AZD5248

Overview

AZD5248 is an orally active, selective dipeptidyl peptidase 1 ( cathepsin C ) inhibitor, with IC 50 values of 1 nM and 17 nM against human CatC , 44 nM against human DPP1 , and 67 nM against rat DPP1 . It exhibits low clearance and high bioavailability in animal models. AZD5248 forms an irreversible covalent bond with the catalytic Cys234 residue of CatC , exerts reversible inhibition via its nitrile moiety, blocks CatC -dependent amyloid formation, and reduces the activation levels of neutrophil serine proteases in bone marrow and blood. AZD5248 reacts with aortic elastin aldehydes to form stable 4-imidazolinones, induces ultrastructural changes in aortic tissue, and has an α-amino acid-based backbone. AZD5248 reduces the severity of acute pancreatitis in mouse models. AZD5248 can be used in research on chronic obstructive pulmonary disease, acute pancreatitis, neurodegenerative diseases, lysosomal storage disorders, acute lung injury, cystic fibrosis, and neutrophil-mediated inflammatory diseases.

Application

Products | Products > Disease Areas > Chronic Disease and Inflammation | Products > Disease Areas > Respiratory Inflammation | Products > Disease Areas > Digestive System Inflammation | Products > Disease Areas > Neurodegenerative Disease | Products > Disease Areas > Chronic Obstructive Pulmonary Disease | Products > Disease Areas > Acute Lung Injury | Products > Disease Areas > Pancreatitis | Products > Disease Areas > Cystic Fibrosis | Products > Disease Areas > Neurological, Eye or Ear Disease | Products > Disease Areas > Inflammation or Immune System Disease | Products > Disease Areas > Respiratory Disease | Products > Disease Areas > Digestive System Disease | Products > Disease Areas > Pulmonary Disease | Products > Signaling Pathways > Metabolic Enzyme/Protease | Products > Research Areas > Neurological Disease | Products > Research Areas > Inflammation/Immunology | Products > Signaling Pathways > Dipeptidyl Peptidase | Products > Signaling Pathways > Cathepsin

Product Information

• Catalog No.: HY-12733
• CAS No.: 1254318-44-9
• Molecular Formula: C22H22N4O2
• Molecular Weight: 374.44
• Purity: 98.9%
• Storage: Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
• Availability: In-stock

Source

Original product source