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Cat. No. M9550
Sivelestat Structure

ONO5046; LY544349; EI546

Size Price Availability Quantity
10mg USD 70  USD70 In stock
25mg USD 150  USD150 In stock
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Quality Control & Documentation
Biological Activity

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.

Product Citations
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.


[1] Guofu Li, et al. Int J Mol Med. The Neutrophil Elastase Inhibitor, Sivelestat, Attenuates Sepsis-Related Kidney Injury in Rats

[2] S Hagiwara, et al. Inflamm Res. Neutrophil Elastase Inhibitor (Sivelestat) Reduces the Levels of Inflammatory Mediators by Inhibiting NF-kB

[3] K Kawabata, et al. Biochem Biophys Res Commun. ONO-5046, a Novel Inhibitor of Human Neutrophil Elastase

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Keywords: Sivelestat, ONO5046; LY544349; EI546 supplier, Elastase, inhibitors, activators

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