BCX-3607 is a potent, selective and orally active tissue factor/factor VIIa (TF-FVIIa) inhibitor with IC50 of 4 nM.
BCX-3607 is selective over other similar serine proteases including trypsin, thrombin, Factor Xa, and others.
BCX-3607 blocks coagulation in the PT assay with a value of 6.2 μM (concentration required to double the baseline clotting time) while having little effect on the activated partial thromboplastin time.
BCX-3607 reduces wet thrombus weight in a dose-dependent manner in rat model of venous thrombosis.
BCX-3607 decreases the murine IL-6 level inflammatory response to endotoxin in mouse model of endotoxemia.
BCX-3607 (3-30 uM) blocks the FVIIa-mediated induction of IL-8 in HaCaT keratinocytes, reduces IL-6 and IL-8 levels generated by TF/FVIIa-stimulated HUVEC cells.
