Sivelestat sodium tetrahydrate

製品コードS4666 バッチS466604

印刷

化学情報

Synonyms

Sivelestat sodium, ONO5046-Na, Sodium sivelestat, EI546 sodium, LY544349 sodium

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₀H₂₁N₂O₇S.4H₂O.Na

分子量

528.51

CAS No.

201677-61-4

Solubility (25°C)*

体外

DMSO

100 mg/mL (189.21 mM)

Ethanol

5 mg/mL (9.46 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	5.000mg/ml (9.46mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.830mg/ml (1.57mM)	Taking the 1 mL working solution as an example, add 50 μL of 16.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Sivelestat sodium tetrahydrate（ONO5046-Na、EI546、LY544349）はヒト好中球エラスターゼの競合阻害剤であり、ウサギ、ラット、ハムスター、マウス由来の白血球エラスターゼも阻害します。
in vitro	Sivelestat suppresses both adhesion and transmigration of neutrophils to the endothelium.
in vivo	Intraoperative administration of sivelestat effectively reduced neutrophil induction and activation in the lung and improved oxygenation after cardiopulmonary bypass in a piglet model.By inhibiting neutrophil elastase, sivelestat has a direct action to the accumulated and activated leucocytes, offering efficient protection against the production of oxygen radicals and cytokines.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	human umbilical vein endothelial cell (HUVEC)
	濃度	1, 10, and 50 μg/mL
	反応時間	1 h
	実験の流れ	HUVEC are grown to confluence on fibronectin (25 μg/mL) coated Falcon cell culture inserts. Neutrophils stimulated by PAF (0.1 mM) are added to the HUVEC monolayers (upper chamber). The upper chamber is exposed to 2 mL of HUMEDIA and rehydrated at 37 ℃ for 1 h in the absence or the presence (50 μg/mL) of sivelestat. Subsequently, the upper chamber is removed and the fluid in the lower chamber is collected.
動物実験	動物モデル	Neonatal piglets
	投薬量	2 mg/kg/h
	投与方法	Intraoperative administration

参考

https://pubmed.ncbi.nlm.nih.gov/18596053/
https://pubmed.ncbi.nlm.nih.gov/24318803/
https://pubmed.ncbi.nlm.nih.gov/20575981/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Sivelestat sodium alleviated sepsis-induced acute lung injury by inhibiting TGF-β/Smad signaling pathways through upregulating microRNA-744-5p [ J Thorac Dis, 2024, 16(10):6616-6633]	PubMed: 39552870
Inhibition of Efferocytosis by Extracellular CIRP-Induced Neutrophil Extracellular Traps [ J Immunol, 2021, 206(4):797-806]	PubMed: 33380498
Neutrophil extracellular traps amplify neutrophil recruitment and inflammation in neutrophilic asthma by stimulating the airway epithelial cells to activate the TLR4/ NF-κB pathway and secrete chemokines [ Aging (Albany NY), 2020, 12(17):16820-16836]	PubMed: 32756014
Identification of Small-Molecule Inhibitors of Brucella Diaminopimelate Decarboxylase by Using a High-Throughput Screening Assay. [ Front Microbiol, 2020, 10:2936]	PubMed: 32038511
Inhibition of Efferocytosis by Extracellular CIRP-Induced Neutrophil Extracellular Traps [ J Immunol, 2020, ji2000091]	PubMed: 33380498
Inhibitors of elastase stimulate murine B lymphocyte differentiation into IgG- and IgA-producing cells [ Eur J Immunol, 2018, 48(8):1295-1301]	PubMed: 29710424

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。