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
|Solubility (25°C)||DMSO ≥ 50 mg/mL|
|Storage||2-8°C, dry, protect from light, sealed|
|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.
|Related Elastase Products|
|Neutrophil elastase inhibitor 4
Neutrophil elastase inhibitor 4 is a competitive human neutrophil elastase (HNE) inhibitor (IC50: 42.30 nM, Ki: 8.04 nM).
Aristololactam IIIa exhibits significant inhibitory effects on superoxide anion generation and elastase release with IC50 values of 0.12 and 0.20 μg/mL, respectively.
KLK7/ELA2-IN-1 is a potent kallikrein-related peptidase 7 (KLK7) and epidermal elastase 2 (ELA2) inhibitor with IC50s of 6 nM and 55 nM, respectively.
Skullcapflavone I can be isolated from A. nallamalayana. Skullcapflavone I inhibits collagenase and elastase enzyme with IC50s of 106.74 μM and 186.70 μM. Skullcapflavone I has anticancer activities by down-regulating miR-23a.
Tutuilamide A is a potent porcine pancreatic elastase (PPE) inhibitor, with an IC50 of 1.2 nM. Tutuilamide A also inhibits human neutrophil elastase (HNE; IC50=0.73 nM) and kallikrein 7 (KLK7; IC50=5.0 nM).
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