[CAS NO. 150374-95-1] Sivelestatsodium
PRODUCTS SPECIFICATIONS [150374-95-1]
DESCRIPTION [150374-95-1]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 456.44 |
| Molecular Formula | C20H21N2NaO7S |
| SMILES | CC(C)(C)C(OC1=CC=C(S(=O)(NC2=CC=CC=C2C(NCC(O[Na])=O)=O)=O)C=C1)=O |
10 Publications Citing Use of MCE
- [1]Nucleic Acids Res. 2021 Jan 8;49(D1):D1113-D1121.
- [2]Biofabrication. 2021 Feb 1.
- [3]Cancers (Basel). 2022, 14(3), 515.
- [4]Oxid Med Cell Longev. 2019 Nov 23;2019:7323986.
- [5]Cell Biosci. 2022 Jul 22;12(1):114.
- [6]J Cell Mol Med. 2022 Feb 11.
- [7]Burns Trauma. 17 September 2021.
- [8]Research Square Preprint. 2021 Aug.
- [9]Research Square Preprint. 2021 Jun.
- [10]J Hepatocell Carcinoma. 2021 May 20;8:451-465.
Summary
Sivelestat (EI546) sodium is a competitive inhibitor of human neutrophil elastase , with an IC 50 of 44 nM and a K i of 200 nM. Sivelestat (EI546) sodium has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19 [1] [2] [3] [4] .
In Vitro
Sivelestat (ONO-5046) does not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G even at 100 μM
[1]
.
Sivelestat (ONO-5046) exhibits IC
50
values of 44 nM, 36 nM, 19 nM, 37 nM and 49 nM for human, rabbit, rat, hamster and mouse neutrophil elastase, respectively
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Sivelestat (ONO-5046, 0.021-2.1 mg/kg, intratracheally) suppresses lung hemorrhage in hamster (ID
50
= 82 pg/kg) by intratracheal administration and increase of skin capillary permeability in guinea pig (ID
50
= 9.6 mg/kg) by intravenous administration, both of which are induced by human neutrophil elastase
[1]
.
Sivelestat (10 mg/kg, infusion via the tail vein) ameliorates lung injury after hemorrhagic shock in rats
[2]
.
Sivelestat (15, 60 mg/kg, ip) prevents ischemia–reperfusion injury in the rat bladder
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male Golden hamsters, weighing 90 to 110 g [1] . |
| Dosage: | 0.021-2.1 mg/kg. |
| Administration: | Intratracheally five min before HNE injection. |
| Result: | Significantly and dosedependently suppressed the lung hemorrhage. |
| Animal Model: | Male Sprague-Dawley rats weighing 350-400 g [2] . |
| Dosage: | 10 mg/kg. |
| Administration: | Continuous infusion via the tail vein at 10 mg/kg/h for 60 min during the resuscitation phase. |
| Result: |
Greatly suppressed lung injury, as revealed by the reduced histological damage.
Significantly ameliorated HSR-induced lung injury. Markedly decreased the levels of TNF-α and iNOS gene. |
| Animal Model: | Male Sprague Dawley rats, 8 weeks old and weighing 250-320 g [3] . |
| Dosage: | 15 mg/kg or 60 mg/kg. |
| Administration: | IP. |
| Result: | Decreased the blood flow in the bladder during reperfusion phase compared to the IR group. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00036062 | Eli Lilly and Company |
Respiratory Distress Syndrome, Adult|Acute Lung Injury
|
August 2001 | Phase 1|Phase 2 |
| NCT01170845 | Yokohama City University Medical Center |
Esophageal Cancer
|
March 2007 | Not Applicable |
| NCT04909697 | Sichuan Provincial People´s Hospital |
Acute Respiratory Distress Syndrome
|
April 18, 2022 | Phase 4 |
| NCT00219375 | Ono Pharmaceutical Co. Ltd |
Acute Lung Injury|Systemic Inflammatory Response Syndrome
|
June 2004 | Phase 4 |
| NCT04973670 | Southeast University, China |
ARDS
|
October 11, 2021 | Phase 3 |
| NCT05020210 | Nanfang Hospital of Southern Medical University|Shenzhen Hospital of Southern Medical University|Guangdong No.2 Provincial People´s Hospital|Foshan Hospital of Traditional Chinese Medicine |
ARDS|Inflammatory Response
|
August 30, 2021 | |
| NCT05343338 | First Affiliated Hospital Xi´an Jiaotong University |
Aortic Dissection|Acute Lung Injury+Acute Respiratory Distress Syndrome (ARDS)
|
April 20, 2022 | Not Applicable |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL ( 219.09 mM ; Need ultrasonic)
H 2 O : 1 mg/mL ( 2.19 mM ; ultrasonic and warming and heat to 80°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.1909 mL | 10.9543 mL | 21.9087 mL |
| 5 mM | 0.4382 mL | 2.1909 mL | 4.3817 mL |
| 10 mM | 0.2191 mL | 1.0954 mL | 2.1909 mL |
References
- [1] Kawabata K, et al. ONO-5046, a novel inhibitor of human neutrophil elastase. Biochem Biophys Res Commun. 1991 Jun 14;177(2):814-20.
- [2] Yuichiro Toda, et al. A neutrophil elastase inhibitor, sivelestat, ameliorates lung injury after hemorrhagic shock in rats. Int J Mol Med. 2007 Feb;19(2):237-43.
- [3] Tomoharu Kono, et al. Neutrophil elastase inhibitor, sivelestat sodium hydrate prevents ischemia-reperfusion injury in the rat bladder. Mol Cell Biochem. 2008 Apr;311(1-2):87-92.
- [4] Adeleh Sahebnasagh, et al. Neutrophil elastase inhibitor (sivelestat) may be a promising therapeutic option for management of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19. J Clin Pharm Ther. 2
Synonyms