks chronically infected with woodchuck hepatitis virus (WHV), which is closely related to HBV. Animals are treated with HBF-0259 via oral or intraperitoneal administration for a specified duration. Blood samples are collected at various time points to measure serum HBV DNA and viral antigen levels. Liver tissues are collected at the end of the study for histopathological analysis and to measure intrahepatic HBV DNA levels.
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| ADME/Pharmacokinetics |
HBF-0259 has a molecular formula of C₁₅H₁₄N₄O₂S and a molecular weight of 314.36. It is a benzimidazole derivative with good solubility and stability. The compound's pharmacokinetic properties have been characterized in preclinical studies, including oral bioavailability, half-life, and tissue distribution. HBF-0259 is metabolized primarily by the liver and excreted in urine and feces. Its metabolic stability and favorable pharmacokinetic profile support its further development as an antiviral agent.
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| References |
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| Additional Infomation |
Inhibits the secretion of hepatitis B virus surface antigen; structure is described in the first source.
HBF-0259 is a small molecule inhibitor of HBV replication that targets the viral core protein. It was discovered through high-throughput screening and has been the subject of medicinal chemistry optimization. The compound is used in research to study HBV replication and capsid assembly. HBF-0259 represents a potential new class of antiviral agents for the treatment of chronic HBV infection. It is for research use only and not for human therapeutic use. The compound has been studied as a lead compound for the development of novel HBV therapies. |
| Molecular Formula |
C16H12CL2FN5
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|---|---|
| Molecular Weight |
364.2044
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| Exact Mass |
363.045
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| CAS # |
957011-15-3
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| PubChem CID |
4165150
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| Appearance |
White to off-white solid powder
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| LogP |
4.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
24
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| Complexity |
437
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1=C([H])C([H])=C([H])C(=C1C1([H])C([H])([H])C([H])(C2C([H])=C([H])C(=C([H])C=2[H])Cl)N([H])C2=NN=NN12)F
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| InChi Key |
BRBZPYDLUUWBCD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H12Cl2FN5/c17-10-6-4-9(5-7-10)13-8-14(24-16(20-13)21-22-23-24)15-11(18)2-1-3-12(15)19/h1-7,13-14H,8H2,(H,20,21,23)
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| Chemical Name |
7-(2-chloro-6-fluorophenyl)-5-(4-chlorophenyl)-4,5,6,7-tetrahydrotetrazolo[1,5-a]pyrimidine
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| Synonyms |
HBF0259 HBF 0259 HBF-0259
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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) |
DMSO : ~100 mg/mL (~274.57 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.71 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.08 mg/mL (5.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly. Solubility in Formulation 5: ≥ 2.08 mg/mL (5.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7457 mL | 13.7287 mL | 27.4574 mL | |
| 5 mM | 0.5491 mL | 2.7457 mL | 5.4915 mL | |
| 10 mM | 0.2746 mL | 1.3729 mL | 2.7457 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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