Tiprelestat

Tiprelestat is a potent human neutrophil elastase inhibitor. Tiprelestat has antimicrobial and anti-inflammatory activities. Tiprelestat can be used in the research of inflammation/immune disease[1].

Research Areas >> Infection

Signaling Pathways >> Metabolic Enzyme/Protease >> Elastase

Research Areas >> Inflammation/Immunology

Tiprelestat (4 and 8 μM) inhibits P. aeruginosa-secreted peptidase[3]. Tiprelestat (10 μg/mL, 1 h) inhibits LPS-induced MCP-1 production in U937 cells[4]. Tiprelestat (10 μg/mL, 1 h) down-regulates LPS-induced AP-1 and NF-κB activation in U937 cells[4]. Western Blot Analysis[4] Cell Line: U937 cells Concentration: 10 μg/mL Incubation Time: 1 h Result: Prevented LPS-induced degradation of IκBα, IκBβ, and IRAK.

Tiprelestat (1 mg/kg, intranasal inhalation) suppresses lung elastase activity and apoptosis in MV-O2 mice[2]. Tiprelestat (0.2 mg/kg, s.c. for 2 weeks) attenuates hypoxic pulmonary hypertension in mice[5]. Animal Model: Mice, treated with Mechanical ventilation with O2-rich gas[2] Dosage: 1 mg/kg Administration: Intranasal inhalation Result: Increased the lung abundance of nuclear Klf4 protein. Animal Model: Su/Hx rat model[5] Dosage: 0.2 mg/kg Administration: Subcutaneous injection (s.c.), daily for 2 weeks. Result: Reduced elastase activity and reversed pulmonary hypertension.