| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Bicyclol does not have a single well-defined target. It is a hepatoprotective agent with antiviral activity. It has been shown to have antiviral activity against hepatitis B, reducing viral DNA and the secretion of HBsAg and HBeAg. Its mechanism of action may involve protection of hepatocytes and modulation of immune responses.
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|---|---|
| ln Vitro |
In vitro, bicyclol has antiviral activity against hepatitis B, reducing viral DNA and the secretion of the HBV antigens HBsAg and HBeAg by 59 and 35%, respectively, in infected 2.2.15 HepG2 cells. It is also effective against hepatitis C. These activities demonstrate its antiviral and hepatoprotective effects.
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| ln Vivo |
In vivo, bicyclol is used for the treatment of chronic liver diseases, including viral hepatitis and drug-induced liver injury. It is a hepatoprotective agent used in China for chronic hepatitis B and presumably C. Its clinical efficacy has been established in numerous studies.
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| Enzyme Assay |
The in vitro antiviral assay for bicyclol measures its ability to inhibit hepatitis B virus replication. These assays use HBV-infected cell lines, such as 2.2.15 HepG2 cells, and measure viral DNA and antigen levels. The compound's antiviral potency is determined by measuring the reduction in these parameters.
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| Cell Assay |
In vitro cellular assays for bicyclol assess its hepatoprotective and antiviral effects. Hepatocytes are treated with bicyclol and then exposed to viral infection or hepatotoxic agents. Cell viability, viral replication, and markers of liver injury are measured. These assays demonstrate the compound's functional activity in a relevant cellular context.
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| Animal Protocol |
In vivo animal studies for bicyclol have been conducted in animal models of liver injury and viral hepatitis to evaluate its efficacy. However, its clinical efficacy has been established in human use for chronic liver diseases.
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| ADME/Pharmacokinetics |
Bicyclol is orally bioavailable. It is administered orally and is well-absorbed. It is metabolized in the liver and excreted in bile and urine. Its pharmacokinetic properties support its use as an oral therapeutic agent.
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| Toxicity/Toxicokinetics |
Bicyclol is generally well-tolerated. Common adverse effects are mild and may include gastrointestinal disturbances. Its safety profile has been established through clinical use in China.
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| References | |
| Additional Infomation |
Bicyclol is currently being investigated in the clinical trial NCT02944552 (a multicenter, randomized, double-blind, positive-controlled study of bicyclol for the treatment of acute drug-induced liver injury). It has been reported that bicyclol is found in Aspergillus flavus and Isatis indigotica, and relevant data are available for reference.
Bicyclol is a hepatoprotective agent used for the treatment of chronic liver diseases, including viral hepatitis and drug-induced liver injury. It has antiviral activity against hepatitis B and C. It is used in China for chronic hepatitis B and presumably C. It is available as a prescription medication in some countries. |
| Molecular Formula |
C19H18O9
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|---|---|
| Molecular Weight |
390.34082
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| Exact Mass |
390.095
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| CAS # |
118159-48-1
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| PubChem CID |
9821754
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| Appearance |
White to off-white solid powder
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| LogP |
2.107
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
28
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| Complexity |
558
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
KXMTXZACPVCDMH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H18O9/c1-22-11-4-9(6-20)13(17-15(11)25-7-27-17)14-10(19(21)24-3)5-12(23-2)16-18(14)28-8-26-16/h4-5,20H,6-8H2,1-3H3
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| Chemical Name |
methyl 4-[5-(hydroxymethyl)-7-methoxy-1,3-benzodioxol-4-yl]-7-methoxy-1,3-benzodioxole-5-carboxylate
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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 (~256.19 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.40 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 25.0 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: 2.5 mg/mL (6.40 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5619 mL | 12.8093 mL | 25.6187 mL | |
| 5 mM | 0.5124 mL | 2.5619 mL | 5.1237 mL | |
| 10 mM | 0.2562 mL | 1.2809 mL | 2.5619 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05711459 | Recruiting | Drug: Bicyclol tablets | Drug-Induced Acute Liver Injury | Tianjin Medical University Cancer Institute and Hospital | 2022-05-01 | Not Applicable |
| NCT02944552 | Completed | Drug: bicyclol tablet 25mg Drug: bicyclol tablet 50mg Drug: polyene phosphatidylcholine capsule 456mg |
Drug-Induced Acute Liver Injury | Drug Induced Liver Disease Study Group | 2017-08-18 | Phase 2 |
| NCT03680183 | Unknown status | Drug: Entecavir 1Mg Oral Tablet | Hepatitis B Non Small Cell Lung Cancer |
Affiliated Cancer Hospital & Institute of Guangzhou Medical University |
2018-05-22 | |
| NCT05063500 | Unknown status | Drug: bicyclol, 25mg/ tablet Drug: polyene phosphatidylcholine capsules, 228mg/ particle. |
Drug-Induced Acute Liver Injury | Drug Induced Liver Disease Study Group | 2021-12-20 | Phase 3 |
| NCT02961413 | Unknown status | Drug-induced Liver Injury | Drug Induced Liver Disease Study Group | 2016-04 |
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