Nafamostat mesilate (FUT-175)

製品コードS1386 バッチS138604

印刷

化学情報

Synonyms

Storage
(From the date of receipt)

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

化学式

C₁₉H₁₇N₅O₂.2CH₄O₃S

分子量

539.58

CAS No.

82956-11-4

Solubility (25°C)*

体外

DMSO

100 mg/mL (185.32 mM)

Water

33 mg/mL (61.15 mM)

Ethanol

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.

* <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	Nafamostat mesilate (FUT-175)は、血液透析時の抗凝固剤として使用される合成serine protease阻害剤です。Nafamostat mesylateはSARS-CoV-2の活性化を阻害し、COVID-19の新しい治療選択肢として研究されています。Nafamostat Mesilateは炎症とapoptosisを軽減します。
in vitro	Nafamostat mesilate (FUT-175) significantly inhibits the release of platelet beta-thromboglobulin (beta TG) at 60 and 120 min. It prevents any significant release of neutrophil elastase; at 120 min, plasma elastase-alpha 1-antitrypsin complex is 0.16 mg/mL in the NM group and 1.24 mg/mL in the control group. This compound completely inhibits formation of complexes of C1 inhibitor with kallikrein and FXIIa. It inhibits several proteases which may be importantly involved in the pathophysiology of disseminated intravascular coagulation (DIC). Nafamostat mesilate inhibits extrinsic pathway activity (TF-F.VIIa mediated-F.Xa generation) in a concentration dependent manner with IC50 of 0.1 μM. It produces concentration-dependent inhibition of the initial-phase transient component of biphasic ASIC3 currents with an IC50 value of approximately 2.5 mM.
in vivo	Nafamostat mesilate (FUT-175) (10 mg/kg) inhibits scratching induced by tryptase but not by histamine and serotonin. It (1-10 mg/kg) produces the dose-dependent inhibition of scratching induced by intradermal compound 48/80 (10 mg/site). This compound (10 mg/kg) suppresses tryptase activity in the mouse skin. It inhibits gemcitabine-induced NF-kappaB activation, enhances apoptosis by gemcitabine and suppresses pancreatic tumor growth. When combined with Gemcitabine, it improves the body weight loss of mice induced by Gemicitabine.

製品説明

Nafamostat mesilate (FUT-175)は、血液透析時の抗凝固剤として使用される合成serine protease阻害剤です。Nafamostat mesylateはSARS-CoV-2の活性化を阻害し、COVID-19の新しい治療選択肢として研究されています。Nafamostat Mesilateは炎症とapoptosisを軽減します。

in vitro

Nafamostat mesilate (FUT-175) significantly inhibits the release of platelet beta-thromboglobulin (beta TG) at 60 and 120 min. It prevents any significant release of neutrophil elastase; at 120 min, plasma elastase-alpha 1-antitrypsin complex is 0.16 mg/mL in the NM group and 1.24 mg/mL in the control group. This compound completely inhibits formation of complexes of C1 inhibitor with kallikrein and FXIIa.

It inhibits several proteases which may be importantly involved in the pathophysiology of disseminated intravascular coagulation (DIC). Nafamostat mesilate inhibits extrinsic pathway activity (TF-F.VIIa mediated-F.Xa generation) in a concentration dependent manner with IC50 of 0.1 μM.

It produces concentration-dependent inhibition of the initial-phase transient component of biphasic ASIC3 currents with an IC50 value of approximately 2.5 mM.

in vivo

Nafamostat mesilate (FUT-175) (10 mg/kg) inhibits scratching induced by tryptase but not by histamine and serotonin. It (1-10 mg/kg) produces the dose-dependent inhibition of scratching induced by intradermal compound 48/80 (10 mg/site). This compound (10 mg/kg) suppresses tryptase activity in the mouse skin.

It inhibits gemcitabine-induced NF-kappaB activation, enhances apoptosis by gemcitabine and suppresses pancreatic tumor growth. When combined with Gemcitabine, it improves the body weight loss of mice induced by Gemicitabine.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	NCM460 cells
	濃度	5 μM
	反応時間	24 h
	実験の流れ	Cells were treated with Nafamostat mesilate (FUT-175) at the indicated concentration for 24 h.
動物実験	動物モデル	Male ICR-SCID nude mice
	投薬量	30 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/8713783/
https://pubmed.ncbi.nlm.nih.gov/8029816/
https://pubmed.ncbi.nlm.nih.gov/17826743/

https://pubmed.ncbi.nlm.nih.gov/16359660/
https://pubmed.ncbi.nlm.nih.gov/19661331/
https://pubmed.ncbi.nlm.nih.gov/32312781/
https://pubmed.ncbi.nlm.nih.gov/35974017/

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カスタマーフィードバック

: , , Cancer Lett, 2016, 380(1):87-97.

: Data from [Data independently produced by , , Med Oncol, 2016, 33(5):53]

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：

Propafenone facilitates mitochondrial-associated ferroptosis and synergizes with immunotherapy in melanoma [ J Immunother Cancer, 2024, 12(11)e009805]	PubMed: 39581704
Decoding the mechanisms of chimeric antigen receptor (CAR) T cell-mediated killing of tumors: insights from granzyme and Fas inhibition [ Cell Death Dis, 2024, 15(2):109]	PubMed: 38307835
Evidences of neurological injury caused by COVID-19 from glioma tissues and glioma organoids [ CNS Neurosci Ther, 2024, 30(6):e14822]	PubMed: 38923860
Generation of a Porcine Cell Line Stably Expressing Pig TMPRSS2 for Efficient Isolation of Swine Influenza Virus [ Pathogens, 2023, 13(1)18]	PubMed: 38251326
Mannose ameliorates experimental colitis by protecting intestinal barrier integrity [ Nat Commun, 2022, 13(1):4804]	PubMed: 35974017
The IDentif.AI-x pandemic readiness platform: Rapid prioritization of optimized COVID-19 combination therapy regimens [ NPJ Digit Med, 2022, 5(1):83]	PubMed: 35773329
Delayed administration of nafamostat mesylate inhibits thrombin-mediated blood-spinal cord barrier breakdown during acute spinal cord injury in rats [ J Neuroinflammation, 2022, 19(1):189]	PubMed: 35842640
Coagulation factors directly cleave SARS-CoV-2 spike and enhance viral entry [ Elife, 2022, 11e77444]	PubMed: 35294338
The Effect of Serine Protease Inhibitors on Visceral Pain in Different Rodent Models With an Intestinal Insult [ Front Pharmacol, 2022, 13:765744]	PubMed: 35721192
Identification of nafamostat mesylate as a selective stimulator of NK cell IFN-γ production via metabolism-related compound library screening [ Immunol Res, 2022, 1-11]	PubMed: 35167033

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。