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S7198

Sigma-Aldrich

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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$119.00
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About This Item

Empirical Formula (Hill Notation):
C20H22N2O7S · xNa+ · yH2O
CAS Number:
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

Quality Level

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

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This Item
M393561668T133
assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥95.0% (TLC), 95-102% anhydrous basis (corrected for sodium, T)

assay

≥98% (HPLC)

form

solid

form

powder

form

powder or solid

form

powder

Quality Level

100

Quality Level

-

Quality Level

100

Quality Level

100

storage temp.

room temp

storage temp.

room temp

storage temp.

2-8°C

storage temp.

-

solubility

DMSO: 10 mg/mL, clear

solubility

DMSO: 5 mg/mL, clear

solubility

-

solubility

H2O: soluble (storage of solutions for more than 8 hours at 4°C is not recommended.)

color

white to off-white

color

light yellow to dark yellow

color

-

color

light yellow

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_germany

nwg

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)


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Katja Herges et al.
Multiple sclerosis (Houndmills, Basingstoke, England), 18(4), 398-408 (2012-02-22)
The pathology of neuromyelitis optica (NMO), in contrast to multiple sclerosis, comprises granulocyte infiltrates along extensive lengths of spinal cord, as well as optic nerve. Furthermore, IFN-β treatment worsens NMO. We recently found that experimental autoimmune encephalomyelitis (EAE) induced with
Shuoqi Zhang et al.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 35(9), e21835-e21835 (2021-08-28)
Circulating neutrophil extracellular traps (NETs) resistant to t-PA have not been studied completely although NETs in thrombi may contribute to tissue plasminogen activator (t-PA) resistance. This research intended to elucidate whether circulating NETs are associated with t-PA resistance and the
Linshui Zhou et al.
Journal of cellular and molecular medicine, 24(20), 11998-12007 (2020-09-17)
The transition of alveolar type II epithelial cells into fibroblasts has been reported to cause and/or aggravate pulmonary fibrosis (PF), which is characterized by fibroblast proliferation, an enhanced production and accumulation of ECM (extracellular matrix), alveolar wall damage and functional
Biswajit Khatua et al.
Journal of leukocyte biology, 91(4), 641-655 (2012-01-14)
PA is an opportunistic pathogen that is commonly associated with severe infection in immunocompromised hosts. Siglec-9 binds with Sias by cis interaction on the neutrophil surface, thereby reducing immunological activity. However, neutrophils bind with pathogens through trans interactions of siglec-9
Naoya Fujino et al.
Experimental lung research, 38(1), 28-36 (2011-12-14)
Excess production of neutrophil elastase contributes to the pathogenesis of acute lung injury (ALI) and acute respiratory distress syndrome (ARDS). However, the role of neutrophil elastase in the repair process following ALI/ARDS is not well understood. The objective of this

Questions

  1. This compound can be used in in vitro assays targeting human neutrophil elastase as a positive control and is water-soluble?

    1 answer
    1. The solubility of this product is tested with DMSO at a concentration of 10 mg/mL. External sources also recommend using DMSO. A literature search indicates that this product has been utilized in in vitro assays targeting human neutrophil elastase as a positive control.

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