Nafamostat mesilate (FUT-175)

製品コードS1386 バッチS138606

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	100 mg/mL (185.32 mM)
		Ethanol	Insoluble
* <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) is a synthetic serine protease inhibitor, used as an anticoagulant during hemodialysis. Nafamostat mesylate blocks activation of SARS-CoV-2 and is investigated as a new treatment option for COVID-19. Nafamostat Mesilate attenuates inflammation and apoptosis.
in vitro	Nafamostat mesilate significantly inhibits the release of platelet beta-thromboglobulin (beta TG) at 60 and 120 min. Nafamostat mesilate (NM) 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. Nafamostat mesilate completely inhibits formation of complexes of C1 inhibitor with kallikrein and FXIIa. ^[1] Nafamostat mesilate 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. ^[2] Nafamostat mesilate produces concentration-dependent inhibition of the initial-phase transient component of biphasic ASIC3 currents with an IC50 value of approximately 2.5 mM. ^[3]
in vivo	Nafamostat mesilate (10 mg/kg) inhibits scratching induced by tryptase but not by histamine and serotonin. Nafamostat mesilate (1-10 mg/kg) produces the dose-dependent inhibition of scratching induced by intradermal compound 48/80 (10 mg/site). Nafamostat mesilate (10 mg/kg) suppresses tryptase activity in the mouse skin. ^[4] Nafamostat mesilate inhibits gemcitabine-induced NF-kappaB activation, enhances apoptosis by gemcitabine and suppresses pancreatic tumor growth. Nafamostat mesilate combined with Gemcitabine improves the body weight loss of mice induced by Gemicitabine. ^[5]

製品説明

Nafamostat mesilate (FUT-175) is a synthetic serine protease inhibitor, used as an anticoagulant during hemodialysis. Nafamostat mesylate blocks activation of SARS-CoV-2 and is investigated as a new treatment option for COVID-19. Nafamostat Mesilate attenuates inflammation and apoptosis.

in vitro

Nafamostat mesilate significantly inhibits the release of platelet beta-thromboglobulin (beta TG) at 60 and 120 min. Nafamostat mesilate (NM) 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. Nafamostat mesilate completely inhibits formation of complexes of C1 inhibitor with kallikrein and FXIIa. ^[1]

Nafamostat mesilate 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. ^[2]

Nafamostat mesilate produces concentration-dependent inhibition of the initial-phase transient component of biphasic ASIC3 currents with an IC50 value of approximately 2.5 mM. ^[3]

in vivo

Nafamostat mesilate (10 mg/kg) inhibits scratching induced by tryptase but not by histamine and serotonin. Nafamostat mesilate (1-10 mg/kg) produces the dose-dependent inhibition of scratching induced by intradermal compound 48/80 (10 mg/site). Nafamostat mesilate (10 mg/kg) suppresses tryptase activity in the mouse skin. ^[4]

Nafamostat mesilate inhibits gemcitabine-induced NF-kappaB activation, enhances apoptosis by gemcitabine and suppresses pancreatic tumor growth. Nafamostat mesilate combined with Gemcitabine improves the body weight loss of mice induced by Gemicitabine. ^[5]

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 indicated concentration of drug 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

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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。

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