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Freselestat quarterhydrate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Freselestat quarterhydrate图片
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品名称
ONO-6818 quarterhydrate
ONO-PO-736 quarterhydrate
产品介绍
Freselestat quarterhydrate (ONO-6818 quarterhydrate) 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 quarterhydrate 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。
生物活性

Freselestat quarterhydrate (ONO-6818 quarterhydrate) is a potent and orally activeneutrophilelastaseinhibitor with aKiof 12.2 nM. Freselestat quarterhydrate is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreaticelastase, plasmin,thrombin, collagenase,cathepsinG, and murine macrophageelastase. Freselestat quarterhydrate has a potent anti-inflammatory activity[1][2][3][4].

IC50& Target

Ki: 12.2 nM (Neutrophil elastase)[3]

体外研究
(In Vitro)

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[3].

体内研究
(In Vivo)

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[1].

Animal Model:Male Wistar rats (228 g) induced by human neutrophil elastase (HNE)[1]
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.
分子量

457.03

性状

Solid

Formula

C23H28N6O4.1/4H2O

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
In solvent-80°C6 months
-20°C1 month