Name | SIVELESTAT |
Synonyms | EI-546 CS-1329 ONO-5046 LY-544349 SIVELESTAT 127373-66-4 EI 546 sodium salt hydrate Elaspol sodium salt hydrate LY 544349 sodium salt hydrate (2-((4-(Pivaloyloxy)phenyl)sulfonamido)benzoyl)glycine o-(p-Hydroxybenzenesulfonamido)hippuric Acid Pivalate (Ester) N-{2-[({4-[(2,2-Dimethylpropanoyl)oxy]phenyl}sulfonyl)amino]benzoyl}glycine o-(p-Hydroxybenzenesulfonamido)hippuric acid, pivalate (ester) sodium salt hydrate 2-[[2-[[4-(2,2-dimethylpropanoyloxy)phenyl]sulfonylamino]benzoyl]amino]acetic acid propanoic acid, 2,2-dimethyl-, 4-[[[2-[[(carboxymethyl)amino]carbonyl]phenyl]amino]sulfonyl]phenyl ester |
CAS | 127373-66-4 |
InChI | InChI=1/C20H22N2O7S/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) |
InChIKey | BTGNGJJLZOIYID-UHFFFAOYSA-N |
Molecular Formula | C20H22N2O7S |
Molar Mass | 434.46 |
Density | 1.369±0.06 g/cm3(Predicted) |
Melting Point | 218-220° |
Solubility | DMSO: soluble10mg/mL, clear |
Appearance | White to off-white solid |
Color | white to off-white |
pKa | 3.67±0.10(Predicted) |
Storage Condition | Keep in dark place,Sealed in dry,2-8°C |
Refractive Index | 1.598 |
Use | The world's first acute lung injury treatment with systemic inflammatory response syndrome |
In vitro study | Sivelestat reduces the expression level of inflammatory mediators by inhibiting NF-kB. It inhibited the release of TGF-α caused by NE and inhibited the growth of gastric cancer cells. Sivelestat also suppresses the level of iNOS gene expression in hepatocytes stimulated by proinflammatory cytokines. |
In vivo study | Sivelestat alleviates (attenuates) sepsis-related kidney damage in rats. It inhibits GAPDH/siah1. Treatment with sivelestat in mice slows pulmonary fibrosis after acute lung injury. |
WGK Germany | nwg |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.302 ml | 11.508 ml | 23.017 ml |
5 mM | 0.46 ml | 2.302 ml | 4.603 ml |
10 mM | 0.23 ml | 1.151 ml | 2.302 ml |
5 mM | 0.046 ml | 0.23 ml | 0.46 ml |
Biological activity | Sivelestat (ONO5046, LY544349, EI546) is an effective inhibitor of neutrophil elastase (neutrophil elastase), IC50 is 44 nM, It has no activity against other proteases. |
Target | Value |
use | is the world's first drug for the treatment of acute lung injury with systemic inflammatory response syndrome |