1. Anti-infection Apoptosis NF-κB Metabolic Enzyme/Protease
  2. Flavivirus TNF Receptor NF-κB Apoptosis Ser/Thr Protease
  3. Nafamostat mesylate

Nafamostat mesylate  (Synonyms: FUT-175)

Cat. No.: HY-B0190A Purity: 98.00%
COA Handling Instructions

Nafamostat mesylate (FUT-175), an anticoagulant, is a synthetic serine protease inhibitor. Nafamostat mesylate has anticancer and antivirus effect. Nafamostat mesylate induce apoptosis by up-regulating the expression of tumor necrosis factor receptor-1 (TNFR1). Nafamostat mesylate can be used in the development of the pathological thickening of the arterial wall3].

For research use only. We do not sell to patients.

Nafamostat mesylate Chemical Structure

Nafamostat mesylate Chemical Structure

CAS No. : 82956-11-4

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
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Solid
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10 mg USD 50 In-stock
50 mg USD 110 In-stock
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Based on 10 publication(s) in Google Scholar

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Description

Nafamostat mesylate (FUT-175), an anticoagulant, is a synthetic serine protease inhibitor. Nafamostat mesylate has anticancer and antivirus effect. Nafamostat mesylate induce apoptosis by up-regulating the expression of tumor necrosis factor receptor-1 (TNFR1). Nafamostat mesylate can be used in the development of the pathological thickening of the arterial wall[1][2]3][4].

IC50 & Target

I-kappaBalpha

 

In Vitro

Nafamostat mesylate (10-80 μg/mL, 3-48 h) inhibits NF-κB activity by blocking IκBα phosphorylation in MDAPanc-28 cells[1].
Nafamostat mesylate (80 μg/mL, 24-48 h) induces apoptosis by up-regulating the expression of tumor necrosis factor receptor-1 (TNFR1) in MDAPanc-28 cells[1].
Nafamostat mesylate (0.1-10 μM, 24 h) has suppressive effect on invasiveness in Panc-1 cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: MDAPanc-28 cells
Concentration: 80 μg/mL
Incubation Time: 24 h, 48 h
Result: Substantially reduced the cell viability of MDAPanc-28 cells at both 24 hours and 48 hours.

Cell Invasion Assay[2]

Cell Line: Inhibited NF-κB DNA-binding activity and the degradation of IκBα in a dose-dependent manner as well as in a time-dependent manner.
Inhibited NF-κB DNA-binding activity and the degradation of IκBα in a dose-dependent manner as well as in a time-dependent manner.
Panc-1 cells
Concentration: 0.1 μM, 1 μM, 10 μM
Incubation Time: 24 h
Result: Observed significant inhibition in Panc-1-Try clones at concentrations as low as 0.1 mM.

Western Blot Analysis[1]

Cell Line: MDAPanc-28 cells
Concentration: 10 μg/mL, 20 μg/mL ,40 μg/mL, 80 μg/mL
Incubation Time: 3 h, 8 h, 24 h, 48 h
Result: Inhibited NF-κB DNA-binding activity and the degradation of IκBα in a dose-dependent manner as well as in a time-dependent manner.
Inhibited phosphorylation of IκBα in a time-dependent manner.
In Vivo

Nafamostat mesylate (10 mg/kg, Intraperitoneal injection, once a day for 18 days) exhibits favourable antiviral effects against Zika virus (ZIKV) infection in A129 mice[3].
Nafamostat mesylate (0.5-2.0 mg/mL (dissolved in saline), Intraperitoneal injection, once a day for 7 consecutive days) has inhibitory effect on neointimal formation after balloon injury of the rat carotid wall[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: A129 mice[3]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Exhibit delayed lethality and improved survival (40%).
Animal Model: Balloon injury of the rat carotid wall [4]
Dosage: 0.5 mg/mL, 1 mg/mL, 2 mg/mL (dissolved in saline)
Administration: Intraperitoneal injection (i.p.)
Result: Showed smaller ratios of the neointima/medial area.
Showed positive but reduced immunoreactivity of the cells in the neointimal.
Clinical Trial
Molecular Weight

539.58

Formula

C21H25N5O8S2

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CS(=O)(O)=O.O=C(OC1=CC=C2C=C(C(N)=N)C=CC2=C1)C3=CC=C(NC(N)=N)C=C3.CS(=O)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 1 years; -20°C, 6 months (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (92.66 mM; Need ultrasonic)

H2O : 33.33 mg/mL (61.77 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8533 mL 9.2665 mL 18.5329 mL
5 mM 0.3707 mL 1.8533 mL 3.7066 mL
10 mM 0.1853 mL 0.9266 mL 1.8533 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.63 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.63 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.63 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 98.06%

References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Nafamostat mesylate
Cat. No.:
HY-B0190A
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