Freselestat

Freselestat (ONO-6818) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat has a potent anti-inflammatory activity[1][2][3][4].

Product Specifications

CAS Number

[208848-19-5]

Product Name Alternative

ONO-6818; ONO-PO-736

UNSPSC

12352005

Target

Elastase

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/freselestat.html

Purity

99.68

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(NC(C(C1=NN=C(C(C)(C)C)O1)=O)C(C)C)CN(C(C2=CC=CC=C2)=NC=C3N)C3=O

Molecular Formula

C23H28N6O4

Molecular Weight

452.51

References & Citations

[1]Am J Respir Crit Care Med. 2002 Aug 15;166 (4) :496-500.|[2]K Ohmoto, et al. Design and synthesis of new orally active inhibitors of human neutrophil elastase. Bioorg Med Chem. 2001 May;9 (5) :1307-23.|[3]Yasushi Hirota, et al. Effects of the neutrophil elastase inhibitor (ONO-6818) on acetic acid induced colitis in Syrian hamsters. J Vet Med Sci. 2004 Oct;66 (10) :1223-8.|[4]Yukihiro Yoshimura, et al. ONO-6818, a novel, potent neutrophil elastase inhibitor, reduces inflammatory mediators during simulated extracorporeal circulation. Ann Thorac Surg. 2003 Oct;76 (4) :1234-9.