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Sivelestat sodium tetrahydrate

SKU: orb1705435

Description

Sivelestat sodium tetrahydrate (ONO-5046) is a potent and competitive inhibitor of human neutrophil elastase, exhibiting an IC50 of 44 nM and a Ki of 200 nM. This compound is a research tool for investigating conditions such as acute lung injury and ARDS, including in the context of COVID-19, with applications in both in vitro and in vivo experimental models.

Research Area

Infectious Disease & Virology, Protein Biochemistry

Images & Validation

Key Properties

CAS Number201677-61-4
MW528.51
Purity99.68% (May vary between batches)
FormulaC20H29N2NaO11S
SMILESO.O.O.O.[NaH].CC(C)(C)C(=O)Oc1ccc(cc1)S(=O)(=O)Nc1ccccc1C(=O)NCC(O)=O
TargetSARS-CoV,Serine Protease
Solubility10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (9.46 mM);DMSO:225 mg/mL (425.73 mM)

Bioactivity

In Vivo
Sivelestat (ONO-5046, 0.021-2.1 mg/kg, intratracheally) suppresses lung hemorrhage in hamsters (ID50 = 82 pg/kg) and increases skin capillary permeability in guinea pigs (ID50 = 9.6 mg/kg) via intravenous administration, both induced by human neutrophil elastase. Additionally, Sivelestat (10 mg/kg, tail vein infusion) ameliorates lung injury after hemorrhagic shock in rats, and prevents ischemia-reperfusion injury in the rat bladder (15, 60 mg/kg, ip).
In Vitro
Sivelestat (ONO-5046) is not an inhibitor of trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin, or cathepsin G, even at concentrations up to 100 μM. However, it effectively inhibits neutrophil elastase across various species, demonstrating IC50 values of 44 nM (human), 36 nM (rabbit), 19 nM (rat), 37 nM (hamster), and 49 nM (mouse), showcasing its specificity and potential for therapeutic applications.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Elaspol, Elaspol sodium, Elaspol sodium tetrahydrate, Elaspol sodium Tetrahydrate, ONO 5046, ONO5046 sodium, ONO-5046 sodium, ONO5046 sodium tetrahydrate, ONO5046 sodium Tetrahydrate, ONO-5046 sodium tetrahydrate, ONO-5046 sodium Tetrahydrate, ONO5046, ONO-5046, Neutrophil elastase (human), Serine Protease, SerineProtease, Sivelestat Sodium, Sivelestat sodium, Sivelestat Sodium Hydrate, Sivelestat sodium Tetrahydrate
Quality Guarantee

Quality Guarantee

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Key Properties

No computed properties available.

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Sivelestat sodium tetrahydrate (orb1705435)

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% DMSO +
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% Tween 80 +
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Available Sizes

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10 mg
$ 80.00
1 ml x 10 mM (in DMSO)
$ 90.00
25 mg
$ 120.00
50 mg
$ 190.00
100 mg
$ 250.00
200 mg
$ 350.00
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