Sivelestat

SKU: orb1226626

Description

A potent, specific and competitive inhibitor of human neutrophil elastase with IC50 of 44 nM; also inhibits leukocyte elastase obtained from rabbit, rat, hamster and mouse, do not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G (>10 uM); attenuates LPS-induced acute lung inflammation in the hamster.Other Indication Approved(In Vitro):Sivelestat (ONO-5046) does not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G even at 100 μM.Sivelestat (ONO-5046) exhibits IC50 values of 44 nM, 36 nM, 19 nM, 37 nM and 49 nM for human, rabbit, rat, hamster and mouse neutrophil elastase, respectively.(In Vivo):Sivelestat (ONO-5046, 0.021-2.1 mg/kg, intratracheally) suppresses lung hemorrhage in hamster (ID50 = 82 pg/kg) by intratracheal administration and increase of skin capillary permeability in guinea pig (ID50 = 9.6 mg/kg) by intravenous administration, both of which are induced by human neutrophil elastase.Sivelestat (10 mg/kg, infusion via the tail vein) ameliorates lung injury after hemorrhagic shock in rats.Sivelestat (15, 60 mg/kg, ip) prevents ischemia–reperfusion injury in the rat bladder.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 127373-66-4
• MW: 434.4629
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₂N₂O₇S
• SMILES: CC(C)(C)C(=O)OC1=CC=C(C=C1)S(=O)(=O)NC2=CC=CC=C2C(=O)NCC(=O)O
• Target: Elastase
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  Animal model: Male Golden hamsters, weighing 90 to 110 g. Dosage: 0.021-2.1 mg/kg. Administration: Intratracheally five min before HNE injection. Result: Significantly and dosedependently suppressed the lung hemorrhage. Animal model: Male Sprague-Dawley rats weighing 350-400 g. Dosage: 10 mg/kg. Administration: Continuous infusion via the tail vein at 10 mg/kg/h for 60 min during the resuscitation phase. Result: Greatly suppressed lung injury, as revealed by the reduced histological damage. Significantly ameliorated HSR-induced lung injury. Markedly decreased the levels of TNF-α and iNOS gene. Animal model: Male Sprague Dawley rats, 8 weeks old and weighing 250-320 g. Dosage: 15 mg/kg or 60 mg/kg. Administration: IP. Result: Decreased the blood flow in the bladder during reperfusion phase compared to the IR group.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

EI-546 | LY-544349 | ONO-5046

Quick Database Links

Gene Symbol

Elastase