N-[2-[[[4-(2,2-二甲基-1-氧代丙氧基)苯基]磺酰]氨基]苯甲酰]-(S)-甘氨酸单钠盐
N-[2-[[[4-(2,2-二甲基-1-氧代丙氧基)苯基]磺酰]氨基]苯甲酰]-(S)-甘氨酸单钠盐
N-[2-[[[4-(2,2-二甲基-1-氧代丙氧基)苯基]磺酰]氨基]苯甲酰]-(S)-甘氨酸单钠盐 性质
| 熔点 | 104-108 °C(Solv: water (7732-18-5)) |
|---|---|
| 储存条件 | Desiccate at RT |
| 溶解度 | 可溶于DMSO(少许)、甲醇(少许) |
| 形态 | 固体 |
| 颜色 | 白色至类白色 |
N-[2-[[[4-(2,2-二甲基-1-氧代丙氧基)苯基]磺酰]氨基]苯甲酰]-(S)-甘氨酸单钠盐 用途与合成方法
Sivelestat (ONO-5046) does not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G even at 100 μM.
Sivelestat (ONO-5046) exhibits IC
50
values of 44 nM, 36 nM, 19 nM, 37 nM and 49 nM for human, rabbit, rat, hamster and mouse neutrophil elastase, respectively.
Sivelestat (ONO-5046, 0.021-2.1 mg/kg, intratracheally) suppresses lung hemorrhage in hamster (ID
50
= 82 pg/kg) by intratracheal administration and increase of skin capillary permeability in guinea pig (ID
50
= 9.6 mg/kg) by intravenous administration, both of which are induced by human neutrophil elastase.
Sivelestat (10 mg/kg, infusion via the tail vein) ameliorates lung injury after hemorrhagic shock in rats.
Sivelestat (15, 60 mg/kg, ip) prevents ischemia–reperfusion injury in the rat bladder.
| Animal Model: | Male Golden hamsters, weighing 90 to 110 g. |
| Dosage: | 0.021-2.1 mg/kg. |
| Administration: | Intratracheally five min before HNE injection. |
| Result: | Significantly and dosedependently suppressed the lung hemorrhage. |
| Animal Model: | Male Sprague-Dawley rats weighing 350-400 g. |
| Dosage: | 10 mg/kg. |
| Administration: | Continuous infusion via the tail vein at 10 mg/kg/h for 60 min during the resuscitation phase. |
| Result: |
Greatly suppressed lung injury, as revealed by the reduced histological damage.
Significantly ameliorated HSR-induced lung injury. Markedly decreased the levels of TNF-α and iNOS gene. |
| Animal Model: | Male Sprague Dawley rats, 8 weeks old and weighing 250-320 g. |
| Dosage: | 15 mg/kg or 60 mg/kg. |
| Administration: | IP. |
| Result: | Decreased the blood flow in the bladder during reperfusion phase compared to the IR group. |
N-[2-[[[4-(2,2-二甲基-1-氧代丙氧基)苯基]磺酰]氨基]苯甲酰]-(S)-甘氨酸单钠盐 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2026-07-06 | E6013 | N-[2-[[[4-(2,2-二甲基-1-氧代丙氧基)苯基]磺酰]氨基]苯甲酰]-(S)-甘氨酸单钠盐 | 150374-95-1 | 5mg | 997 |
| 2026-07-06 | E6013 | N-[2-[[[4-(2,2-二甲基-1-氧代丙氧基)苯基]磺酰]氨基]苯甲酰]-(S)-甘氨酸单钠盐 | 150374-95-1 | 25mg | 2397 |