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Key Documents

S7198

Sigma-Aldrich

Sivelestat sodium salt hydrate

≥98% (HPLC), solid

Synonyme(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

Formule empirique (notation de Hill):
C20H22N2O7S · xNa+ · yH2O
Numéro CAS:
Poids moléculaire :
434.46 (anhydrous free acid basis)
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

Pureté

≥98% (HPLC)

Forme

solid

Couleur

white to off-white

Solubilité

DMSO: 10 mg/mL, clear

Température de stockage

room temp

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)

Clé InChI

BTGNGJJLZOIYID-UHFFFAOYSA-N

Application

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

Actions biochimiques/physiologiques

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.

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

nwg

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Équipement de protection individuelle

Eyeshields, Gloves, type N95 (US)


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Lymphatic vasculature critically depends on the connections of lymphatic endothelial cells with the extracellular matrix (ECM), which are mediated by anchoring filaments (AFs). The ECM protein EMILIN1 is a component of AFs and is involved in the regulation of lymphatic
Shigehiro Tsujii et al.
World journal of surgery, 36(5), 1122-1127 (2012-03-01)
The effects of sivelestat on endotoxin-induced lung injury, postperfusion lung injury, and ischemia-reperfusion are known, yet the benefits of sivelestat during liver surgery have yet to be elucidated. The aim of the present study was to assess the effects of
Y Nakajima et al.
Journal of perinatology : official journal of the California Perinatal Association, 32(6), 466-468 (2012-05-31)
Intrauterine infection and inflammation are recognized as major contributors to the onset of preterm labor. We describe two cases of severe preterm labor with bulging membrane that were treated by intravenous injection of Sivelestat, a neutrophil elastase inhibitor. Ritodrine hydrochloride
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
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

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