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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

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Product Name

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

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

assay

≥98% (HPLC)

form

solid

color

white to off-white

solubility

DMSO: 10 mg/mL, clear

storage temp.

room temp

Quality Level

100

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

11 - Combustible Solids

wgk

nwg

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)

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Certificates of Analysis (COA)

Lot/Batch Number
0000524799
0000524798
0000524798
0000524799
0000413436

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Surfactant protein D (SP-D), a pattern recognition molecule, is emerging as a potent anti-tumoural innate immune defense molecule in a range of cancers. Previously, SP-D expression was found to be significantly downregulated at the malignant sites of human prostate adenocarcinoma
Daniel Appelgren et al.
Cells, 9(1) (2019-12-28)
Neutrophils operate as part of the innate defence in the skin and may eliminate the Borrelia spirochaete via phagocytosis, oxidative bursts, and hydrolytic enzymes. However, their importance in Lyme neuroborreliosis (LNB) is unclear. Neutrophil extracellular trap (NET) formation, which is
Kenji Okada et al.
The Journal of thoracic and cardiovascular surgery, 144(1), 139-145 (2011-10-01)
Recent advancements in total aortic arch replacement achieved by our approach were presented. From January 2002 to December 2010, 321 consecutive patients (mean age 69.8 ± 13.3 years) underwent total arch replacement through a median sternotomy at our institute. Aortic
Seigo Miyoshi et al.
Drug design, development and therapy, 7, 305-316 (2013-04-19)
Neutrophil elastase plays a crucial role in the development of acute lung injury (ALI) in patients with systemic inflammatory response syndrome (SIRS). The clinical efficacy of the neutrophil elastase inhibitor, sivelestat, for patients with ALI associated with SIRS has not
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