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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO ≥ 50 mg/mL|
|Storage||2-8°C, dry, protect from light, sealed|
|Related Elastase Products|
DMP 777 is a potent, selective, and orally active human leukocyte elastase (HLE) inhibitor.
BAY-85-8501 is a selective, reversible and potent inhibitor of Human Neutrophil Elastase (HNE), with an IC50 of 65 pM.
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.
GW311616 HCl (GW311616A) is a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase(HNE) with IC50 of 22 nM.
GW311616 is a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase(HNE) with IC50 of 22 nM.
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