Tiprelestat 是一种有效的人类中性粒细胞弹性蛋白酶 (elastase) 抑制剂。Tiprelestat 具有抗菌和抗炎活性。Tiprelestat 可用于炎症/免疫疾病的研究。
生物活性 | Tiprelestat is a potent human neutrophilelastaseinhibitor. Tiprelestat has antimicrobial and anti-inflammatory activities. Tiprelestat can be used in the research of inflammation/immune disease[1]. |
体外研究 (In Vitro) | Tiprelestat (4 and 8 μM) inhibitsP. 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. |
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体内研究 (In Vivo) | Tiprelestat (1 mg/kg, intranasal inhalation) suppresses lung elastase activity and apoptosis in MV-O2mice[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.
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |