1. Cell Cycle/DNA Damage Epigenetics Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Apoptosis Anti-infection
  2. Sirtuin PPAR Fatty Acid Synthase (FASN) c-Myc Bacterial
  3. Agrimol B

Agrimol B, a polyphenol, is an orally active and potent SIRT1 activator. Agrimol B shows anti-adipogenic and anticancer activity. Agrimol B shows antibacterial activity against plant pathogens. Agrimol B dramatically inhibits 3T3-L1 adipocyte differentiation by reducing PPARγ, C/EBPα, FAS, UCP-1, and apoE expression. The action of Agrimol B on the cancer cells is likely derived from its effect on c-MYC, SKP2 and p27.

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Agrimol B Chemical Structure

Agrimol B Chemical Structure

CAS No. : 55576-66-4

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Based on 1 publication(s) in Google Scholar

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Description

Agrimol B, a polyphenol, is an orally active and potent SIRT1 activator. Agrimol B shows anti-adipogenic and anticancer activity. Agrimol B shows antibacterial activity against plant pathogens. Agrimol B dramatically inhibits 3T3-L1 adipocyte differentiation by reducing PPARγ, C/EBPα, FAS, UCP-1, and apoE expression. The action of Agrimol B on the cancer cells is likely derived from its effect on c-MYC, SKP2 and p27[1][2][3].

IC50 & Target[1]

SIRT1

 

PPARγ

 

In Vitro

Agrimol B blocks adipogenesis at the early stage of differentiation in a dose-dependent manner, with an IC50 of 3.35 ± 0.32 μM[1].
Agrimol B induces SIRT1 (silent information regulator 2 homolog 1) translocation and expression in 3T3-L1 adipocytes[1].
Agrimol B inhibits PC-3 and A549 cells growth, with GI50 (growth inhibition 50%) values of 29 and 19 μM, GI75 values of 49 and 50 μM, and GI90 values of 63 and 76 μM, respectively[2].
Agrimol B (0-76 μM) dose-dependently increases cells at G0 in both cell lines[2].
Agrimol B (0-76 μM, 3 days) reduces the protein expression of c-MYC and SKP2 (S-phase kinase-associated protein 2), increases p27 (cyclin-dependent kinase inhibitor 1B), and down-regulates SPT16 (Suppressor of Ty Homolog-16) and SSRP1 (Structure-Specific Recognition Protein 1)[2].

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

Cell Cycle Analysis[2]

Cell Line: PC-3 and A549 cells
Concentration: 29 and 63 μM (PC-3), 19 and 76 μM (A549)
Incubation Time: 10 min
Result: Dose-dependently increased cells at G0 in both cell lines. Reduced percentage of cells positive for Ki-67, and increased p27 positive cell population in PC-3 and A549 cells.

Western Blot Analysis[2]

Cell Line: PC-3 and A549 cells
Concentration: 0, 29, 49, 63 μM (PC-3); 0, 19, 50, and 76 μM (A549)
Incubation Time: 3 days
Result: Reduced c-MYC, SKP2 and increased p27 in both cell lines, and down-regulated SPT16 and SSRP1 in A549 cells with no effect on CRM1 in both cell lines.

Immunofluorescence[1]

Cell Line: 3T3-L1 preadipocyte
Concentration: 0, 3, and 10 μM
Incubation Time: 6 days
Result: Significantly increased nuclear positive rate of SIRT1; Markedly increased SIRT1 expression at 10 μM, the effect vanished at 3 μM. Down-regulated PPARγ and C/EBPα (CCAAT/enhancer-binding protein α) expression; Significantly decreased FAS (fatty acid synthesis), UCP-1 (uncoupling protein-1), and apoE (apolipoprotein E) expression at 10 μM.
In Vivo

Agrimol B (10 mg/kg, Orally, daily) reduces growth of prostate cancer cell xenograft in mice[2].

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

Animal Model: BALB/c nude mice (6-week-old, male, injected with PC-3 cells in 0.2 mL PBS subcutaneously)[2]
Dosage: 10 mg/kg
Administration: Orally, daily, after 15 days of cancer cell implantation
Result: Inhibited tumor growth in a mouse model of human prostate cancer, reduced the tumor volume at day 31 and day 32.
Molecular Weight

682.75

Formula

C37H46O12

CAS No.
Appearance

Solid

Color

White to yellow

SMILES

CC[C@H](C)C(C1=C(O)C(CC2=C(O)C(C(CCC)=O)=C(OC)C(C)=C2O)=C(O)C(CC3=C(O)C(C(CCC)=O)=C(OC)C(C)=C3O)=C1O)=O

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (7.32 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 1.4647 mL 7.3233 mL 14.6467 mL
5 mM 0.2929 mL 1.4647 mL 2.9293 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 0.5 mg/mL (0.73 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 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% Corn Oil

    Solubility: ≥ 0.5 mg/mL (0.73 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.5 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 (5.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

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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).
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: 99.75%

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. 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 1.4647 mL 7.3233 mL 14.6466 mL 36.6166 mL
5 mM 0.2929 mL 1.4647 mL 2.9293 mL 7.3233 mL
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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.

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Agrimol B
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