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  3. Bilobetin

Bilobetin, an active component of Ginkgo biloba, can reduce blood lipids and improve the effects of insulin. Bilobetin ameliorated insulin resistance, increased the hepatic uptake and oxidation of lipids, reduced very-low-density lipoprotein triglyceride secretion and blood triglyceride levels, enhanced the expression and activity of enzymes involved in β-oxidation and attenuated the accumulation of triglycerides and their metabolites in tissues. Bilobetin also increased the phosphorylation, nuclear translocation and activity of PPARα accompanied by elevated cAMP level and PKA activity.

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Bilobetin Chemical Structure

Bilobetin Chemical Structure

CAS No. : 521-32-4

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5 mg USD 180 In-stock
10 mg USD 320 In-stock
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Based on 1 publication(s) in Google Scholar

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1 Publications Citing Use of MCE Bilobetin

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Bilobetin, an active component of Ginkgo biloba, can reduce blood lipids and improve the effects of insulin. Bilobetin ameliorated insulin resistance, increased the hepatic uptake and oxidation of lipids, reduced very-low-density lipoprotein triglyceride secretion and blood triglyceride levels, enhanced the expression and activity of enzymes involved in β-oxidation and attenuated the accumulation of triglycerides and their metabolites in tissues. Bilobetin also increased the phosphorylation, nuclear translocation and activity of PPARα accompanied by elevated cAMP level and PKA activity[1].

IC50 & Target[1]

PPARα

 

PKA

 

In Vitro

Bilobetin (0-40 μM, 24/48/72 h) inhibits the cell proliferation in Huh7 and HepG2 cells[4].
Bilobetin (0-20 μM, 24 and 48 h) induces apoptosis and increases sub G1 population in Huh7 and HepG2 cells[4].
Bilobetin (0-20 μM, 24 h) induces accumulation of ROS and DNA damage in Huh7 and HepG2 cells[4].
Bilobetin (1-2 μM, 1 days) inhibits the phosphorylation of AKT in sebocytes[5].

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

Cell Viability Assay[4]

Cell Line: Huh7 and HepG2 cells
Concentration: 0, 2.5, 5, 10, 20, and 40 μM
Incubation Time: 24/48/72 h
Result: Inhibited cell proliferation in a dose dependent manner, with IC50s of 18.28 μM at 48 h in Huh7 cells, and 19 μM at 72 h in HepG2 cells.

Apoptosis Analysis[4]

Cell Line: Huh7 and HepG2 cells
Concentration: 0, 2.5, 5, 10, 20 μM
Incubation Time: 24/48 h
Result: Showed the total apoptotic cell rate of 2.2, 2.2, 1.9, and 10.6% for 24 h (Huh7 cells) at 0, 5, 10, and 20 μM, and 1.7, 1.5, 7.5, and 22.5% for 48 h (Huh7 cells) at 0, 5, 10, and 20 μM.
Showed the total apoptotic cell rate of 1.1, 1.2, 1.6, and 3.0% for 24 h (Huh7 cells) at 0, 5, 10, and 20 μM, and 1.5, 1.1, 3.2, and 14.2% for 48 h (Huh7 cells) at 0, 5, 10, and 20 μM, respectively.
In Vivo

Bilobetin (i.p., 12 mg/kg/day, 4 or 14 days) ameliorates hyperlipidaemia, lipotoxicity and insulin resistance by PKA-mediated phosphorylation of PPARα in rats fed a high-fat diet[1].
Bilobetin (i.p., 50 mg/kg, for 7 days) induces kidney injury in rats, and promotes the trafficking of AQP-2 onto the plasma membrane in rats[2].
Bilobetin (6 and 12 mg/kg, i.p., daily for ten days.) shows protective effects against Cisplatin (HY-17394) (7 mg/kg, i.p., a single dose on the third day)-induced testicular toxicity in rats[3].

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

Animal Model: rats fed a high-fat diet[1]
Dosage: 12 mg/kg/day
Administration: i.p., 4 or 14 days after mice were fed a HFD for 8 weeks.
Result: Increased glucose infusion rate (GIR, P < 0.05) and reduced EGP (P < 0.05) in basal and clamp states.
Reduced total TG (P < 0.01) and VLDL-TG (P < 0.01).
Enhances hepatic Intralipid-TG uptake.
Reduced the total amount of lipid level in the liver and muscle.
Promoted the phosphorylation of PPARα and the translocation of PPARα from the cytoplasm to the nucleus in rats liver.
Molecular Weight

552.48

Formula

C31H20O10

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C=C(C2=CC=C(O)C=C2)OC3=C(C4=CC(C5=CC(C6=C(O)C=C(O)C=C6O5)=O)=CC=C4OC)C(O)=CC(O)=C13

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

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

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (452.51 mM; Need ultrasonic; 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 1.8100 mL 9.0501 mL 18.1002 mL
5 mM 0.3620 mL 1.8100 mL 3.6200 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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    90% (20% SBE-β-CD in Saline)

    Solubility: 2.08 mg/mL (3.76 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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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)

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: 99.39%

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). 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
DMSO 1 mM 1.8100 mL 9.0501 mL 18.1002 mL 45.2505 mL
5 mM 0.3620 mL 1.8100 mL 3.6200 mL 9.0501 mL
10 mM 0.1810 mL 0.9050 mL 1.8100 mL 4.5251 mL
15 mM 0.1207 mL 0.6033 mL 1.2067 mL 3.0167 mL
20 mM 0.0905 mL 0.4525 mL 0.9050 mL 2.2625 mL
25 mM 0.0724 mL 0.3620 mL 0.7240 mL 1.8100 mL
30 mM 0.0603 mL 0.3017 mL 0.6033 mL 1.5084 mL
40 mM 0.0453 mL 0.2263 mL 0.4525 mL 1.1313 mL
50 mM 0.0362 mL 0.1810 mL 0.3620 mL 0.9050 mL
60 mM 0.0302 mL 0.1508 mL 0.3017 mL 0.7542 mL
80 mM 0.0226 mL 0.1131 mL 0.2263 mL 0.5656 mL
100 mM 0.0181 mL 0.0905 mL 0.1810 mL 0.4525 mL
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  • 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.

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Bilobetin
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