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  • DC Chemicals Limited
  • China
  • Product Name: BAY-678
  • Price: $450.0/100mg $750.0/250mg $1500.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

675103-36-3

675103-36-3 structure
675103-36-3 structure
  • Name: BAY 678
  • Chemical Name: BAY-678
  • CAS Number: 675103-36-3
  • Molecular Formula: C20H15F3N4O2
  • Molecular Weight: 400.35
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease Elastase
  • Create Date: 2019-02-08 19:56:19
  • Modify Date: 2024-04-05 18:51:44
  • 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).

Name BAY-678
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).
Related Catalog
Target

IC50: 20 nM (HNE)[1].

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 4 th generation inhibitor of HNE[1]. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC)[2].
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].
References

[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.

[2]. von Nussbaum F, et al. Neutrophil elastase inhibitors for the treatment of (cardio)pulmonary diseases: Into clinical testing with pre-adaptive pharmacophores. Bioorg Med Chem Lett. 2015 Oct 15;25(20):4370-81.

Molecular Formula C20H15F3N4O2
Molecular Weight 400.35
Storage condition 2-8℃