Referencia número: HY-W018791

Bifendate

(Synonyms: DDB)

2 Cited Publications

Revisión del cliente

Based on 2 publication(s) in Google Scholar

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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Pureza: 99.92%
No. CAS: 73536-69-3
Fòrmula: C₂₀H₁₈O₁₀
Peso molecular:418.35

Almacenamiento:

4°C, protect from light, stored under nitrogen

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

Bifendate Chemical Structure

No. CAS: 73536-69-3

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Actividad biológica
- Descripciòn
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

Ver todos los productos específicos de isoformas Cytochrome P450 :

Cellular Effect

Cell Line	Type	Value	Description	References
K562	IC₅₀	>100 μM Compound: Bifendate	Cytotoxicity against human K562 cells after 72 hrs by MTS assay Cytotoxicity against human K562 cells after 72 hrs by MTS assay	[PMID: 22429509]
K562	IC₅₀	>200 μM Compound: Bifendate	Anti-proliferative activity against human K562 cells measured after 72 hrs by MTS assay Anti-proliferative activity against human K562 cells measured after 72 hrs by MTS assay	[PMID: 28068095]
K562/A02	IC₅₀	>100 μM Compound: Bifendate	Cytotoxicity against human K562/A02 cells overexpress P-gp after 72 hrs by MTS assay Cytotoxicity against human K562/A02 cells overexpress P-gp after 72 hrs by MTS assay	[PMID: 22429509]
K562/A02	IC₅₀	>200 μM Compound: Bifendate	Anti-proliferative activity against P-gp overexpressing/drug resistant human K562/A02 cells measured after 72 hrs by MTS assay Anti-proliferative activity against P-gp overexpressing/drug resistant human K562/A02 cells measured after 72 hrs by MTS assay	[PMID: 28068095]

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.

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	C_max (μg/mL)	T_max (h)	AUC_{0-12 h} (μg/mL)·h	MRT (h)	F_{0-12 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.

Chemical Information

No. CAS 73536-69-3
Appearance Solid
Peso molecular 418.35
Fòrmula C₂₀H₁₈O₁₀
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
Synonyms

DDB
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

4°C, protect from light, stored under nitrogen

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

Publications (2)

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Journal Impact Factor

J Ethnopharmacol

Sesquiterpene lactones from Cichorium intybus exhibit potent anti-inflammatory and hepatoprotective effects by repression of NF-κB and enhancement of NRF2. [Abstract]

2025 Feb 2:119439. PMID: 39904423
Vet Microbiol

The Chinese medicine monomer Schisandrin C inhibits PRRSV infection by regulating the OGT-PI3K/AKT/mTOR signaling pathway. [Abstract]

2026 May:316:110992. PMID: 41865607

Solvente y solubilidad

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (287 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Cui S, et al. [Anti-HBV efficacy of bifendate in treatment of chronic hepatitis B, a primary study]. Zhonghua Yi Xue Za Zhi. 2002 Apr 25;82(8):538-40. [Content Brief]

[2]. Yuan W, et al. Bifendate inhibits autophagy at multiple steps and attenuates oleic acid-induced lipid accumulation. Biochem Biophys Res Commun. 2022 Nov 26;631:115-123. [Content Brief]

[3]. Xiao Y, et al. Self-emulsifying bifendate pellets: preparation, characterization and oral bioavailability in rats. Drug Dev Ind Pharm. 2013 May;39(5):724-32. [Content Brief]

[4]. Pan SY, et al. Bifendate treatment attenuates hepatic steatosis in cholesterol/bile salt- and high-fat diet-induced hypercholesterolemia in mice. Eur J Pharmacol. 2006 Dec 15;552(1-3):170-5. [Content Brief]

[5]. Yue S, et al. Hepatoprotective Effect of Apigenin Against Liver Injury via the Non-canonical NF-κB Pathway In Vivo and In Vitro. Inflammation. 2020 Oct;43(5):1634-1648. [Content Brief]

[6]. Zeng Y, et al. Effect of bifendate on the pharmacokinetics of cyclosporine in relation to the CYP3A4*18B genotype in healthy subjects. Acta Pharmacol Sin. 2009 Apr;30(4):478-84. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3903 mL	11.9517 mL	23.9034 mL	59.7586 mL
	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

Bifendate

2 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) Bifendate

Ver todos los productos específicos de isoformas Cytochrome P450

Actividad biológica

Chemical Information

Publications (2)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Bifendate Related Classifications

HY-W018791 Related Classifications