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BAY-678
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BAY-678图片
CAS NO:675103-36-3
规格:98%
分子量:400.4
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
HNE inhibitor
CAS:675103-36-3
分子式:C20H15F3N4O2
分子量:400.4
纯度:98%
存储:Store at -20°C

Background:

BAY-678 is an orally active, potent and selective inhibitor of human neutrophil elastase (HNE) [1][2].


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) [1].


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 [1].


In rats, BAY-678 showed medium clearance with t1/2 of 1.3h [1].


参考文献:
[1].  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.
[2].  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.