1. Immunology/Inflammation Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  2. Glucocorticoid Receptor MMP
  3. Flocoumafen

Flocoumafen (WL 108366) is an orally active vitamin K epoxide reductase inhibitor and a multi-target ligand, which includes prostaglandin F synthase, serum albumin, glucocorticoid receptor 2, and MMP-9. Flocoumafen is a second-generation anticoagulant rodenticide (ARs) with a half-life of 177.4 hours and has deadly anticoagulant effects.

For research use only. We do not sell to patients.

Flocoumafen Chemical Structure

Flocoumafen Chemical Structure

CAS No. : 90035-08-8

Size Price Stock Quantity
5 mg In-stock
10 mg In-stock
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

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

Other Forms of Flocoumafen:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Flocoumafen (WL 108366) is an orally active vitamin K epoxide reductase inhibitor and a multi-target ligand, which includes prostaglandin F synthase, serum albumin, glucocorticoid receptor 2, and MMP-9. Flocoumafen is a second-generation anticoagulant rodenticide (ARs) with a half-life of 177.4 hours and has deadly anticoagulant effects[1][2][3].

IC50 & Target

MMP-9

 

Glucocorticoid Receptor 2

 

In Vitro

Flocoumafen best compound is prostaglandin F synthase and serum albumin (binding affinity ≥ 14.0 kcal/mol), followed by glucocorticoid receptor 2, matrix metalloproteinase-9, nuclear receptor ROR-alpha, and activin receptor type-1, with a binding affinity of ≥ 13.5 kcal/mol[1].

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

In Vivo

Flocoumafen (0.02-0.1 mg/kg, once a week for 14 weeks) accumulates residues in the liver of rats and cannot be completely metabolized, showing anticoagulant toxicity at high doses[3].

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

Animal Model: Male Fischer rats[3]
Dosage: 0.02 and 0.1 mg/kg; once a week; for 14 weeks
Administration: Oral
Result: Caused noticeable cell accumulation in the liver, with residuals increasing as the dose rises at low doses, while at high doses, it stabilized after a while. The lethal anticoagulant effected only occurs when the binding sites were saturated.
Showed about 30% of the cumulative dosage disappeared from the feces within 3 days after each administration at low doses,for high doses, this value ranges from 18% after the first dose to 59% after the tenth dose, and anticoagulant toxicity appeared after six weeks.
Molecular Weight

542.54

Formula

C33H25F3O4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C(C2CC(C3=CC=C(OCC4=CC=C(C(F)(F)F)C=C4)C=C3)CC5=C2C=CC=C5)=C(O)C6=CC=CC=C6O1

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 : 100 mg/mL (184.32 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 1.8432 mL 9.2159 mL 18.4318 mL
5 mM 0.3686 mL 1.8432 mL 3.6864 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.61 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 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)

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).
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
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 1.8432 mL 9.2159 mL 18.4318 mL 46.0796 mL
5 mM 0.3686 mL 1.8432 mL 3.6864 mL 9.2159 mL
10 mM 0.1843 mL 0.9216 mL 1.8432 mL 4.6080 mL
15 mM 0.1229 mL 0.6144 mL 1.2288 mL 3.0720 mL
20 mM 0.0922 mL 0.4608 mL 0.9216 mL 2.3040 mL
25 mM 0.0737 mL 0.3686 mL 0.7373 mL 1.8432 mL
30 mM 0.0614 mL 0.3072 mL 0.6144 mL 1.5360 mL
40 mM 0.0461 mL 0.2304 mL 0.4608 mL 1.1520 mL
50 mM 0.0369 mL 0.1843 mL 0.3686 mL 0.9216 mL
60 mM 0.0307 mL 0.1536 mL 0.3072 mL 0.7680 mL
80 mM 0.0230 mL 0.1152 mL 0.2304 mL 0.5760 mL
100 mM 0.0184 mL 0.0922 mL 0.1843 mL 0.4608 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
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.

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Flocoumafen
Cat. No.:
HY-111186
Quantity:
MCE Japan Authorized Agent: