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.

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Flocoumafen Chemical Structure

Flocoumafen Chemical Structure

CAS No. : 90035-08-8

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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

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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
Purity & Documentation
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Product Name:
Flocoumafen
Cat. No.:
HY-111186
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