Fiboflapon is an orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood.

Fiboflapon ?also demonstrated an extended pharmacodynamic effect in a rodent bronchoalveolar lavage (BAL) model .Fiboflapon ?exhibits excellent preclinical toxicology and pharmacokinetics in rat and dog.

When rat lungs are challenged in vivo with calcium-ionophore, Fiboflapon ?inhibits LTB4 and cysteinyl leukotriene (CysLT) production with ED50s of 0.12 mg/kg and 0.37 mg/kg, respectively.?The inhibition measured 16 h following a single oral dose of 3 mg/kg was 86% and 41% for LTB4 and CysLTs, respectively.?In an acute inflammation setting, Fiboflapon dose-dependently reduced LTB4, CysLTs, plasma protein extravasation and neutrophil influx induced by peritoneal zymosan injection.?Finally, Fiboflapon increases survival time in mice exposed to a lethal intravenous injection of platelet activating factor (PAF).Oral administration of Fiboflapon ?results in sustained inhibition of ex vivo ionophore-challenged whole blood LTB4 biosynthesis with >90% inhibition for up to 12 h and an EC50 of approximately 7 nM.

936350-00-4

C38H43N3O4S

637.83

GSK2190915;AM-803

DMSO:50 mg/mL (78.39 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years