Sivelestat sodium

SKU: orb1705069

Description

Sivelestat sodium is a potent and selective human neutrophil elastase inhibitor. It has been shown to ameliorate sepsis-induced myocardial dysfunction in research models by activating the PI3K/AKT/mTOR pathway, supporting its investigation for conditions like acute lung injury and acute respiratory distress syndrome.

Research Area

Infectious Disease & Virology, Protein Biochemistry

Images & Validation

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Key Properties

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CAS Number	150374-95-1
MW	456.45
Formula	C₂₀H₂₁N₂NaO₇S
SMILES	O=C(CNC(C1=C(NS(=O)(C2=CC=C(C=C2)OC(C(C)(C)C)=O)=O)C=CC=C1)=O)[O-].[Na+]
Target	Serine Protease,SARS-CoV
Solubility	H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.23 mM);DMSO:80 mg/mL (175.27 mM)

Bioactivity

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Target IC50	Neutrophil elastase (mouse):49 nM\|Neutrophil elastase (human):44 nM\|Neutrophil elastase (human):200 nM (Ki)\|Neutrophil elastase (rabbit):36 nM\|Neutrophil elastase (hamster):37 nM\|Neutrophil elastase (rat):19 nM Read more...
In Vivo	By intratracheal administration (0.021-2.1 mg/kg), Sivelestat sodium was able to effectively inhibit hamster lung hemorrhage induced by human neutrophil elastase (ID50 = 82 pg/kg), as well as the increase in guinea pig skin capillary permeability caused by i.v. administration (ID50 = 9.6 mg/kg). Sivelestat sodium (10 mg/kg via tail vein infusion) ameliorated lung injury due to hemorrhagic shock in rats. Sivelestat sodium was able to prevent ischemia-reperfusion injury in the bladder of rats by intraperitoneal injection (15 mg/kg and 60 mg/kg). Read more...
In Vitro	Sivelestat sodium, a competitive inhibitor of human neutrophil elastase, has a Ki value of 200 nM, and does not inhibit trypsin, thrombin, fibrinolytic enzymes, plasma kallikrein-releasing enzyme, pancreatic kallikrein-releasing enzyme, chytolysin, or histone G, even at concentrations up to 100 μM. The IC50 values of Sivelestat sodium on neutrophil elastase in different species are 44 nM in humans, 36 nM in rabbits, 19 nM in rats, 37 nM in hamsters, and 49 nM in mice. Read more...

Storage & Handling

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Storage	store at low temperature,keep away from direct sunlight \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Sivelestat sodium, Sivelestat sodium salt, EI546 sodium, EI 546 sodium, LY 544349, LY544349, LY-544349, LY544349 sodium, LY-544349 sodium, ONO5046, ONO-5046, ONO5046 sodium, ONO 5046, ONO 5046 sodium

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Compound Identifiers

PubChem CID

23664980 ↗

Key Properties

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No computed properties available.

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