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Sivelestat

Product Name
Sivelestat
CAS No.
127373-66-4
Chemical Name
Sivelestat
Synonyms
EI 546;CS-1329;Severus;ONO 5046;LY 544349;sivelestat;Sivelestate;Sivelestat RS;Sivelestat-d4;Sivelestat-d9
CBNumber
CB0511469
Molecular Formula
C20H22N2O7S
Formula Weight
434.46
MOL File
127373-66-4.mol
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Sivelestat Property

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
InChIKey
BTGNGJJLZOIYID-UHFFFAOYSA-N
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Safety

WGK Germany 
nwg
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
S7198
Product name
Sivelestat sodium salt hydrate
Purity
≥98% (HPLC), solid
Packaging
5mg
Price
$108
Updated
2024/03/01
Sigma-Aldrich
Product number
324759
Product name
Elastase Inhibitor IV
Packaging
1mg
Price
$113
Updated
2024/03/01
Sigma-Aldrich
Product number
S7198
Product name
Sivelestat sodium salt hydrate
Purity
≥98% (HPLC), solid
Packaging
25mg
Price
$445
Updated
2024/03/01
American Custom Chemicals Corporation
Product number
INB0000053
Product name
SIVELESTAT
Purity
95.00%
Packaging
5MG
Price
$501.96
Updated
2021/12/16
ApexBio Technology
Product number
B6189
Product name
Sivelestat(ONO-5046)
Packaging
200mg
Price
$558
Updated
2021/12/16
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Sivelestat Chemical Properties,Usage,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

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Sivelestat Suppliers

Changzhou Chenhong Biotechnology Co., Ltd.
Tel
0519-85788828 13775037613
Email
sales@chemrenpharm.com
Country
China
ProdList
3600
Advantage
58
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6005
Advantage
61
Adamas Reagent, Ltd.
Tel
400-6009262 16621234537
Fax
021-64823266
Email
chenyj@titansci.com
Country
China
ProdList
14103
Advantage
59
China Langchem Inc.
Tel
0086-21-58956006
Fax
0086-21-58956100
Country
China
ProdList
7811
Advantage
57
Hangzhou Yuhao Chemical Technology Co., Ltd
Tel
0571-82693216
Fax
+86-571-82880190
Email
info@yuhaochemical.com
Country
China
ProdList
9387
Advantage
52
S.Z. PhyStandard Bio-Tech. Co., Ltd.
Tel
0755-83725681-603
Fax
+86 755 28094224
Country
China
ProdList
4496
Advantage
50
MedChemexpress LLC
Tel
021-58955995
Fax
609-228-5909
Email
sales@medchemexpress.cn
Country
United States
ProdList
4861
Advantage
58
Bide Pharmatech Ltd.
Tel
400-164-7117 13681763483
Fax
+86-21-61629029
Email
product02@bidepharm.com
Country
China
ProdList
41462
Advantage
60
Shanghai DiBai Chemicals Co., Ltd.
Tel
021-54359730 400-008-9730
Fax
021-54353864
Email
info@chemxyz.com
Country
China
ProdList
3991
Advantage
60
Shanghai Macklin Biochemical Co.,Ltd.
Tel
15221275939 15221275939
Fax
021-50706099
Email
shenlinxing@macklin.cn
Country
China
ProdList
16166
Advantage
55
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View Lastest Price from Sivelestat manufacturers

Zhuozhou Wenxi import and Export Co., Ltd
Product
Sivelestat 127373-66-4
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-07-10
Zhuozhou Wenxi import and Export Co., Ltd
Product
Sivelestat 127373-66-4
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-07-09
Career Henan Chemical Co
Product
Sivelestat 127373-66-4
Price
US $1.00/KG
Min. Order
1KG
Purity
98%-99.9%
Supply Ability
200kg
Release date
2020-01-12

127373-66-4, SivelestatRelated Search:


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