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BAY-678 HNE inhibitor

Catalog No.C4325
Size Price Stock Qty
5mg
$90.00
In stock
10mg
$162.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

BAY-678

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Chemical Properties

Cas No. 675103-36-3 SDF Download SDF
Chemical Name 5-[(4R)-5-acetyl-1,2,3,4-tetrahydro-6-methyl-2-oxo-1-[3-(trifluoromethyl)phenyl]-4-pyrimidinyl]-2-pyridinecarbonitrile
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
Formula C20H15F3N4O2 M.Wt 400.4
Solubility ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide Storage Store at 2-8°C
Physical Appearance A crystalline solid 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.

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].

References:
[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.