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  3. Lipofermata

Lipofermata is a fatty acid transport protein 2 (FATP2) inhibitor. Lipofermata shows fatty acid transport inhibition with an IC50 of 4.84 μM in Caco-2 cells. Lipofermata, an analog of spiro-indoline-thadiazole, shows zinc-specific suppression of antibacterial activity. Lipofermata perturbs zinc homeostasis in E. coli K-12 with a MIC of 16 μM.

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Lipofermata Chemical Structure

Lipofermata Chemical Structure

CAS No. : 297180-15-5

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Based on 2 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

Lipofermata is a fatty acid transport protein 2 (FATP2) inhibitor. Lipofermata shows fatty acid transport inhibition with an IC50 of 4.84 μM in Caco-2 cells. Lipofermata, an analog of spiro-indoline-thadiazole, shows zinc-specific suppression of antibacterial activity. Lipofermata perturbs zinc homeostasis in E. coli K-12 with a MIC of 16 μM[1][2][3].

Cellular Effect
Cell Line Type Value Description References
HepG2 IC50
6.7 μM
Compound: Lipofermata; CB16.2
Inhibition of FATP2 in human HepG2 cells assessed as decrease in fatty acid transport after 5 mins by trypan blue dye based fluorescence quenching method
Inhibition of FATP2 in human HepG2 cells assessed as decrease in fatty acid transport after 5 mins by trypan blue dye based fluorescence quenching method
[PMID: 27446528]
In Vitro

Lipofermata inhibits C1-BODIPY-C12 transport into C2C12, INS-1E, Caco-2 and HepG2 cells at comparable levels yielding sigmoidal dose-response curves with IC50s in the low micromolar range (IC50=2.74-39.34 μM)[2].

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

Molecular Weight

360.23

Formula

C15H10BrN3OS

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1NC2=C(C=C(Br)C=C2)C13SC(C4=CC=CC=C4)=NN3

Shipping

Room temperature in continental US; may vary elsewhere.

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

DMSO : 100 mg/mL (277.60 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 2.7760 mL 13.8800 mL 27.7600 mL
5 mM 0.5552 mL 2.7760 mL 5.5520 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.

  • Molarity Calculator

  • Dilution Calculator

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: ≥ 2.08 mg/mL (5.77 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.77 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    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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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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+
%
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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).
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 2.7760 mL 13.8800 mL 27.7600 mL 69.4001 mL
5 mM 0.5552 mL 2.7760 mL 5.5520 mL 13.8800 mL
10 mM 0.2776 mL 1.3880 mL 2.7760 mL 6.9400 mL
15 mM 0.1851 mL 0.9253 mL 1.8507 mL 4.6267 mL
20 mM 0.1388 mL 0.6940 mL 1.3880 mL 3.4700 mL
25 mM 0.1110 mL 0.5552 mL 1.1104 mL 2.7760 mL
30 mM 0.0925 mL 0.4627 mL 0.9253 mL 2.3133 mL
40 mM 0.0694 mL 0.3470 mL 0.6940 mL 1.7350 mL
50 mM 0.0555 mL 0.2776 mL 0.5552 mL 1.3880 mL
60 mM 0.0463 mL 0.2313 mL 0.4627 mL 1.1567 mL
80 mM 0.0347 mL 0.1735 mL 0.3470 mL 0.8675 mL
100 mM 0.0278 mL 0.1388 mL 0.2776 mL 0.6940 mL
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Lipofermata 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.

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