BAY-678
- Product Name
- BAY-678
- CAS No.
- 675103-36-3
- Chemical Name
- BAY-678
- Synonyms
- BAY-678;BAY 678,BAY678;BAY-678, 10 mM in DMSO;5-[(4R)-5-Acetyl-1,2,3,4-tetrahydro-6-methyl-2-oxo-1-[3-(trifluoromethyl)phenyl]-4-pyrimidinyl]-2-pyridinecarbonitrile;2-Pyridinecarbonitrile, 5-[(4R)-5-acetyl-1,2,3,4-tetrahydro-6-methyl-2-oxo-1-[3-(trifluoromethyl)phenyl]-4-pyrimidinyl]-
- CBNumber
- CB84666242
- Molecular Formula
- C20H15F3N4O2
- Formula Weight
- 400.35
- MOL File
- 675103-36-3.mol
BAY-678 Property
- Boiling point:
- 623.9±55.0 °C(Predicted)
- Density
- 1.42±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide
- form
- powder
- pka
- 9.35±0.70(Predicted)
- color
- white to light brown
- optical activity
- [α]/D +21 to +29°, c = 0.5 in methanol
N-Bromosuccinimide Price
- Product number
- SML1563
- Product name
- BAY-678
- Purity
- ≥98% (HPLC)
- Packaging
- 5MG
- Price
- $105.45
- Updated
- 2025/07/31
- Product number
- SML1563
- Product name
- BAY-678
- Purity
- ≥98% (HPLC)
- Packaging
- 25MG
- Price
- $424.65
- Updated
- 2025/07/31
- Product number
- 18615
- Product name
- BAY-678
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $38
- Updated
- 2024/03/01
- Product number
- 18615
- Product name
- BAY-678
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $93
- Updated
- 2024/03/01
- Product number
- 18615
- Product name
- BAY-678
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $166
- Updated
- 2024/03/01
BAY-678 Chemical Properties,Usage,Production
Uses
BAY 678, is a human neutrophil elastase (HNE) inhibitor with >2,000-fold selectivity for HNE over a panel of 21 other serine proteases.
Biological Activity
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].
Biochem/physiol Actions
BAY-678 is an orally available, highly potent and selective inhibitor of human neutrophil elastase (HNE). For full characterization details, please visit the BAY-678 probe summary on the Structural Genomics Consortium (SGC) website.BAY-677 is used as a negative control and is available from Sigma. To learn more about and purchase BAY-677, click here.To learn about other SGC chemical probes for protein targets, visit sigma.com/sgc
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].
storage
Store at -20°C
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.
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