中文名 | 西维来司他钠 |
英文名 | Sivelestat Sodium |
别名 | 西维来司钠 西维来司他钠 化合物 T21414 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 |
英文别名 | Sivelestat Sodium SIVELESTAT SODIUM Sivelestat sodium salt Sivelestat SodiuM anhydrous N-{2-[({4-[(2,2-Dimethylpropanoyl)oxy]phenyl}sulfonyl)amino]benzoyl}glycinesodiumsalt sodium,2-[[2-[[4-(2,2-dimethylpropanoyloxy)phenyl]sulfonylamino]benzoyl]amino]acetate Sodium ({2-[({4-[(2,2-dimethylpropanoyl)oxy]phenyl}sulfonyl)amino]benzoyl}amino)acetate Glycine, N-[2-[[[4-(2,2-diMethyl-1-oxopropoxy)phenyl]sulfonyl]aMino]benzoyl]-, MonosodiuM salt n-[2-[[[4-(2,2-dimethyl-1-oxopropoxy)phenyl]sulfonyl]amino]benzoyl]-(s)-glycine monosodium salt N-[2-[[[4-(2,2-Dimethyl-1-oxopropoxy)phenyl]sulfonyl]amino]benzoyl]-(S)-glycine monosodium salt sodium 2-[[[2-[[4-(2,2-dimethyl-1-oxopropoxy)phenyl]sulfonylamino]phenyl]-oxomethyl]amino]acetate |
CAS | 150374-95-1 |
化学式 | C20H21N2NaO7S |
分子量 | 456.44 |
InChI | InChI=1/C20H22N2O7S.Na/c1-20(2,3)19(26)29-13-8-10-14(11-9-13)30(27,28)22-16-7-5-4-6-15(16)18(25)21-12-17(23)24;/h4-11,22H,12H2,1-3H3,(H,21,25)(H,23,24);/q;+1/p-1 |
熔点 | 104-108 °C(Solv: water (7732-18-5)) |
溶解度 | DMSO (微溶) 、甲醇 (微溶) |
存储条件 | Desiccate at RT |
外观 | 固体 |
颜色 | White to Off-White |
体外研究 | 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. |
体内研究 | 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. |
参考资料 展开查看 | 1. [IF=5.396] Zhu Tao et al."Evaluation of the anti-inflammatory properties of the active constituents in Ginkgo biloba for the treatment of pulmonary diseases."Food Funct. 2019 Apr;10(4):2209-2220 |
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