FRESELESTAT

生物活性靶点体外研究体内研究 FRESELESTAT 试剂级价格

FRESELESTAT

CAS号:208848-19-5
英文名:FRESELESTAT
中文名:FRESELESTAT
CBNumber:CB12451308
分子式:C23H28N6O4
分子量:452.51
MOL File:208848-19-5.mol

FRESELESTAT化学性质

熔点 :151-153oC
密度 :1.32±0.1 g/cm3(Predicted)
储存条件 :-20°C Freezer
溶解度 :DMSO (Slightly), Methanol (Slightly)
酸度系数(pKa) :12.43±0.46(Predicted)
形态 :Solid
颜色 :Off-White to Pale Yellow

FRESELESTAT性质、用途与生产工艺

生物活性 Freselestat (ONO-6818) 是一种有效且具有口服活性的嗜中性粒细胞弹性蛋白酶 (neutrophil elastase) 抑制剂，Ki 为 12.2 nM。Freselestat 对其他蛋白酶（例如胰蛋白酶，蛋白酶3，胰弹性蛋白酶，纤溶酶，凝血酶，胶原酶，组织蛋白酶G和鼠巨噬细胞弹性蛋白酶）的活性低 100 倍以上，并具有有效的抗炎活性。
靶点

Ki: 12.2 nM (Neutrophil elastase)
体外研究

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.

体内研究

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.