Sivelestat sodium tetrahydrate (Synonyms: EI546 sodium tetrahydrate; LY544349 sodium tetrahydrate; ONO5046 sodium tetrahydrate) |
| رقم الكتالوجGC19523 |
Sivelestat sodium tetrahydrate is a specific inhibitor of neutrophil elastase with an IC50 value of 14nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 201677-61-4
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
Sivelestat sodium tetrahydrate is a specific inhibitor of neutrophil elastase with an IC50 value of 14nM[1]. Sivelestat sodium tetrahydrate has shown potential in the study of ischemia-reperfusion injury, acute respiratory distress syndrome and acute lung injury[2][3][5][6].
In vitro, sivelestat sodium tetrahydrate (0.1–1.0µg/mL) treated human umbilical vein endothelial cells (HUVEC) for 24, 48, or 72h inhibited the migration and adhesion of neutrophils to endothelial cells[2]. Sivelestat sodium tetrahydrate (50, 100µg/mL) treated TNF-α stimulated human pulmonary microvascular endothelial cells (HPMECs) for 24h enhanced cell viability and allievated oxidative stress and inflammatory response by Nrf2/HO-1 and JNK/NF-κB signaling pathways[3]. Sivelestat sodium tetrahydrate (0.1-1000µg/mL) incubated TMK‐1 gastric cancer cells for 24h shown to suppress cell growth by inhibiting the release of TGF-α stimulated by neutrophil elastase[4].
In vivo, sivelestat sodium tetrahydrate (100mg/kg) administrated intraperitoneally into murine model of ventilator-induced lung injury played a protective role against cell death in injured lungs by decreasing in JNK activity and Egr-1 mRNA expression that resulted in a decreased level of the inflammatory cytokines and a reduction in the number of apoptotic cells[5]. Sivelestat sodium tetrahydrate (150mg/kg) was administered via intraperitoneal injection in mouse model of renal ischemia-reperfusion injury 24 and 2h before surgery and every 12h thereafter. Sivelestat sodium tetrahydrate significantly reduced inflammation and oxidative stress, leading to decline in renal cell apoptosis and improved renal function [6].
References:
[1] Kawabata K, Suzuki M, Sugitani M, et al. ONO-5046, a novel inhibitor of human neutrophil elastase. Biochem Biophys Res Commun. 1991 Jun 14;177(2):814-20
[2] Wada Y, Yoshida K, Hihara J, et al. Sivelestat, a specific neutrophil elastase inhibitor, suppresses the growth of gastric carcinoma cells by preventing the release of transforming growth factor-alpha. Cancer Sci. 2006 Oct;97(10):1037-43.
[3] Zhang H, Zeng J, Li J K, et al. Sivelestat sodium attenuates acute lung injury by inhibiting JNK/NF-κB and activating Nrf2/HO-1 signaling pathways. Biomol Biomed. 2023 May 1;23(3):457-470.
[4] Sakai S, Tajima H, Miyashita T, et al. Sivelestat sodium hydrate inhibits neutrophil migration to the vessel wall and suppresses hepatic ischemia-reperfusion injury. Dig Dis Sci. 2014 Apr;59(4):787-94.
[5] Sakashita A, Nishimura Y, Nishiuma T, et al. Neutrophil elastase inhibitor (sivelestat) attenuates subsequent ventilator-induced lung injury in mice. Eur J Pharmacol. 2007 Sep 24;571(1):62-71.
[6] Liu Y Q, Xin Y, Yuan M Y,et al. Sivelestat sodium protects against renal ischemia/reperfusion injury by reduction of NETs formation.Arch Biochem Biophys. 2025 Mar:765:110318
| Cell experiment [1]: | |
Cell lines | TMK‐1 gastric cancer cells |
Preparation Method | TMK‐1 gastric carcinoma cells were seeded into 96‐well culture plates (5 × 103 cells/well) in RPMI containing 7% FBS, 2.0mM L‐glutamine, and 1% nonessential amino acids. Following 24h incubation in RPMI1640 medium with 5% FBS, the cells were incubated for 24, 48 or 72h at 37°C in a humidified atmosphere of 5% CO2 with varied concentrations (0.1–1.0µg/mL) of neutrophil elastase, or with varied concentrations (0.1–1000µg/mL) of sivelestat sodium tetrahydrate or with concentrations (10 and 100ng/mL) of anti‐TGF‐α antibody in the presence of 1µg/mL neutrophil elastase. |
Reaction Conditions | 0.1–1000µg/mL; 24, 48 or 72h |
Applications | Sivelestat sodium tetrahydrate not only inhibited the inflammatory response, but also inhibited the neutrophil elastase stimulated growth of the tumor. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | To the murine model of ventilator-induced lung injury, mice were anesthetized intraperitoneally (i.p.) with pentobarbital sodium (50mg/kg). After inserting a 22-gauge ventilation cannula into the trachea, the mice were placed in the supine position on a warming device and then connected to a ventilator. Then, the mice were injected with sivelestat sodium tetrahydrate (100mg/kg, i.p.) or saline (10ml/kg, i.p.) 30 min before ventilation to examine the inhibitory effect of neutrophil elastase inhibitor. |
Dosage form | 100mg/kg; i.p.; once |
Applications | Sivelestat sodium tetrahydrate suppressed subsequent neutrophilic inflammation induced by ventilator-induced lung injury with high VT ventilation. |
References: | |
| Cas No. | 201677-61-4 | SDF | |
| المرادفات | EI546 sodium tetrahydrate; LY544349 sodium tetrahydrate; ONO5046 sodium tetrahydrate | ||
| Canonical SMILES | [O-]C(CNC(C1=CC=CC=C1NS(C2=CC=C(OC(C(C)(C)C)=O)C=C2)(=O)=O)=O)=O.[Na+].O.O.O.O | ||
| Formula | C₂₀H₂₉N₂NaO₁₁S | M.Wt | 528.51 |
| الذوبان | DMF: 25 mg/ml,DMSO: 15 mg/ml,Ethanol: 0.3 mg/ml,PBS (pH 7.2): 2 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.8921 mL | 9.4606 mL | 18.9211 mL |
| 5 mM | 378.4 μL | 1.8921 mL | 3.7842 mL |
| 10 mM | 189.2 μL | 946.1 μL | 1.8921 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *