??????
|
|
?????? ??
- ???
- 218-220°
- ??
- 1.369±0.06 g/cm3(Predicted)
- ?? ??
- Keep in dark place,Sealed in dry,2-8°C
- ???
- DMSO: ???10mg/mL, ??
- ??? ??
- ???? ??? ??
- ?? ?? (pKa)
- 3.67±0.10(Predicted)
- ??
- ???? ?????
- InChI
- InChI=1S/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
- SMILES
- C(OC1=CC=C(S(NC2=CC=CC=C2C(NCC(O)=O)=O)(=O)=O)C=C1)(=O)C(C)(C)C
??
| WGK ?? | nwg | ||
|---|---|---|---|
| ???? ??? | 11 - Combustible Solids |
?????? C??? ??, ??, ??
??
Sivelestat is an inhibitor of neutrophil elastase that prevents neutrophil extracellular trap formation and rescues mice from endotoxic shock. The inhibition of neutropil elastase by Sivelestat is a promising therapeutic strategy to inhibit glial scar and promote functional recovery by upregulating angiopoietin-1 after spinal cord injury.?? ??
A cell-permeable, potent, substrate-competitive, and highly specific inhibitor of neutrophil elastase (IC50 = 19-49 nM using rat, rabbit, hamster, human, and mouse leukocyte elastase). Displays about 100-fold greater selectivity over pancreatic elastase (IC50 = 5.6 μM) and is inactive against trypsin, thrombin, plasmin, kallikrein, chymotrypsin, and cathepsin G even at concentrations as high as 100 μM. Effectively suppresses human neutrophil elastase-induced lung hemorrhage and skin capillary permeability in vivo. Also reported to inhibit mast cell Stat6-protease.Biochem/physiol Actions
Sivelestat is a competitive human neutrophil elastase (HNE) inhibitor (IC50 = 44 nM, Ki = 0.2 μM). It also inhibits leukocyte elastase obtained from rabbit, rat, hamster and mouse (IC50 = 19 to 49 nM). However, it does not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G even at 100 μM. In in-vivo studies, it suppressed lung hemorrhage in hamster (ID50 = 82 μg/kg) by intratracheal administration and increase of skin capillary permeability in guinea pig (ID50 = 9.6 mg/kg) by intravenous administration, both of which were induced by human neutrophil elastase.?????? ?? ?? ? ???
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| ??? | ?? | ??? | ?? | ?? ? | ?? |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 |
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