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Sivelestat (ONO5046; LY544349; EI546) is a potent and selective inhibitor of neutrophil elastase with IC50 of 44nM. Sivelestat suppresses the growth of gastric cancer cells by inhibiting the release of TGF-α stimulated by NE. Sivelestat reduces the levels of inflammatory mediators by inhibiting NF-kB.
In vivo, Sivelestat (ONO5046) suppressed lung hemorrhage in hamster (ID50 = 82 micrograms/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. It blocks GAPDH/Siah1 which is a novel signaling pathway during the progression of spinal cord injury. Sivelestat could attenuate sepsis-related kidney injury in rats.
EBioMedicine. 2023 Aug 4;95:104739.
Neutrophil infiltration leads to fetal growth restriction by impairing the placental vasculature in DENV-infected pregnant mice
Sivelestat purchased from AbMole
| Molecular Weight | 434.46 |
| Formula | C20H22N2O7S |
| CAS Number | 127373-66-4 |
| Solubility (25°C) | DMSO ≥ 50 mg/mL |
| Storage | 2-8°C, dry, protect from light, sealed |
| Related Elastase Products |
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| Chrysophanol-8-O-β-D-glucopyranoside
Chrysophanol 8-O-glucoside is derived from the root of Rumex acetosa and has moderate elastase inhibitory activity. |
| GW311616
GW311616 is a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase(HNE) with IC50 of 22 nM and Ki value of 0.31 nM. |
| GW311616 hydrochloride
GW311616 HCl (GW311616A) is a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase(HNE) with IC50 of 22 nM. |
| Alvelestat (AZD9668)
Alvelestat (AZD9668) is an oral, highly selective inhibitor of neutrophil elastase (NE) with IC50 and Ki of 12 nM and 9.4 nM, at least 600-fold more selective over other serine proteases. |
| Sivelestat sodium tetrahydrate
Sivelestat sodium tetrahydrate is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM. Sivelestat (EI546) sodium tetrahydrate also inhibits leukocyte elastase obtained from rabbit, rat, hamster and mouse. |
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