BAY-678 is an orally bioavailable, highly potent, selective, and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM. It is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC). For research use only; not sold to patients.
- Orally bioavailable
- Highly potent and selective inhibitor of human neutrophil elastase (HNE)
- Cell-permeable
- IC50 of 20 nM (HNE)
- Ki value for MNE is 700 nM
- Fourth-generation HNE inhibitor
- More than 2,000-fold selectivity in a panel of 21 serine proteases
- Reveals significant efficacy in preclinical models of ALI and lung emphysema, demonstrating anti-inflammatory and anti-remodeling mode of action
- Shown significant beneficial pulmonary hemodynamic and vascular effects in models of PAH in rats and mice