2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Immunology/Inflammation NF-κB Apoptosis Autophagy
  3. RAR/RXR Reactive Oxygen Species Apoptosis Autophagy
  4. Bigelovin

Bigelovin, a sesquiterpene lactone isolated from Inula hupehensis, is a selective retinoid X receptor α agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation.

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Bigelovin Chemical Structure

Bigelovin Chemical Structure

CAS No. : 3668-14-2

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5 mg USD 280 In-stock
10 mg USD 370 In-stock
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Based on 1 publication(s) in Google Scholar

Bigelovin Related Antibodies

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Description

Bigelovin, a sesquiterpene lactone isolated from Inula hupehensis, is a selective retinoid X receptor α agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation[1].

In Vitro

Bigelovin (0-20 μM, 24-72 h) significantly inhibits cell viability of liver cancer cells and induces apoptosis and autophagy[1].
Bigelovin causes a significant increase of p62, LC3B-II, Beclin-1 and a corresponding decrease of p62 levels in a time-dependent manner[1].
Bigelovin induces cell death involves the suppression of mTOR pathway regulated by ROS production[1].

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

Bigelovin Related Antibodies

Cell Viability Assay[1]

Cell Line: HepG2 and SMMC-7721 cells.
Concentration: 0-20 μM.
Incubation Time: 24, 48, 72 h.
Result: Significantly reduced the cell viability of HepG2 and SMMC-7721 cells in a dose- and time dependent manner.
No significant difference observed in cell viability of normal liver cell lines, LO2 and LX2, after BigV treatment for 24, 48 or 72 h.

Western Blot Analysis[1]

Cell Line: HepG2 and SMMC-7721 cells.
Concentration: 0-10 μM.
Incubation Time: 24 h.
Result: The expression of Bcl-2 was decreased, whereas Bax was increased after treatment with BigV. Moreover, Caspase-9, -3 and PARP cleavage were activated significantly after BigV treatment.
In Vivo

Bigelovin (BigV, 5, 10, 20 mg/kg) exerts anti-tumor activity in HepG2 xenograft tumor model[1].

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

Animal Model: HepG2 xenograft model based on the male athymic BALB/c nude mice (5-6 weeks old, 18-22 g)[1].
Dosage: 5, 10, 20 mg/kg.
Administration: Intravenous injection every 2 days.
Result: The tumor growth rate was significantly slower in BigV treated groups in a dose-dependent manner, along with the reduced tumor weight.
No significant alteration of body weight and hepatic enzyme levels (AST, ALT and LDH) in serum was observed after BigV administration.
Western blot findings of tumor tissues indicated the activation of apoptosis and autophagy characterized by the increase of cleaved Caspase-3 and PARP, as well as LC3BII levels.
The inactivation of mTOR was also observed in tumor tissues isolated from BigV-treated mice.
Molecular Weight

304.34

Formula

C17H20O5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@@]12C(C=C[C@]1([C@@H](C[C@]3([C@H]([C@@H]2OC(C)=O)C(C(O3)=O)=C)[H])C)[H])=O
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 : 100 mg/mL (328.58 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 3.2858 mL 16.4290 mL 32.8580 mL
5 mM 0.6572 mL 3.2858 mL 6.5716 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

  • Dilution Calculator

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

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Molecular Weight *

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (8.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (8.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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:

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)

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: 99.92%

COA (273 KB) HNMR (270 KB) LCMS (87 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). 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 3.2858 mL 16.4290 mL 32.8580 mL 82.1450 mL
5 mM 0.6572 mL 3.2858 mL 6.5716 mL 16.4290 mL
10 mM 0.3286 mL 1.6429 mL 3.2858 mL 8.2145 mL
15 mM 0.2191 mL 1.0953 mL 2.1905 mL 5.4763 mL
20 mM 0.1643 mL 0.8214 mL 1.6429 mL 4.1072 mL
25 mM 0.1314 mL 0.6572 mL 1.3143 mL 3.2858 mL
30 mM 0.1095 mL 0.5476 mL 1.0953 mL 2.7382 mL
40 mM 0.0821 mL 0.4107 mL 0.8214 mL 2.0536 mL
50 mM 0.0657 mL 0.3286 mL 0.6572 mL 1.6429 mL
60 mM 0.0548 mL 0.2738 mL 0.5476 mL 1.3691 mL
80 mM 0.0411 mL 0.2054 mL 0.4107 mL 1.0268 mL
100 mM 0.0329 mL 0.1643 mL 0.3286 mL 0.8214 mL
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Bigelovin 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:

Bigelovin3668-14-2RAR/RXRReactive Oxygen SpeciesApoptosisAutophagyRetinoic acid receptorsRetinoid X receptorsInhibitorinhibitorinhibit

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