BAY-678 is an orally active, potent and selective inhibitor of human neutrophil elastase (HNE) .
Human neutrophil elastase (HNE) is a member of the chymotrypsin-like family of serine proteases and is stored in the neutrophil cytoplasm. HNE is a key protease for matrix degradation and high HNE activity is occured in inflammatory diseases. So HNE is a potential target for the treatment of pulmonary diseases such as acute lung injury (ALI), acute respiratory distress syndrome (ARDS), chronic obstructive pulmonary disease (COPD), bronchiectasis (BE), and pulmonary hypertension (PH) .
BAY-678 is an orally active, potent and selective inhibitor of human neutrophil elastase (HNE). BAY-678 inhibited HNE reversibly with IC50 value of 20 nM and Ki value of 15 nM. BAY-678 showed no inhibition against 21 related serine proteases, up to a concentration of 30 μM .
In rats, BAY-678 showed medium clearance with t1/2 of 1.3h .
. von Nussbaum F, Li VM, Allerheiligen S, et al. Freezing the Bioactive Conformation to Boost Potency: The Identification of BAY 85-8501, a Selective and Potent Inhibitor of Human Neutrophil Elastase for Pulmonary Diseases. ChemMedChem. 2015 Jul;10(7):1163-73.
. von Nussbaum F, Li VM, Meibom D, et al. Potent and Selective Human Neutrophil Elastase Inhibitors with Novel Equatorial Ring Topology: in vivo Efficacy of the Polar Pyrimidopyridazine BAY-8040 in a Pulmonary Arterial Hypertension Rat Model. ChemMedChem. 2016 Jan 19;11(2):199-206.
|Physical Appearance||A crystalline solid|
|Storage||Store at 2-8°C|
|Solubility||≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide|
|Canonical SMILES||O=C1N(C2=CC(C(F)(F)F)=CC=C2)C(C)=C(C(C)=O)[[email protected]@H](C3=CN=C(C#N)C=C3)N1|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|