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BAY-678

Catalog No. T10473   CAS 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).

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BAY-678 Chemical Structure
BAY-678, CAS 675103-36-3
Pack Size Availability Price/USD Quantity
5 mg In stock $ 55.00
10 mg In stock $ 97.00
25 mg In stock $ 213.00
50 mg In stock $ 378.00
100 mg In stock $ 562.00
500 mg In stock $ 1,230.00
1 mL * 10 mM (in DMSO) In stock $ 61.00
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Purity: 98.25%
ee: 100%
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Biological Description
Chemical Properties
Storage & Solubility Information
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).
Targets&IC50 HNE:20 nM, MNE:700 nM(Ki)
In vitro BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium.[2]
The Ki value of BAY-678 for MNE is 700 nM. BAY-678 is the 4th generation inhibitor of HNE.[1]
In vivo BAY-678 reveals significant efficacy in preclinical models of ALI and lung emphysema. Additionally, BAY-678 has shown significant beneficial pulmonary hemodynamic and vascular effects in models of PAH in rats and mice.[2]
Molecular Weight 400.35
Formula C20H15F3N4O2
CAS No. 675103-36-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90.0 mg/mL (224.8 mM)

Ethanol: 4.3 mg/mL (10.7 mM)

TargetMolReferences and Literature

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. 3. BAY-678 Selective chemical probe for Human Neutrophil Elastase.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Bioactive Compounds Library Max Bioactive Compound Library Covalent Inhibitor Library

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Keywords

BAY-678 675103-36-3 Others BAY 678 BAY678 inhibitor inhibit

 

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