BAY-678

CAS No. 675103-36-3

BAY-678( —— )

Catalog No. M32798 CAS No. 675103-36-3

BAY-678 is a human neutrophil elastase (HNE; IC50: 20 nM) inhibitor with oral bioactivity, potency and selectivity.BAY-678 is a chemical probe recommended by the Structural Genomics Consortium (SGC).

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    BAY-678
  • Note
    Research use only, not for human use.
  • Brief Description
    BAY-678 is a human neutrophil elastase (HNE; IC50: 20 nM) inhibitor with oral bioactivity, potency and selectivity.BAY-678 is a chemical probe recommended by the Structural Genomics Consortium (SGC).
  • 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).
  • 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 4th generation inhibitor of HNE. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC). BAY-678 has more than 2,000-fold selectivity in a panel of 21 serine proteases.
  • 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.
  • Synonyms
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    Others
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    675103-36-3
  • Formula Weight
    400.35
  • Molecular Formula
    C20H15F3N4O2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : ≥ 100 mg/mL (249.78 mM ) Ethanol : ≥ 4.76 mg/mL (11.89 mM)
  • SMILES
    CC(=O)C1=C(C)N(C(=O)N[C@@H]1c1ccc(nc1)C#N)c1cccc(c1)C(F)(F)F
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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.?
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