Sivelestat
SIVELESTAT
CAS: 127373-66-4
Molecular Formula: C20H22N2O7S
Sivelestat - Names and Identifiers
| 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 |
Sivelestat - Physico-chemical Properties
| 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. |
Sivelestat - Risk and Safety
| WGK Germany | nwg |
Sivelestat - Preparation solution concentration reference
| 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 |
Last Update：2024-01-02 23:10:35
Sivelestat - Reference Information
| 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 |
Last Update：2024-04-09 21:48:26
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