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Sivelestat

Sivelestat Structure
Sivelestat structure
CAS No.
127373-66-4
Chemical Name:
Sivelestat
Synonyms
Sivelestat sodium salt hydrate;(2-((4-(Pivaloyloxy)phenyl)sulfonamido)benzoyl)glycine;EI 546;CS-1329;Severus;ONO 5046;LY 544349;sivelestat;Sivelestate;Sivelestat RS
CBNumber:
CB0511469
Molecular Formula:
C20H22N2O7S
Molecular Weight:
434.46
MDL Number:
MFCD00889071
MOL File:
127373-66-4.mol
MSDS File:
SDS
TDS File:
TDS
Last updated:2026-07-27 17:00:41
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Sivelestat Properties

Melting point 218-220°
Density 1.369±0.06 g/cm3(Predicted)
storage temp. Keep in dark place,Sealed in dry,2-8°C
solubility DMSO: soluble10mg/mL, clear
pka 3.67±0.10(Predicted)
form White to off-white solid
color white to off-white
InChI 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)
InChIKey BTGNGJJLZOIYID-UHFFFAOYSA-N
SMILES C(OC1=CC=C(S(NC2=CC=CC=C2C(NCC(O)=O)=O)(=O)=O)C=C1)(=O)C(C)(C)C
FDA UNII DWI62G0P59
UNSPSC Code 12352200
NACRES NA.77

SAFETY

Risk and Safety Statements

PPE Eyeshields, Gloves, type N95 (US)
WGK Germany  nwg
Storage Class 11 - Combustible Solids

Sivelestat price More Price(62)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich S7198 Sivelestat sodium salt hydrate ≥98% (HPLC), solid 127373-66-4 5mg $119 2026-04-30 Buy
Sigma-Aldrich 324759 Elastase Inhibitor IV 127373-66-4 1mg $105 2026-04-30 Buy
Biosynth FS170937 Sivelestat 127373-66-4 25mg $150 2026-06-04 Buy
Biosynth FS170937 Sivelestat 127373-66-4 10mg $150 2026-06-04 Buy
Biosynth FS170937 Sivelestat 127373-66-4 5mg $150 2026-06-04 Buy
Product number Packaging Price Buy
S7198 5mg $119 Buy
324759 1mg $105 Buy
FS170937 25mg $150 Buy
FS170937 10mg $150 Buy
FS170937 5mg $150 Buy

Sivelestat Chemical Properties, Uses, Production

Uses

Treatment of acute lung injury; acute respiratory distress syndrome (elastase inhibitor).

Uses

Sivelestat is an inhibitor of neutrophil elastase that prevents neutrophil extracellular trap formation and rescues mice from endotoxic shock. The inhibition of neutropil elastase by Sivelestat is a promising therapeutic strategy to inhibit glial scar and promote functional recovery by upregulating angiopoietin-1 after spinal cord injury.

Definition

ChEBI: Sivelestat is a N-acylglycine and a pivalate ester. It is functionally related to a N-benzoylglycine.

General Description

A cell-permeable, potent, substrate-competitive, and highly specific inhibitor of neutrophil elastase (IC50 = 19-49 nM using rat, rabbit, hamster, human, and mouse leukocyte elastase). Displays about 100-fold greater selectivity over pancreatic elastase (IC50 = 5.6 μM) and is inactive against trypsin, thrombin, plasmin, kallikrein, chymotrypsin, and cathepsin G even at concentrations as high as 100 μM. Effectively suppresses human neutrophil elastase-induced lung hemorrhage and skin capillary permeability in vivo. Also reported to inhibit mast cell Stat6-protease.

Biological Activity

sivelestat (ono-5046) is a neutrophil elastase inhibitor.human neutrophil elastase is a protease that hydrolyzes most connective tissue components, and it has been reported to participate in the tissue injury of rheumatoid arthritis, emphysema, adult respiratory distress syndrome as well as septic shock.

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.

in vitro

sivelestat was found to be able to competitively inhibit the human neutrophil elastase, and it could inhibit leukocyte elastase from rat, rabbit, mouse and hamster. whereas, sivelestat even at 100 microm could not inhibit thrombin, plasmin, trypsin, pancreas kallikrein, plasma kallikrein, chymotrypsin and cathepsin g [1].

in vivo

in animal study, 50 or 100 mg/kg sivelestat were immediately administered by i.p. injection after the surgical procedure to male sprague-dawley rats with bacterial infection caused by cecal ligation and puncture. results showed that in the untreated rats, the mean arterial pressure(map) and glomerular filtration rate(gfr) decreased, while serum blood urea nitrogen(bun) and neutrophil gelatinase-associated lipocalin(ngal) levels increased. sivelestat was found to promot the survival of the rats with sepsis, restored the impairment of map and gfr, and inhibited the increased bun and ngal levels. in addition, sivelestat could suppress the clp-induced macrophage infiltration in the rats [2].

IC 50

44 nm

References

[1] kawabata k,suzuki m,sugitani m,imaki k,toda m,miyamoto t. ono-5046, a novel inhibitor of human neutrophil elastase. biochem biophys res commun.1991 jun 14;177(2):814-20.
[2] li g,jia j,ji k,gong x,wang r,zhang x,wang h,zang b. the neutrophil elastase inhibitor, sivelestat, attenuates sepsis-related kidney injury in rats. int j mol med.2016 sep;38(3):767-75.
[3] aikawa n,kawasaki y. clinical utility of the neutrophil elastase inhibitor sivelestat for the treatment of acute respiratory distress syndrome. ther clin risk manag.2014 aug 5;10:621-9.

Sivelestat Preparation Products And Raw materials

Raw materials

Preparation Products

Sivelestat Suppliers

Global Suppliers ( 171)
Supplier Tel Email Country ProdList Advantage
Changzhou Chenhong Biotechnology Co., Ltd. +86-0519-85788828 +86-13775037613 sales@chemrenpharm.com China 4058 58
Hangzhou Xiao Bei Medical Technology Co., LTD +86-571-8526 3177 13962438025 beixi.dong@heryipharma.com China 196 58
Jiangsu Baiaoxinkang Pharmaceutical Technology Co. , Ltd. 18015077019 18015077019 jwang@bioscenepharma.com China 105 58
Lanzhou Dawnrays Pharmaceutical Co Ltd 0931-0931-4910898 19913936884 sales@dawnrays.com China 39 58
Chembest Research Laboratories Limited 021-20908456 sales@BioChemBest.com China 5996 61
Adamas Reagent, Ltd. 400-6009262 15618770481 yhx@titansci.com China 14098 59
China Langchem Inc. 0086-21-58956006 China 7798 57
BOC Sciences 1-631-485-4226; 16314854226 info@bocsci.com United States 9920 65
S.Z. PhyStandard Bio-Tech. Co., Ltd. 0755-83725681-603 China 4484 50
Shanghai Arbor Chemical Co., Ltd. 021-60451683 15021268886 sales@arborchemical.com China 837 55
Supplier Advantage
Changzhou Chenhong Biotechnology Co., Ltd. 58
Hangzhou Xiao Bei Medical Technology Co., LTD 58
Jiangsu Baiaoxinkang Pharmaceutical Technology Co. , Ltd. 58
Lanzhou Dawnrays Pharmaceutical Co Ltd 58
Chembest Research Laboratories Limited 61
Adamas Reagent, Ltd. 59
China Langchem Inc. 57
BOC Sciences 65
S.Z. PhyStandard Bio-Tech. Co., Ltd. 50
Shanghai Arbor Chemical Co., Ltd. 55

View Latest Price from Sivelestat manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Sivelestat pictures 2026-07-27 Sivelestat
127373-66-4
 $40.00-105.00 99.58% 10g TargetMol Chemicals Inc.
Sivelestat pictures 2021-07-13 Sivelestat
127373-66-4
 $10.00-15.00 1KG 99%+ HPLC Zhuozhou Wenxi import and Export Co., Ltd
Sivelestat pictures 2021-07-10 Sivelestat
127373-66-4
 $10.00-15.00 1KG 99%+ HPLC Zhuozhou Wenxi import and Export Co., Ltd
  • Sivelestat pictures
  • Sivelestat
    127373-66-4
  • $40.00-105.00
  • 99.58%
  • TargetMol Chemicals Inc.
  • Sivelestat pictures
  • Sivelestat
    127373-66-4
  • $10.00-15.00
  • 99%+ HPLC
  • Zhuozhou Wenxi import and Export Co., Ltd
  • Sivelestat pictures
  • Sivelestat
    127373-66-4
  • $10.00-15.00
  • 99%+ HPLC
  • Zhuozhou Wenxi import and Export Co., Ltd

Sivelestat Spectrum

Sivelestat(127373-66-4)1HNMR

127373-66-4 (Sivelestat) Related Search:

Oseltamivir Oseltamivir phosphate ULINASTATIN Dimethyl fumarate Diethoxydimethylsilane
Sulfuryl chloride Betahistine Diphenyl ether Benzoyl chloride Orlistat
Phenyl salicylate N,N-Dimethyl-1,4-phenylenediamine N,N-Dimethylformamide Aminoethoxyvinyl glycine hydrochloride Ethane
Phenyl valerate Benzoyl isocyanate Dimethylaminopyridine, polymer-bound

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Elastase Inhibitor IV - CAS 127373-66-4 - Calbiochem EI-546;LY-544349;ONO-5046 CS-1329 EI 546 sodium salt hydrate Elaspol sodium salt hydrate LY 544349 sodium salt hydrate o-(p-Hydroxybenzenesulfonamido)hippuric acid, pivalate (ester) sodium salt hydrate Ono-5046 sodium salt hydrate Sivelestat (ONO-5046) N-[2-{N'-(carboxy-methyl-)-amino-carbonyl-}-phenyl-]-4-t-butyl-carbonyl-oxy-benz-enesulfo-mide SIVELESTAT(ONO5046; LY544349; EI546) 2-[[2-[[4-(2,2-dimethylpropanoyloxy)phenyl]sulfonylamino]benzoyl]amino]acetic acid n-(2-(((4-(2,2-dimethyl-1-oxopropoxy)phenyl)sulfonyl)amino)benzoyl)glycine Sivelestate sodium Sivelestat(anhydrous, free acid) ONO 5046 2-[[2-[(4-pivaloyloxyphenyl)sulfonylamino]benzoyl]amino]acetic acid 2-[[2-[[4-(2,2-dimethylpropanoyloxy)phenyl]sulfonylamino]phenyl]carbonylamino]ethanoic acid Sivelestate Glycine, N-[2-[[[4-(2,2-diMethyl-1-oxopropoxy)phenyl]sulfonyl]aMino]benzoyl]- Sivelestat SodiuM anhydrous, free acid 2-{[2-({4-[(2,2-diMethylpropanoyl)oxy]benzene}sulfonaMido)phenyl]forMaMido}acetic acid EI 546 LY 544349 Sivelestat sodium Impurity sivelestat Sivelestat RS Propanoic acid, 2,2-dimethyl-, 4-[[[2-[[(carboxymethyl)amino]carbonyl]phenyl]amino]sulfonyl]phenyl ester Sivelestat-d4 Sivelestat-d9 2-[[2-[[4-(2,2-dimethylpropanoyloxy)phenyl]sulfonylamino]benzoyl]amino]aceticaci N-[2[[[4-(2,2-Dimethylpropanoyl)oxy]phenyl]sulfonyl)amino]benzoyl]glycine Severus Sivelestat, neutrophil elastase inhibitor Sivelestat, 10 mM in DMSO (2-((4-(Pivaloyloxy)phenyl)sulfonamido)benzoyl)glycine Sivelestat sodium salt hydrate 127373-66-4