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BAY 678

Names

[ CAS No. ]:
675103-36-3

[ Name ]:
BAY 678

Biological Activity

[Description]:

BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC).

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Elastase
Research Areas >> Inflammation/Immunology

[Target]

IC50: 20 nM (HNE)[1].


[In Vitro]

BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM. The Ki value of BAY-678 for MNE is 700 nM. BAY-678 is the 4 th generation inhibitor of HNE[1]. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC)[2].

[In Vivo]

BAY-678 (17) reveals significant efficacy in preclinical models of ALI and lung emphysema, demonstrating their anti-inflammatory and anti-remodeling mode of action. Additionally, BAY-678 (17) has shown significant beneficial pulmonary hemodynamic and vascular effects in models of PAH in rats and mice[2].

[References]

[1]. von Nussbaum F, 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.

[2]. von Nussbaum F, et al. Neutrophil elastase inhibitors for the treatment of (cardio)pulmonary diseases: Into clinical testing with pre-adaptive pharmacophores. Bioorg Med Chem Lett. 2015 Oct 15;25(20):4370-81.


[Related Small Molecules]

DMP 777 | GW311616 | Sivelestat Sodium tetrahydrate | Alvelestat | AE-3763 | BAY-678 racemate | BAY-85-8501 | Lodelaben | ZD-0892 | ZD8321

Chemical & Physical Properties

[ Molecular Formula ]:
C20H15F3N4O2

[ Molecular Weight ]:
400.35

[ Storage condition ]:
2-8℃

Related Compounds