Bifendate (Synonyms: DDB)

Name: Bifendate
Brand: MedChemExpress
SKU: HY-W018791
Rating: 5.0 (2 reviews)

Cat. No.: HY-W018791 Pureza: 99.92%: Ficha de datos
COA

SDS
Instrucciones de manejo
FAQs
Technical Support

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).

Para uso exclusivo en investigación. No vendemos a pacientes.

Bifendate Estructura química

No. CAS : 73536-69-3

Tamaño	Stock	Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
100 mg	En stock	Estimated Time of Arrival: December 31
200 mg	Obtener un presupuesto
500 mg	Obtener un presupuesto

or Consulta para venta a granel

* Seleccione Cantidad antes de agregar artículos.

This product is a controlled substance and not for sale in your territory.

Revisión del cliente

Based on 2 publication(s) in Google Scholar

Other Forms of Bifendate:

Bifendate (Standard) Obtener un presupuesto

2 Publications Citing Use of MCE Bifendate

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas Cytochrome P450:

Ver todas las isoformas

CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

Actividad biológica
Pureza y Documentación
Referencias
Revisión del cliente

Descripciòn

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.

Peso molecular

418.35

Fòrmula

C₂₀H₁₈O₁₀

No. CAS

73536-69-3

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

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)

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)

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
10 mM	0.2390 mL	1.1952 mL	2.3903 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.

Calculadora de molaridad
Calculadora de dilución

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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

Animal weight
(per animal)

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.

Pureza y Documentación

Purity: 99.92%

Select Batch:

Ficha de datos (287 KB) SDS (393 KB)

COA (257 KB) LCMS (94 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]

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 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.

Productos vistos recientemente:

Nombre del producto

Requested Quantity *

Nombre del solicitante *

Saludo

Direcciòn del E-mail *

Número de teléfono *

Department

Nombre de la Organizaciòn *

City

Provincia

Country or Region *

Observaciones

Nombre del producto

Lot #

Nombre del solicitante *

Direcciòn del E-mail *

Número de teléfono

Department *

Nombre de la Organizaciòn *

Country or Region *

Observaciones

Name
E-mail *

	Sorry, but the email address you supplied was invalid.

Bifendate (Synonyms: DDB)

Revisión del cliente

Other Forms of Bifendate:

Bifendate Related Antibodies

2 Publications Citing Use of MCE Bifendate

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas Cytochrome P450:

Actividad biológica

Pureza y Documentación

Referencias

Revisión del cliente

Bifendate Related Antibodies

Calculadora de molaridad

Calculadora de dilución

Complete Stock Solution Preparation Table

Bifendate Related Classifications

Keywords:

Productos vistos recientemente:

Revisión del cliente

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report