Cathepsin C-IN-5 (C09-1120-662)

Cathepsin C-IN-5 (compound SF38) is a potent, selective and orally active Cathepsin C inhibitor with IC 50 s 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 activityIn VitroCathepsin C-IN-5 (compound SF38) shows inhibition in THP-1 and U937 cells with IC 50 s of 115.4, 70.2 nM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoCathepsin C-IN-5 (1500 mg/kg) shows no significant weight loss or toxic reaction within 7 days after the administration in ICR mice . Cathepsin C-IN-5 (10 mg/kg for p.o.; 2 mg/kg for i.v.) shows good bioavailability with F=42.07% . 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57BL/6 male mice (acute lung injury (ALI) mice model) Dosage: 2, 10, 50 mg/kg (one hour after administration, received LPS (20 mg/kg)) Administration: P.o. Result: Decreased the levels of proinflammatory cytokines (TNF-a, IL-6, and GM-CSF) and increased the the concentration of the anti-inflammatory cytokine (IL-10) in a dose-dependent manner.Form:SolidIC50& Target:IC 50 : 59.9 nM (Cat C),4.26 µM (Cat L),>5 µM (Cat S),>5 µM (Cat B),>5 µM (Cat K). Specification: 0.95 Molecular Formula: C21H17ClN6OS Molecular Weight: 436.92