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| BAY-678 Basic information |
| Product Name: | BAY-678 | | Synonyms: | BAY-678;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]- | | CAS: | 675103-36-3 | | MF: | C20H15F3N4O2 | | MW: | 400.35 | | EINECS: | | Product Categories: | | Mol File: | 675103-36-3.mol |
| BAY-678 Chemical Properties |
| 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 | | pka | 9.35±0.70(Predicted) | | form | powder | | color | white to light brown | | optical activity | [α]/D +21 to +29°, c = 0.5 in methanol |
| BAY-678 Usage And Synthesis |
| 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 | | 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. |
| BAY-678 Preparation Products And Raw materials |
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