| Size | Price | Stock | Qty |
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| 2mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 100mg |
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| Other Sizes |
Purity: =97.6%
| Targets |
Bepirovirsen targets all HBV messenger RNAs, leading to reductions in HBV-derived RNAs, HBV DNA, and viral proteins. It is a second-generation 2‘-O-methoxyethyl (2‘-MOE) chimeric antisense oligonucleotide (ASO) with a phosphorothioate (PS) backbone, designed for high nuclease resistance and potency.
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| ln Vitro |
In cellular models of HBV infection (e.g., HepG2.2.15 cells, primary human hepatocytes), Bepirovirsen reduces levels of HBV pregenomic RNA (pgRNA) and subgenomic RNAs, leading to reduced secretion of HBsAg, HBeAg, and other viral proteins. It potently inhibits HBV replication without significant cytotoxicity at effective concentrations.
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| ln Vivo |
In mouse models (e.g., HBV transgenic mice, AAV-HBV mouse models), systemic administration of Bepirovirsen leads to profound and sustained reductions in serum HBV DNA, HBsAg, and HBeAg levels. It has shown superior activity compared to earlier generation ASOs and is well-tolerated. It is currently being evaluated in Phase 3 clinical trials.
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| Enzyme Assay |
Not applicable. Bepirovirsen is an antisense oligonucleotide that binds to complementary sequences on HBV RNAs, activating RNase H-mediated degradation. Target engagement and RNA degradation are measured by direct RNA quantification methods, not by classical cell-free enzyme assays.
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| Cell Assay |
HBV-infected cells (e.g., HepG2.2.15, HepAD38, primary human hepatocytes) are treated with Bepirovirsen (0.1-10 uM) for 3-7 days. Intracellular HBV RNAs (pgRNA and subgenomic RNAs) are quantified by qRT-PCR or Northern blot. Secreted HBsAg and HBeAg levels in culture medium are measured by ELISA. HBV DNA is quantified by qPCR. Cytotoxicity is assessed by MTT.
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| Animal Protocol |
In an AAV-HBV mouse model, Bepirovirsen is administered subcutaneously at doses of 10-50 mg/kg once or twice weekly for 2-4 weeks. Blood is collected weekly for serum HBsAg, HBeAg, and HBV DNA measurement. Mice are euthanized, and liver tissues are collected for analysis of HBV RNA and DNA by qRT-PCR and qPCR, and for histological analysis of inflammation and steatosis.
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| ADME/Pharmacokinetics |
Following subcutaneous administration in animals and humans, Bepirovirsen shows a long elimination half-life (2-4 weeks) due to high nuclease resistance and high protein binding. It is widely distributed, with significant accumulation in the liver. It is cleared slowly. Formulation: saline or PBS. Storage: -80degC for long-term. Avoid freeze-thaw cycles.
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| Toxicity/Toxicokinetics |
In clinical trials, Bepirovirsen has shown a favorable safety profile. The most common adverse events are injection site reactions, mild to moderate flu-like symptoms, and transient ALT flares (likely immune-mediated). Serious adverse events are rare. It has not been approved yet. Standard oligonucleotide safety precautions apply.
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| References |
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| Additional Infomation |
Bepirovirsen (also known as GSK3228836, ISIS 505358) is an investigational drug. It has received Fast Track designation from the FDA and PRIME designation from the EMA for chronic HBV infection. It is currently in Phase 3 clinical trials. Molecular weight: 7344. Sequence: proprietary.
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| CAS # |
1403787-62-1
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| Appearance |
White to off-white solid powder
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
H2O : ≥ 20 mg/mL (~2.72 mM)
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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.) |
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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