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Nafamostat mesilate (FUT-175) Serine Protease inhibitor

Name: Nafamostat mesilate (FUT-175)
Brand: Selleck Chemicals
SKU: S1386
Rating: 5 (20 reviews)

Cat.nr.: S1386

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

Nafamostat mesilate (FUT-175) Serine Protease inhibitor Chemical Structure

Chemische structuur

Molecuulgewicht: 539.58

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.81%

99.81

Gerelateerde doelwitten	HDAC Caspase Proteasome Secretase MMP HCV Protease Cysteine Protease Tyrosinase HIV Protease DPP
Overig Serine Protease Inhibitoren	Leupeptin Hemisulfate PMSF AEBSF HCl Alvelestat (AZD9668) Gabexate Mesylate Sivelestat sodium tetrahydrate Sivelestat sodium UK-371804 HCl Fulacimstat ZK824859

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)

Cellijnen	Assaytype	Incubatietijd	Activiteitsbeschrijving	PMID
NS0	Function assay	15 mins	Inhibition of recombinant C-terminal His10-tagged human Hepsin (R45 to L17 residues) D161E/ R162K double mutant expressed in mouse NS0 cells using Boc-QRR-AMC as substrate after 15 mins by automated fluorescence assay, IC50=0.005μM.	29701962
Sf9	Function assay	30 mins	Inhibition of recombinant N-terminal His-tagged HGFA (unknown origin) expressed in baculovirus-infected Sf9 cells using Boc-QLR-AMC as substrate incubated for 30 mins prior to substrate addition by fluorescence assay, Ki=0.025μM.	25882520
Sf9	Function assay	30 mins	Inhibition of recombinant N-terminal His-tagged HGFA (unknown origin) expressed in baculovirus-infected Sf9 cells incubated for 30 mins prior to cromogenic substrate addition by spectrophotometry, IC50=0.15μM.	25882520
MDA-MB-231	Function assay	15 mins	Inhibition of HGFA in human MDA-MB-231 cells assessed as inhibition of c-MET phosphorylation after 15 mins by immunoblotting, EC50=0.49μM.	25408834
Klik om meer experimentele gegevens over cellijnen te bekijken

Chemische informatie, opslag en stabiliteit (Chemical Information, Storage & Stability)

Molecuulgewicht	539.58	Formule	C₁₉H₁₇N₅O₂.2CH₄O₃S	Opslag (vanaf de datum van ontvangst)	3 jaar-20°Cpoeder
CAS-nr.	82956-11-4	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 100 mg/mL (185.32 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : 100 mg/mL

Ethanol : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Molecuulgewicht
=	×	×

Verdunningscalculator Molecuulgewichtcalculator

In vivo Batch:
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.
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.
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.
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.
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.

In vivo formulatiecalculator (heldere oplossing)

Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH₂O, mengen en verhelderen.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme (Mechanism of Action)

Targets/IC₅₀/Ki	serine protease
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.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/8713783/ [2] https://pubmed.ncbi.nlm.nih.gov/8029816/ [3] https://pubmed.ncbi.nlm.nih.gov/17826743/ [4] https://pubmed.ncbi.nlm.nih.gov/16359660/ [5] https://pubmed.ncbi.nlm.nih.gov/19661331/ [6] https://pubmed.ncbi.nlm.nih.gov/32312781/ [7] https://pubmed.ncbi.nlm.nih.gov/35974017/

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