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Merck
CN

S7198

Sivelestat sodium salt hydrate

≥98% (HPLC), HNE inhibitor, solid

Synonym(s):

EI 546 sodium salt hydrate, Elaspol sodium salt hydrate, LY 544349 sodium salt hydrate, Ono-5046 sodium salt hydrate, o-(p-Hydroxybenzenesulfonamido)hippuric acid, pivalate (ester) sodium salt hydrate

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About This Item

Empirical Formula (Hill Notation):
C20H22N2O7S · xNa+ · yH2O
CAS Number:
127373-66-4
Molecular Weight:
434.46 (anhydrous free acid basis)
UNSPSC Code:
12352200
NACRES:
NA.77

Key Documents

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Product Name

Sivelestat sodium salt hydrate, ≥98% (HPLC), solid

Quality Level

100

Assay

≥98% (HPLC)

form

solid

color

white to off-white

solubility

DMSO: 10 mg/mL, clear

storage temp.

room temp

SMILES string

[S](=O)(=O)(Nc2c(cccc2)C(=O)NCC(=O)O)c1ccc(cc1)OC(=O)C(C)(C)C

InChI

1S/C20H22N2O7S/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)

InChI key

BTGNGJJLZOIYID-UHFFFAOYSA-N

Related Categories

Application

Sivelestat sodium salt hydrate may be used to inhibit human neutrophil elastase-mediated cell signaling.

Biochem/physiol Actions

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.
Sivelestat is a competitive human neutrophil elastase (HNE) inhibitor.

Storage Class Code

11 - Combustible Solids

WGK

nwg

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Personal Protective Equipment

dust mask type N95 (US), Eyeshields, Gloves

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Certificates of Analysis (COA)

Lot/Batch Number
0000413436
0000413436
0000413437
0000413437
0000405016

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