FRESELESTAT
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- CAS号:
- 208848-19-5
- 英文名:
- FRESELESTAT
- 英文别名:
- ONO6818;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-
- 中文名:
- FRESELESTAT
- 中文别名:
- 化合物 T31877;夫瑞司他 ONO6818
- CBNumber:
- CB12451308
- 分子式:
- C23H28N6O4
- 分子量:
- 452.51
- MOL File:
- 208848-19-5.mol
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FRESELESTAT化学性质
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熔点:
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151-153oC
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密度:
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1.32±0.1 g/cm3(Predicted)
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储存条件:
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-20°C Freezer
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溶解度:
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DMSO (Slightly), Methanol (Slightly)
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酸度系数(pKa):
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12.43±0.46(Predicted)
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形态:
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Solid
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颜色:
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Off-White to Pale Yellow
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FRESELESTAT性质、用途与生产工艺
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。
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.
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Animal Model:
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Male Wistar rats (228 g) induced by human neutrophil elastase (HNE)
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Dosage:
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10 mg/kg, 100 mg/kg
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Administration:
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Oral administration; daily; for 8 weeks
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Result:
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Attenuated dose-dependently HNE-induced increases in lung myeloperoxidase activity, hemoglobin, and neutrophil count in bronchoalveolar lavage fluid.
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FRESELESTAT
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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| 2024/01/25 | HY-15652 | Freselestat | | 5 mg | 1900元 |
| 2024/01/25 | HY-15652 | Freselestat | | 10 mg | 3100元 |
208848-19-5, FRESELESTAT 相关搜索:
- C23H28N6O4
- 化合物 T31877
- 夫瑞司他 ONO6818
- 208848-19-5
- Freselesat
- 5-Amino-N-[1-[[5-(1,1-dimethylethyl)-1,3,4-oxadiazol-2-yl]carbonyl]-2-methylpropyl]-6-oxo-2-phenyl-1(6H)-pyrimidineacetamide
- ONO-PO-736
- ONO-6818
- ONO6818
- ONO 6818
- 1(6H)-PyriMidineacetaMide,5-aMino-N-[1-[[5-(1,1-diMethylethyl)-1,3,4-oxadiazol-2-yl]carbonyl]-2-Methylpropyl]-6-oxo-2-phenyl-
- FRESELESTAT