Sivelestat sodium
Based on 33 publication(s) in Google Scholar
Sivelestat (EI546) sodium is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki 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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.77%
- CAS 番号: 150374-95-1
- 分子式: C20H21N2NaO7S
- 分子量:456.44
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
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Help & FAQs
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HY-15651
AlvelestatNeutrophil Elastase Inhibitor -
HY-136865
MeOSuc-AAPV-AMCElastase Fluorogenic Substrate -
HY-17443
SivelestatElastase Inhibitor -
HY-15891A
GW311616 hydrochlorideHNE Inhibitor -
HY-17443B
Sivelestat sodium tetrahydrateNeutrophil Elastase Inhibitor -
HY-12821
AEBSF hydrochlorideThrombin Inhibitor -
HY-15891
GW311616HNE Inhibitor -
HY-75957
DMP 777Elastase Inhibitor -
HY-15651R
Alvelestat (Standard)Reference Standard -
HY-103445
SSR69071Neutrophil Elastase Inhibitor -
HY-111457A
BAY-678 -
HY-19908
BAY-85-8501HNE Inhibitor
MedChemExpress（MCE）の使用を引用している文献 Sivelestat sodium
More- Cell Mol Immunol. 2026 Jul 17.
- Nat Commun. 2025 Feb 5;16(1):1378. [Abstract]
- Exp Mol Med. 2025 Sep;57(9):2067-2082. [Abstract]
- Exp Mol Med. 2024 Dec;56(12):2602-2616. [Abstract]
- Nucleic Acids Res. 2021 Jan 8;49(D1):D1113-D1121. [Abstract]
- Adv Sci (Weinh). 2026 Apr;13(24):e19500. [Abstract]
- J Exp Med. 2023 Sep 4;220(9):e20221751. [Abstract]
- J Neuroinflammation. 2025 Aug 26;22(1):206. [Abstract]
- Burns Trauma. 2021 Sep 17:9:tkab030. [Abstract]
- J Tissue Eng. 2025 Aug 19:16:20417314251348038. [Abstract]
- Biofabrication. 2021 Apr 8;13(3):10.1088/1758-5090/abe1cf. [Abstract]
- Hepatol Int. 2026 Jul 8.
- ACS Appl Mater Interfaces. 2026 Jun 25. [Abstract]
- Brain Behav Immun. 2024 Jun 12:120:403-412. [Abstract]
- JCI Insight. 2025 Dec 9:e193884. [Abstract]
- Ecotoxicol Environ Saf. 2023 Dec:268:115694. [Abstract]
- Cell Biosci. 2022 Jul 22;12(1):114. [Abstract]
- Int Immunopharmacol. 2025 Oct 10:163:115276. [Abstract]
- Cancers (Basel). 2022 Jan 20;14(3):515. [Abstract]
- J Cell Mol Med. 2022 Apr;26(7):2089-2103. [Abstract]
- iScience. 2025 Dec 5.
- FASEB J. 2024 Dec 15;38(23):e70238. [Abstract]
- J Infect Dis. 2024 May 15;229(5):1352-1365. [Abstract]
- J Hepatocell Carcinoma. 2021 May 20:8:451-465. [Abstract]
- PLoS One. 2025 Nov 6;20(11):e0336333. [Abstract]
- Res Sq. 2025 May 08.
- Res Sq. 2024 Jul 30.
- Heliyon. 2024 Oct 5;10(19):e38895. [Abstract]
- Research Square Preprint. 2023 Dec 11.
- Elife. 2022 Mar 23:11:e77444. [Abstract]
- Research Square Preprint. 2021 Aug.
- Research Square Preprint. 2021 Jun.
- Oxid Med Cell Longev. 2019 Nov 23:2019:7323986. [Abstract]
Customer Validation & Images
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Flow Cytometry
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In Vivo Efficacy Study
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In Vivo Imaging
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In Vivo Efficacy Study
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In Vivo Efficacy Study
生物活性
製品説明
体外実験
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 IC50 values of 44 nM, 36 nM, 19 nM, 37 nM and 49 nM for human, rabbit, rat, hamster and mouse neutrophil elastase, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
体内実験
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Golden hamsters, weighing 90 to 110 g[1].
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Dosage:0.021-2.1 mg/kg.
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Administration:Intratracheally five min before HNE injection.
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Result:Significantly and dosedependently suppressed the lung hemorrhage.
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Animal Model:Male Sprague-Dawley rats weighing 350-400 g[2].
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Dosage:10 mg/kg.
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Administration:Continuous infusion via the tail vein at 10 mg/kg/h for 60 min during the resuscitation phase.
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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.
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Animal Model:Male Sprague Dawley rats, 8 weeks old and weighing 250-320 g[3].
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Dosage:15 mg/kg or 60 mg/kg.
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Administration:IP.
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Result:Decreased the blood flow in the bladder during reperfusion phase compared to the IR group.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 150374-95-1
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性状 Solid
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分子量 456.44
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分子式 C20H21N2NaO7S
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Color White to off-white
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SMILES
CC(C)(C)C(OC1=CC=C(S(=O)(NC2=CC=CC=C2C(NCC(O[Na])=O)=O)=O)C=C1)=O
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別名
ONO5046-Na; Sodium sivelestat; EI546 sodium; LY544349 sodium
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (33)
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Journal Impact Factor
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Most Recent
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Nat Commun
Brd7 loss reawakens dormant metastasis initiating cells in lung by forging an immunosuppressive niche. [Abstract]2025 Feb 5;16(1):1378. PMID: 39910049
Sivelestat sodium purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 5;16(1):1378. [Abstract]
To evaluate this specific effect of NETosis in the Brd7-deficient context, we treated the mice injected with Brd7-KO cells with either Sivelestat (50 mg/kg) or DMSO starting at the 2-week timepoint, which marks the onset of lung metastatic outgrowth. FACS analysis of dissociated lungs isolated at the 4-week timepoint demonstrated a significant decrease in CTLA4 + CD8 + and PD1 + CD8 + T cells upon Sivelestat treatment.
Sivelestat sodium purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 5;16(1):1378. [Abstract]
To evaluate this specific effect of NETosis in the Brd7-deficient context, we treated the mice injected with Brd7-KO cells with either Sivelestat (50 mg/kg) or DMSO starting at the 2-week timepoint, which marks the onset of lung metastatic outgrowth.
Sivelestat sodium purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 5;16(1):1378. [Abstract]
The mice injected with the 4T07-TGL-Brd7 KO cells (Day 0) were i.p. injected with Sivelestat (50 mg/kg) or DMSO control on days -5,-3,-1,1 and on every alternate day thereafter until Week 4. Represent bioluminescence images for the indicated murine cohorts at 30 min, 1 week, and 4 weeks post tumor cell injection.
Sivelestat sodium purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 5;16(1):1378. [Abstract]
The mice injected with the 4T07-TGL-Brd7 KO cells (Day 0) were i.p. injected with Sivelestat (50 mg/kg) or DMSO control on days -5,-3,-1,1 and on every alternate day thereafter until Week 4. Line graph showing the normalized photon flux for the indicated murine cohorts over time.
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Exp Mol Med
Prolonged immune activation in post-acute sequelae of SARS-CoV-2: neutrophil dynamics and therapeutic insights. [Abstract]2025 Sep;57(9):2067-2082. PMID: 40987794
Sivelestat sodium purchased from MedChemExpress. Usage Cited in: Exp Mol Med. 2025 Sep;57(9):2067-2082. [Abstract]
Sivelestat treatment selectively modulates innate immune cell populations in lung and spleen. Data on weight change in the untreated group (infected with SARS-CoV-2 only) and the Sivelestat (10 mg/kg/day, 50 μL, intraperitoneally)/2% DMSO saline treatment group.
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Exp Mol Med
IL33-induced neutrophil extracellular traps (NETs) mediate a positive feedback loop for synovial inflammation and NET amplification in rheumatoid arthritis. [Abstract]2024 Dec;56(12):2602-2616. PMID: 39617790 -
Nucleic Acids Res
COVID19 Drug Repository: text-mining the literature in search of putative COVID19 therapeutics. [Abstract]2021 Jan 8;49(D1):D1113-D1121. PMID: 33166390 -
Adv Sci (Weinh)
Diabetes Mellitus Facilitates Gallstone Formation Through CXCR2-NETs-Mediated Liver-Bile Barrier Damage. [Abstract]2026 Apr;13(24):e19500. PMID: 41698066 -
J Exp Med
Neutrophil extracellular traps and extracellular histones potentiate IL-17 inflammation in periodontitis. [Abstract]2023 Sep 4;220(9):e20221751. PMID: 37261457 -
J Neuroinflammation
TLR9/NF-κB-mediated dendritic cell activation by neutrophil extracellular traps drives pathogenesis in experimental cerebral malaria. [Abstract]2025 Aug 26;22(1):206. PMID: 40859255 -
Burns Trauma
Neutrophil-derived heparin binding protein triggers vascular leakage and synergizes with myeloperoxidase at the early stage of severe burns (With video). [Abstract]2021 Sep 17:9:tkab030. PMID: 34646891 -
J Tissue Eng
Formation of neutrophil extracellular traps in the early stages exacerbate the healing process by regulating macrophage polarization in Achilles tendon-bone injury. [Abstract]2025 Aug 19:16:20417314251348038. PMID: 40843411 -
Biofabrication
A novel tumor-immune microenvironment (TIME)-on-Chip mimics three dimensional neutrophil-tumor dynamics and neutrophil extracellular traps (NETs)-mediated collective tumor invasion. [Abstract]2021 Apr 8;13(3):10.1088/1758-5090/abe1cf. PMID: 33524968 -
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ACS Appl Mater Interfaces
Ferritin Nanoparticle-Mediated Sustained Delivery of Sivelestat with Poor Water Affinity Attenuates Acute Lung Injury via Dual Inhibition of NETs and Pyroptosis. [Abstract]2026 Jun 25. PMID: 42348834 -
Brain Behav Immun
2024 Jun 12:120:403-412. PMID: 38871062 -
JCI Insight
Thrombomodulin protects against acute vascular and multiorgan injury in Sickle Cell disease. [Abstract]2025 Dec 9:e193884. PMID: 41364503 -
Ecotoxicol Environ Saf
2023 Dec:268:115694. PMID: 37984289 -
Cell Biosci
Neutrophil extracellular traps promote thrombogenicity in cerebral venous sinus thrombosis. [Abstract]2022 Jul 22;12(1):114. PMID: 35869501 -
Int Immunopharmacol
Mac-1/ICAM-1-dependent trogocytosis contributes to ICAM-1hi neutrophils-induced lung injury in traumatic brain injury. [Abstract]2025 Oct 10:163:115276. PMID: 40749609 -
Cancers (Basel)
2022 Jan 20;14(3):515. PMID: 35158784 -
J Cell Mol Med
CD44/ERM/F-actin complex mediates targeted nuclear degranulation and excessive neutrophil extracellular trap formation during sepsis. [Abstract]2022 Apr;26(7):2089-2103. PMID: 35146909 -
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FASEB J
Macrophage extracellular traps are induced by Mycoplasma bovis in bovine macrophages through NADPH oxidase/ROS-dependent manner and their antibacterial efficacy. [Abstract]2024 Dec 15;38(23):e70238. PMID: 39652064 -
J Infect Dis
2024 May 15;229(5):1352-1365. PMID: 38015657 -
J Hepatocell Carcinoma
The Crosstalk Between Cancer Cells and Neutrophils Enhances Hepatocellular Carcinoma Metastasis via Neutrophil Extracellular Traps-Associated Cathepsin G Component: A Potential Therapeutic Target. [Abstract]2021 May 20:8:451-465. PMID: 34046369 -
PLoS One
Xiao Qing Long Tang ameliorates neutrophil extracellular trap-dendritic cells-T helper 17 cell axis in Neutrophilic Asthma. [Abstract]2025 Nov 6;20(11):e0336333. PMID: 41196933 -
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Heliyon
The bacterial serine protease inhibitor ecotin inhibits neutrophil elastase enzymatic activity in cystic fibrosis sputa. [Abstract]2024 Oct 5;10(19):e38895. PMID: 39444402 -
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Elife
2022 Mar 23:11:e77444. PMID: 35294338 -
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Oxid Med Cell Longev
Neutrophil Elastase Inhibitors Suppress Oxidative Stress in Lung during Liver Transplantation. [Abstract]2019 Nov 23:2019:7323986. PMID: 31871555
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (219.09 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
プロトコル
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Inhalation Toxicity Study
Inhalation toxicity studies expose rodents to a controlled aerosol, vapor, gas, or smoke atmosphere and assess respiratory and systemic toxicity using exposure-atmosphere characterization, clinical observations, body and organ weights, bronchoalveolar lavage fluid, histopathology, blood chemistry, hematology, and, when included, molecular endpoints such as transcriptomics, proteomics, lipidomics, or tissue burden analysis. The primary biological readouts are airway irritation, pulmonary inflammation, cytotoxicity, altered surfactant or lipid homeostasis, impaired particle clearance, and tissue remodeling, reflected by BALF cell differentials, BALF protein, LDH, phosphatase activities, cytokines, lung weight, microscopic respiratory-tract lesions, and retained lung burden.
純度とドキュメンテーション
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データシート (277 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
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- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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取扱説明書 (2659 KB)
参考文献
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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 [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1909 mL | 10.9543 mL | 21.9087 mL | 54.7717 mL |
| 5 mM | 0.4382 mL | 2.1909 mL | 4.3817 mL | 10.9543 mL | |
| 10 mM | 0.2191 mL | 1.0954 mL | 2.1909 mL | 5.4772 mL | |
| 15 mM | 0.1461 mL | 0.7303 mL | 1.4606 mL | 3.6514 mL | |
| 20 mM | 0.1095 mL | 0.5477 mL | 1.0954 mL | 2.7386 mL | |
| 25 mM | 0.0876 mL | 0.4382 mL | 0.8763 mL | 2.1909 mL | |
| 30 mM | 0.0730 mL | 0.3651 mL | 0.7303 mL | 1.8257 mL | |
| 40 mM | 0.0548 mL | 0.2739 mL | 0.5477 mL | 1.3693 mL | |
| 50 mM | 0.0438 mL | 0.2191 mL | 0.4382 mL | 1.0954 mL | |
| 60 mM | 0.0365 mL | 0.1826 mL | 0.3651 mL | 0.9129 mL | |
| 80 mM | 0.0274 mL | 0.1369 mL | 0.2739 mL | 0.6846 mL | |
| 100 mM | 0.0219 mL | 0.1095 mL | 0.2191 mL | 0.5477 mL |
Sivelestat sodium 関連分類
HY-17443A 関連分類
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