| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Bifendate targets the autophagy pathway and lysosomal function. It reduces lysosomal function and prevents autophagosome-lysosome fusion induced by the mTOR inhibitor Torin 2. The compound also has antioxidant effects and reduces lipid accumulation. As a synthetic intermediate of schisandrin C, bifendate may share some of the biological activities of this traditional medicine constituent. Its hepatoprotective effects are attributed to its ability to reduce alanine aminotransferase (ALT) levels and improve hepatic steatosis. Bifendate also has the ability to reverse multidrug resistance.
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| ln Vitro |
In vitro, bifendate exhibits diverse biological activities. It reduces lysosomal function and prevents autophagosome-lysosome fusion induced by the mTOR inhibitor Torin 2. The compound has antioxidant effects and reduces lipid accumulation. Bifendate improves hepatic steatosis and reduces alanine aminotransferase (ALT) levels. It also has the ability to reverse multidrug resistance. In cell-based assays, bifendate treatment results in reduced lipid accumulation and improved cellular antioxidant capacity. The compound's effects on autophagy and lysosomal function make it a valuable tool for studying these cellular processes.
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| ln Vivo |
In vivo, bifendate has been used as an anti-HBV drug in the treatment of chronic hepatitis B. It has also been used as a hepatoprotectant adjuvant in the treatment of liver diseases, such as chronic viral hepatitis or drug-induced hepatic damage. Bifendate improves hepatic steatosis and reduces ALT levels. The compound's hepatoprotective effects are well-documented in clinical use in some countries. It is used as a therapeutic agent for liver diseases, including hepatitis and cirrhosis. Further clinical studies are ongoing.
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| Enzyme Assay |
In vitro enzyme assays for bifendate are not extensively documented, as the compound's primary mechanism involves autophagy and lysosomal function rather than direct enzyme inhibition. However, its antioxidant activity can be assessed using assays that measure free radical scavenging or inhibition of lipid peroxidation. The compound's effects on lysosomal function can be assessed using lysosomal activity assays with fluorescent substrates. These assays provide insights into the compound's mechanisms of action.
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| Cell Assay |
In vitro cell-based assays for bifendate evaluate its effects on autophagy, lysosomal function, and lipid metabolism. Cells are cultured and treated with bifendate, and autophagosome-lysosome fusion is assessed using fluorescent markers such as LC3 and LAMP1. Lipid accumulation is assessed using Oil Red O staining or by measuring triglyceride levels. Antioxidant activity is assessed by measuring reactive oxygen species (ROS) production. Cell viability is assessed using MTT or LDH release assays. These assays confirm the compound's cellular activities.
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| Animal Protocol |
In vivo animal experiments for bifendate have been conducted in models of liver disease. The compound has been shown to improve hepatic steatosis and reduce ALT levels. Bifendate has been used in the treatment of chronic hepatitis B and as a hepatoprotectant adjuvant. Animal studies have demonstrated the compound's efficacy in reducing liver damage and improving liver function. Comprehensive pharmacokinetic and toxicological studies have been conducted in the context of its clinical use.
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| ADME/Pharmacokinetics |
Metabolism / Metabolites
The known metabolites of bifendate include methyl 4-(2,3-dihydroxy-4-methoxy-6-methoxycarbonylphenyl)-7-methoxy-1,3-benzodioxane-5-carboxylate and mono-O-demethylated bdd. Pharmacokinetic (PK) data for bifendate are available from clinical studies. The compound has a molecular weight of 418.40 g/mol and is a synthetic intermediate of schisandrin C. It is typically administered orally and is metabolized in the liver. The compound's half-life, bioavailability, and excretion profile have been characterized in the context of its clinical use for hepatitis B treatment. Comprehensive PK data are available from pharmaceutical studies. |
| Toxicity/Toxicokinetics |
The toxicity profile of bifendate has been evaluated in clinical and preclinical studies. The compound is generally well-tolerated at therapeutic doses. It has been used as a therapeutic agent for liver diseases. Common side effects are mild and transient. The compound should be used under medical supervision. Comprehensive toxicological studies are available from clinical use and pharmaceutical development.
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| References | |
| Additional Infomation |
Bifendate (DDB, dimethyl diphenyl bicarboxylate) is a synthetic intermediate of schisandrin C and an anti-HBV drug used in the treatment of chronic hepatitis B. It has a molecular formula of C₂₀H₁₈O₁₀ and a molecular weight of 418.40 g/mol. Bifendate reduces lysosomal function and prevents autophagosome-lysosome fusion. It has antioxidant effects, reduces lipid accumulation, and improves hepatic steatosis. Bifendate is used as a hepatoprotectant adjuvant in the treatment of liver diseases.
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| Molecular Formula |
C20H18O10
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| Molecular Weight |
418.3509
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| Exact Mass |
418.089
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| CAS # |
73536-69-3
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| PubChem CID |
108213
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
606.9±55.0 °C at 760 mmHg
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| Melting Point |
181 °C
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| Flash Point |
265.9±31.5 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.580
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| LogP |
2.23
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
30
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| Complexity |
587
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JMZOMFYRADAWOG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H18O10/c1-23-11-5-9(19(21)25-3)13(17-15(11)27-7-29-17)14-10(20(22)26-4)6-12(24-2)16-18(14)30-8-28-16/h5-6H,7-8H2,1-4H3
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| Chemical Name |
methyl 7-methoxy-4-(7-methoxy-5-methoxycarbonyl-1,3-benzodioxol-4-yl)-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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), 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) |
DMSO : ~12.5 mg/mL (~29.88 mM)
H2O : ~1 mg/mL (~2.39 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.99 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 12.5 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: ≥ 1.25 mg/mL (2.99 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 12.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3903 mL | 11.9517 mL | 23.9034 mL | |
| 5 mM | 0.4781 mL | 2.3903 mL | 4.7807 mL | |
| 10 mM | 0.2390 mL | 1.1952 mL | 2.3903 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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