Nafamostat mesylate
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Category：Active Pharmaceutical Ingredients Own Brand：MT /MOQ:100KG /From China/ B2B only.
Introduction
Catalog ID80021057
CAS NO.82956-11-4
Purity 96%
MDL NumberMFCD00941430
Colecular formula C19H17N5O2.2CH3SO3H
Molecular weight 539.5819
Melting point: 259~263°C
| Category | Information |
|---|---|
| Chemical Properties | Nafamostat mesylate (FUT-175) is a synthetic serine protease inhibitor with the molecular formula C₂₁H₂₅N₅O₈S₂ and a molecular weight of 539.58. It is a tan to pale orange solid. |
| Physical Properties | It appears as an off-white to light yellow solid. The melting point is not explicitly mentioned, but it is a crystalline substance. |
| Mechanism of Action | Nafamostat mesylate inhibits serine proteases, including trypsin (Ki = 15 nM) and tryptase (Ki = 95.3 pM). It also inhibits the coagulation cascade, kallikrein, and has anticomplement activity. |
| Biological Activity | – Anticoagulant: Used in hemodialysis.<br>- Antiviral: Demonstrated activity against SARS-CoV-2.<br>- Anticancer: Induces apoptosis by up-regulating TNFR1 and inhibits NF-κB activity.<br>- Anti-inflammatory: Reduces eosinophil infiltration and mast cell activation in asthma models. |
| Clinical Uses | – Acute Pancreatitis: Used as a protease inhibitor to manage acute pancreatitis.<br>- COVID-19: Investigated as a potential treatment for COVID-19 due to its antiviral properties.<br>- Autoimmune Diseases: Studied for its potential use in autoimmune conditions due to its broad inhibitory effects. |
| Storage Conditions | Store at 4°C, sealed, away from moisture and light. |
| Solubility | – DMSO: Soluble up to 50 mg/mL.<br>- Water: Soluble up to 33.33 mg/mL. |
| Additional Information | – IC50 Values: Inhibits SARS-CoV-2 induced cytotoxicity in Caco-2 cells with an IC50 of 0.04 μM.<br>- Clinical Trials: Ongoing studies include trials for COVID-19 treatment (e.g., NCT04623021, NCT04390594). |
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