208848-19-5
208848-19-5 結(jié)構(gòu)式
基本信息
ONO 6818
ONO-6818
ONO-PO-736
Freselesat
FRESELESTAT
5-Amino-N-[1-[[5-(1,1-dimethylethyl)-1,3,4-oxadiazol-2-yl]carbonyl]-2-methylpropyl]-6-oxo-2-phenyl-1(6H)-pyrimidineacetamide
1(6H)-PyriMidineacetaMide,5-aMino-N-[1-[[5-(1,1-diMethylethyl)-1,3,4-oxadiazol-2-yl]carbonyl]-2-Methylpropyl]-6-oxo-2-phenyl-
物理化學(xué)性質(zhì)
常見(jiàn)問(wèn)題列表
Ki: 12.2 nM (Neutrophil elastase)
Simulated extracorporeal circulation is established by recirculating fresh heparinized (3.75 U/mL) human blood for 120 minutes in a membrane oxygenator and a roller pump with and without 1.0 μM of Freselestat (ONO-6818). Neutrophil elastase levels are significantly lower in the Freselestat group. Freselestat significantly reduces interleukin 8 and C5b-9 production. Freselestat does not modulate changes of CD11b and L-selectin during recirculation.
Freselestat (ONO-6818; 10-100 mg/kg; oral administration; daily; for 8 weeks) treatment attenuates dose-dependently HNE-induced increases in lung myeloperoxidase activity, hemoglobin, and neutrophil count in bronchoalveolar lavage fluid. ONO-6818 inhibits acute lung injury induced by HNE by minimizing lung hemorrhage and accumulation of neutrophils in the lung.
| Animal Model: | Male Wistar rats (228 g) induced by human neutrophil elastase (HNE) |
| Dosage: | 10 mg/kg, 100 mg/kg |
| Administration: | Oral administration; daily; for 8 weeks |
| Result: | Attenuated dose-dependently HNE-induced increases in lung myeloperoxidase activity, hemoglobin, and neutrophil count in bronchoalveolar lavage fluid. |