Sivelestat sodium tetrahydrate

Category	SARS-CoV
CAS	201677-61-4
Description	Sivelestat is a competitive human neutrophil elastase (HNE) inhibitor (IC50 = 44 nM, Ki = 0.2 μM). It also inhibits leukocyte elastase obtained from rabbit, rat, hamster and mouse (IC50 = 19 to 49 nM). However, it does not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G even at 100 μM. In in-vivo studies, it suppressed lung hemorrhage in hamster (ID50 = 82 μg/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.

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Product Information

Synonyms	EI546 sodium tetrahydrate; EI 546 sodium tetrahydrate; EI-546 sodium tetrahydrate; LY544349 sodium tetrahydrate; LY 544349 sodium tetrahydrate; LY-544349 sodium tetrahydrate; ONO5046 sodium tetrahydrate; ONO 5046 sodium tetrahydrate; ONO-5046 sodium tetrahydrate
IUPAC Name	sodium;2-[[2-[[4-(2,2-dimethylpropanoyloxy)phenyl]sulfonylamino]benzoyl]amino]acetate;tetrahydrate
Molecular Weight	528.51
Molecular Formula	C20H29N2NaO11S
Canonical SMILES	CC(C)(C)C(=O)OC1=CC=C(C=C1)S(=O)(=O)NC2=CC=CC=C2C(=O)NCC(=O)[O-].O.O.O.O.[Na+]
InChI	InChI=1S/C20H22N2O7S.Na.4H2O/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);;4*1H2/q;+1;;;;/p-1
InChIKey	PLHREJBSQUSUCW-UHFFFAOYSA-M
Purity	>98%
Solubility	In vitro: 10 mM in DMSO
Appearance	White to off-white (Solid)
Application	Serine Proteinase Inhibitors
Storage	4°C, sealed storage, away from moisture * In solvent : -80°C, 6 months -20°C, 1 month (sealed storage, away from moisture)
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	187.00000
Target	Elastase; SARS-CoV