Freselestat (quarterhydrate)

Freselestat quarterhydrate (ONO-6818 quarterhydrate) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat quarterhydrate 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 quarterhydrate has a potent anti-inflammatory activity[1][2][3][4].

Product Specifications

Product Name Alternative

ONO-6818 (quarterhydrate) ; ONO-PO-736 (quarterhydrate)

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-quarterhydrate.html

Purity

99.0

Solubility

DMSO : 40 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL (ultrasonic; warming; heat to 60°C)

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.[1/4].O

Molecular Formula

C23H28N6O4.1/4H2O

Molecular Weight

457.03

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.