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

Nafamostat mesylate  (Synonyms: FUT-175)

Cat. No.: HY-B0190A Purity: 99.85%
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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].

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Nafamostat mesylate Chemical Structure

Nafamostat mesylate Chemical Structure

CAS No. : 82956-11-4

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10 mM * 1 mL in DMSO
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Based on 10 publication(s) in Google Scholar

Other Forms of Nafamostat mesylate:

Nafamostat mesylate Related Antibodies

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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.

Nafamostat mesylate Related Antibodies

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 year; -20°C, 6 months (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (92.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture and light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.85%

COA (249 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture and light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.8533 mL 9.2665 mL 18.5329 mL 46.3323 mL
5 mM 0.3707 mL 1.8533 mL 3.7066 mL 9.2665 mL
10 mM 0.1853 mL 0.9266 mL 1.8533 mL 4.6332 mL
15 mM 0.1236 mL 0.6178 mL 1.2355 mL 3.0888 mL
20 mM 0.0927 mL 0.4633 mL 0.9266 mL 2.3166 mL
25 mM 0.0741 mL 0.3707 mL 0.7413 mL 1.8533 mL
30 mM 0.0618 mL 0.3089 mL 0.6178 mL 1.5444 mL
40 mM 0.0463 mL 0.2317 mL 0.4633 mL 1.1583 mL
50 mM 0.0371 mL 0.1853 mL 0.3707 mL 0.9266 mL
60 mM 0.0309 mL 0.1544 mL 0.3089 mL 0.7722 mL
DMSO 80 mM 0.0232 mL 0.1158 mL 0.2317 mL 0.5792 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Nafamostat mesylate Related Classifications

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.

Keywords:

Nafamostat82956-11-4FUT-175FUT175FUT 175FlavivirusTNF ReceptorNF-κBApoptosisSer/Thr ProteaseTumor Necrosis Factor ReceptorTNFRNuclear factor-κBNuclear factor-kappaBSerine proteasesSerine endopeptidasesThreonine proteasesMDAPanc-28 cellsPanc-1 cellsA129 miceBalloon injury of the rat carotid wallInhibitorinhibitorinhibit

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