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Sivelestat sodium

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Category SARS-CoV
CAS 150374-95-1
Description Sivelestat sodium(ONO5046; LY544349; EI546) is a competitive inhibitor of human neutrophil elastase(IC50 = 44 nM; Ki=200 nM); also inhibited leukocyte elastase obtained from rabbit, rat, hamster and mouse.
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Product Information

Synonyms Sivelestat sodium
IUPAC Name sodium;2-[[2-[[4-(2,2-dimethylpropanoyloxy)phenyl]sulfonylamino]benzoyl]amino]acetate
Molecular Weight 456.44
Molecular Formula C20H21N2NaO7S
Canonical SMILES CC(C)(C)C(=O)OC1=CC=C(C=C1)S(=O)(=O)NC2=CC=CC=C2C(=O)NCC(=O)[O-].[Na+]
InChI InChI=1S/C20H22N2O7S.Na/c1-20(2,3)19(26)29-13-8-10-14(11-9-13)30(27,28)22-16-7-5-4-6-15(16)18(25)21-12-17(23)24;/h4-11,22H,12H2,1-3H3,(H,21,25)(H,23,24);/q;+1/p-1
InChIKey ZAIFANJZUGNYCK-UHFFFAOYSA-M
Purity >98%
Solubility In vitro:
10 mM in DMSO
Appearance White to off-white (Solid)
Storage 4°C, sealed storage, away from moisture
* In solvent :
-80°C, 6 months
-20°C, 1 month (sealed storage, away from moisture)
Complexity 738
Exact Mass 528.13897520
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.
PSA 150.08000
Target Elastase; SARS-CoV

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