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N0289

Sigma-Aldrich

Nafamostat mesylate

≥98% (HPLC), powder, serine protease inhibitor

Synonyme(s) :

4-[(Aminoiminomethyl)amino]benzoic acid 6-(aminoiminomethyl)-2-naphthalenyl ester dimethanesulfonate, FUT-175

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About This Item

Formule empirique (notation de Hill):
C19H17N5O2 · 2CH4O3S
Numéro CAS:
82956-11-4
Poids moléculaire :
539.58
Numéro MDL:
MFCD00941430
Code UNSPSC :
51111800
ID de substance PubChem :
329818423
Nomenclature NACRES :
NA.77

product name

Nafamostat mesylate, ≥98% (HPLC)

Niveau de qualité

100

Pureté

≥98% (HPLC)

Forme

powder

Couleur

white to beige

Solubilité

DMSO: 10 mg/mL, clear
H2O: >10 mg/mL

Température de stockage

room temp

Chaîne SMILES 

CS(O)(=O)=O.CS(O)(=O)=O.NC(=N)Nc1ccc(cc1)C(=O)Oc2ccc3cc(ccc3c2)C(N)=N

InChI

1S/C19H17N5O2.2CH4O3S/c20-17(21)14-2-1-13-10-16(8-5-12(13)9-14)26-18(25)11-3-6-15(7-4-11)24-19(22)23;2*1-5(2,3)4/h1-10H,(H3,20,21)(H4,22,23,24);2*1H3,(H,2,3,4)

Clé InChI

SRXKIZXIRHMPFW-UHFFFAOYSA-N

Application

Nafamostat mesylate has been used:
  • as a serine protease inhibitor to study its effects on proteolytic degradation of therapeutic proteins recombinantly expressed in Chinese hamster ovary (CHO)-K1-derived cells
  • to stop complement activation to validate the assay for murine C3 fragments
  • as a serine protease inhibitor to study its effects on house dust mite extract evoked Ca2+ entry

Actions biochimiques/physiologiques

Nafamostat mesylate is a broad spectrum serine protease inhibitor, kallikrein inhibitor, and inhibits blood coagulation. It is also a possible complement inhibitor.
Nafamostat mesylate is used in the treatment of disseminated intravascular coagulation (DIC), pancreatitis, and systemic inflammatory response syndrome. It can block the proliferation, adhesion, and invasion of cancer cells and repress tumor progression in animal models. Nafamostat mesylate is involved in the development of immune activity. In combination with favipiravir, nafamostat mesylate may block virus entry and replication, and inhibit the pathogenic host response. This combination treatment might be effective for critically ill Covid-19 patients.

Pictogrammes

Health hazard
GHS08

Mention d'avertissement

Warning

Mentions de danger

H361fd

Classification des risques

Repr. 2

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Équipement de protection individuelle

Eyeshields, Gloves, type N95 (US)

Certificats d'analyse (COA)

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Consulter la Bibliothèque de documents

Claire Rolland-Fourcade et al.
Gut, 66(10), 1767-1778 (2017-01-18)
Proteases are key mediators of pain and altered enteric neuronal signalling, although the types and sources of these important intestinal mediators are unknown. We hypothesised that intestinal epithelium is a major source of trypsin-like activity in patients with IBS and
Nafamostat Mesylate Blocks Activation of SARS-CoV-2: New Treatment Option for COVID-19.
Markus Hoffmann et al.
Antimicrobial agents and chemotherapy, 64(6) (2020-04-22)
Complement Components Showed a Time-Dependent Local Expression Pattern in Constant and Acute White Light-Induced Photoreceptor Damage.
Nicole Schäfer et al.
Frontiers in molecular neuroscience, 10, 197-197 (2017-07-06)
Catherine Martel et al.
PloS one, 6(4), e18812-e18812 (2011-04-29)
The activation of complement during platelet activation is incompletely understood. We sought to explore the formation of C5b-9 and anaphylatoxins binding to collagen-activated platelets. C5b-9, anaphylatoxins C3a, C4a and C5a, and anaphylatoxin receptors C3aR1 and C5aR were measured by flow
Yu-Ping Lin et al.
Molecular cell, 70(2), 228-241 (2018-04-21)
The house dust mite is the principal source of perennial aeroallergens in man. How these allergens activate innate and adaptive immunity is unclear, and therefore, there are no therapies targeting mite allergens. Here, we show that house dust mite extract
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