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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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