2. Anti-infection Autophagy Metabolic Enzyme/Protease Membrane Transporter/Ion Channel
  3. HBV Autophagy Cytochrome P450 Atg8/LC3 p62 P-glycoprotein
  4. Bifendate

Bifendate (DDB), extracted from Schisandrae chinensis, is an orally active anti-HBV agent against chronic hepatitis B. Bifendate inhibits ATG5-dependent autophagy and attenuates oleic acid-induced lipid accumulation with anti-oxidant properties in vitro. Bifendate can decrease alanine transaminase (ALT) level in mice. Bifendate attenuates hepatic steatosis in cholesterol/bile salt- and high-fat diet-induced hypercholesterolemia in mice. Bifendate potently increases the activity of cytochrome proteins (CYPs) and reverse P-gp-mediated multi-drug resistance (MDR).

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Bifendate Chemical Structure

Bifendate Chemical Structure

CAS No. : 73536-69-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 61 In-stock
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10 mM * 1 mL in DMSO USD 61 In-stock
Solid
100 mg USD 55 In-stock
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Based on 1 publication(s) in Google Scholar

Bifendate Related Antibodies

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

  • Biological Activity

  • Purity & Documentation

  • References

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Description

Bifendate (DDB), extracted from Schisandrae chinensis, is an orally active anti-HBV agent against chronic hepatitis B. Bifendate inhibits ATG5-dependent autophagy and attenuates oleic acid-induced lipid accumulation with anti-oxidant properties in vitro. Bifendate can decrease alanine transaminase (ALT) level in mice. Bifendate attenuates hepatic steatosis in cholesterol/bile salt- and high-fat diet-induced hypercholesterolemia in mice. Bifendate potently increases the activity of cytochrome proteins (CYPs) and reverse P-gp-mediated multi-drug resistance (MDR)[1][2][3][4][5][6].

In Vitro

Bifendate (0-50 μM, 12 h) inhibits autophagy degradation in a ATG5-dependent manner and inhibits lysosomal activity in Hela cells and MEFs[2].
Bifendate (50 μM, 12 h) attenuates oleic acid (OA)-induced lipid droplet accumulation which is consistent with reduced autophagy activity and lysosome acidity in HepG2 cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Bifendate Related Antibodies

Cell Autophagy Assay[2]

Cell Line: Hela cells and MEFs
Concentration: 0-50 μM
Incubation Time: 12 h
Result: Significantly increased LC3-II expression and enhanced p62 expression, which is dependent on ATG5 in Hela cells.

Western Blot Analysis[2]

Cell Line: Hela cells
Concentration: 50 μM
Incubation Time: 12 h
Result: Significantly reduced the mCTSD level and led to the accumulation of LC3-II and p62 combined with Torin2 (HY-13002) in Hela cells.

Immunofluorescence[2]

Cell Line: HepG2 cells
Concentration: 50 μM
Incubation Time: 12 h
Result: Protected cells from OA-induced cell death, decreased the number of OA-induced intracellular lipid droplets and inhibited the increased lysosomal acid-ity caused by OA in HepG2 cells.
In Vivo


Pharmacokinetic parameters of Bifendate (12 mg/kg, p.o., pills, the liquid SEDDS and the SEP) in rats (SEDDS: self-emulsifying drug delivery system; SEP: self-emulsifying pellet)[3]

Parameters Cmax (μg/mL) Tmax (h) AUC0-12 h (μg/mL)·h MRT (h) F0-12 h(%)
Bifendate pills 0.46±0.074 1.5±0.17 1322.29±421.85 3.43±0.74
The liquid SEDDS 0.98±0.101 0.75±0.11 3272.73±304.49 3.77±0.46 247.51±26.23
The SEP 0.83±0.215 2.0±0.12 3122.85±289.27 3.39±0.21 236.17±58.12
Bifendate (12 mg/kg, oral gavage, a single dose) from the liquid SEDDS and the SEP significantly increases oral bioavailability than that from pills in rats[3].
Bifendate (0.03-0.3 g/kg, i.g., daily from day 6 to day 9) attenuates hepatic steatosis in cholesterol/bile salt- and high-fat diet-induced hypercholesterolemia in mice[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Cholesterol/bile salt-induced hypercholesterolemic mice[4]
Dosage: 0.03-0.3 g/kg
Administration: i.g., daily from day 6 to day 9
Result: Dose-dependently decreased the hepatic total cholesterol (20-35%) and triglyceride (13–37%) levels in hypercholesterolemic mice.
Animal Model: Male Sprague Dawley rats (body weight 200-250 g)[3]
Dosage: 12 mg/kg
Administration: oral gavage, a single dose
Result: Was released quickly and completely from the liquid SEDDS and the SEP in the 0.1N HCl solution, whereas incompletely released from pills in rats.
Molecular Weight

418.35

Formula

C20H18O10
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C2=C(OC)C1=C(OCO1)C(=C2C(OC)=O)C3=C(C=C(OC)C4=C3OCO4)C(OC)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 12.5 mg/mL (29.88 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 1 mg/mL (2.39 mM; ultrasonic and warming and heat to 80°C)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.25 mg/mL (2.99 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 1.25 mg/mL (2.99 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.91%

COA (257 KB) HNMR (186 KB) RP-HPLC (193 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.3903 mL 11.9517 mL 23.9034 mL 59.7586 mL
DMSO 5 mM 0.4781 mL 2.3903 mL 4.7807 mL 11.9517 mL
10 mM 0.2390 mL 1.1952 mL 2.3903 mL 5.9759 mL
15 mM 0.1594 mL 0.7968 mL 1.5936 mL 3.9839 mL
20 mM 0.1195 mL 0.5976 mL 1.1952 mL 2.9879 mL
25 mM 0.0956 mL 0.4781 mL 0.9561 mL 2.3903 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Bifendate Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Bifendate73536-69-3DDBHBVAutophagyCytochrome P450Atg8/LC3p62P-glycoproteinHepatitis B virusCYPsAutophagy-related 8Sequestosome-1SQSTM1P-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Schisandrin Cchronic hepatitis Banti-HBVautophagylipid accumulationanti-oxidantALTMDRInhibitorinhibitorinhibit

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