Acetamide, N-[3-[[5-chloro-2-[[5-(3-thienyl)-2-pyridinyl]amino]-4-pyrimidinyl]amino]phenyl]-

Description

Cathepsin C-IN-5 (compound SF38) is a potent, selective and orally active Cathepsin C inhibitor with IC₅₀s of 59.9 nM, 4.26 µM, >5 µM, >5 µM, >5 µM for Cat C, Cat L, Cat S, Cat B, Cat K, respectively. Cathepsin C-IN-5 inhibits the Cat C activity in bone marrow and blood. Cathepsin C-IN-5 decreases the activation of NSPs (neutrophil serine proteases). Cathepsin C-IN-5 shows anti-inflammatory activity^[1].

Cathepsin C-IN-5 (compound SF38) shows inhibition in THP-1 and U937 cells with IC₅₀s of 115.4, 70.2 nM, respectively^[1].

Cathepsin C-IN-5 (1500 mg/kg) shows no significant weight loss or toxic reaction within 7 days after the administration in ICR mice^[1].
Cathepsin C-IN-5 (10 mg/kg for p.o.; 2 mg/kg for i.v.) shows good bioavailability with F=42.07%^[1].
Cathepsin C-IN-5 (2, 10, 50 mg/kg; p.o.) shows effective antiinflammatory activity and potential protective effect in an animal model of ALI^[1].