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Sivelestat

Cat. No. M9550
Sivelestat Structure
Synonym:

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
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 434.46
Formula C20H22N2O7S
CAS Number 127373-66-4
Purity >98.5%
Solubility DMSO ≥ 50 mg/mL
Storage 2-8°C, dry, protect from light, sealed
References

[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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  Catalog
Abmole Inhibitor Catalog




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

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