Nafamostat Mesylate (FUT175)

Alias: FUT175; Nafamostat mesylate; FUT 175; FUT-175; nafamostat mesilate
Cat No.:V0707 Purity: ≥98%
Nafamostat mesylate (formerly also known as FUT-175) is a novel and synthetic serine protease inhibitor, which is used as ashort-acting anticoagulant during hemodialysis.
Nafamostat Mesylate (FUT175) Chemical Structure CAS No.: 82956-11-4
Product category: Serine Protease
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
50mg
100mg
250mg
500mg
1g
2g
5g
Other Sizes

Other Forms of Nafamostat Mesylate (FUT175):

  • Nafamostat (FUT-175)
  • Nafamostat hydrochloride (FUT-175)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Nafamostat mesylate (formerly also known as FUT-175) is a novel and synthetic serine protease inhibitor, which is used as a short-acting anticoagulant during hemodialysis. is a novel and synthetic serine protease inhibitor, which is used as a short-acting anticoagulant during hemodialysis. By means of the Akt-eNOS dependent pathway, napamostat facilitates endothelium-dependent vasorelaxation. Nafamostat mesylate possesses antiviral and anti-cancer properties and is also utilized in the treatment of pancreatitis.

Biological Activity I Assay Protocols (From Reference)
Targets
Serine Protease; Granzyme
ln Vitro
Nafamostat mesilate significantly prevents platelet beta-thromboglobulin (beta TG) from being released after 60 and 120 minutes. Neutrophil elastase is not significantly released when using napamostat mesilate (NM); at 120 minutes, the plasma elastase-alpha 1-antitrypsin complex is 0.16 mg/mL in the NM group and 1.24 mg/mL in the control group. The formation of complexes between C1 inhibitor and FXIIa and kallikrein is entirely inhibited by napamostat mesilate.[1]
Nafamostat mesilate inhibits a number of proteases that could play a significant role in the pathogenesis of disseminated intravascular coagulation (DIC).At an IC50 of 0.1 μM, napamostat mesilate inhibits the activity of the TF-F.VIIa mediated-F.Xa extrinsic pathway in a concentration-dependent manner.[2]
Nafamostat mesilate inhibits the initial-phase transient component of biphasic ASIC3 currents in a concentration-dependent manner with an IC50 value of approximately 2.5 mM.[3]
ln Vivo
Nafamostat mesilate (10 mg/kg) prevents scratching brought on by tryptase, but not by serotonin or histamine. The dose-dependent inhibition of scratching induced by intradermal compound 48/80 (10 mg/site) is produced by napamostat mesilate (1–10 mg/kg). Tryptase activity is inhibited in the mouse skin by nafamostat mesilate (10 mg/kg).[4]
Nafamostat mesilate increases gemcitabine-induced apoptosis, inhibits gemcitabine-induced NF-kappaB activation, and inhibits the growth of pancreatic tumors. When paired with gemcitabine, napamostat mesilate enhances the weight loss that gemcitabine causes in mice. [5]
Cell Assay
The drug was applied to the cells at the specified concentration for a full day.
Animal Protocol
Male ICR-SCID nude mice
30 mg/kg
i.p.
References

[1]. Thromb Haemost . 1996 Jan;75(1):76-82.

[2]. Thromb Res . 1994 Apr 15;74(2):155-61.

[3]. Biochem Biophys Res Commun . 2007 Nov 9;363(1):203-8.

[4]. Eur J Pharmacol . 2006 Jan 13;530(1-2):172-8.

[5]. Anticancer Res . 2009 Aug;29(8):3173-8.

[6]. Antimicrob Agents Chemother . 2020 May 21;64(6):e00754-20.

[7]. Nat Commun . 2022 Aug 16;13(1):4804.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C21H25N5O8S2
Molecular Weight
539.58
Exact Mass
539.11445512
Elemental Analysis
C, 46.75; H, 4.67; N, 12.98; O, 23.72; S, 11.88
CAS #
82956-11-4
Appearance
Solid powder
SMILES
CS(=O)(=O)O.CS(=O)(=O)O.C1=CC(=CC=C1C(=O)OC2=CC3=C(C=C2)C=C(C=C3)C(=N)N)N=C(N)N
InChi Key
SRXKIZXIRHMPFW-UHFFFAOYSA-N
InChi Code
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)
Chemical Name
(6-carbamimidoylnaphthalen-2-yl) 4-(diaminomethylideneamino)benzoate;methanesulfonic acid
Synonyms
FUT175; Nafamostat mesylate; FUT 175; FUT-175; nafamostat mesilate
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~20 mg/mL (~37.1 mM)
Water: ~53 mg/mL (~98.2 mM)
Ethanol: <1 mg/mL
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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In vivo Formulation Calculator (Clear solution)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT06078839 Not yet recruiting Drug: Nafamostat mesilate
Drug: 5% glucose
Sepsis
Nafamostat Mesilate
Xu Li October 1, 2023 Phase 4
NCT05555641 Recruiting Drug: Nafamostat Mesylate
Drug: Unfractionated Heparin
Critical Illness
Anticoagulation
Xiaobo Yang, MD December 20, 2022 Phase 2
NCT05090280 Active
Recruiting
Drug: Nafamostat Mesylate
Drug: PF614 solution
Pharmacokinetics Ensysce Biosciences December 1, 2021 Phase 1
NCT04483960 Recruiting Drug: Nafamostat Mesilate
Drug: Enoxaparin
SARS-CoV-2 Infection
(COVID-19)
University of Melbourne July 28, 2020 Phase 3
NCT04473053 Recruiting Drug: Nafamostat Mesylate
Drug: TD139
COVID-19 University of Edinburgh July 3, 2020 Phase 1
Phase 2
Biological Data
  • Nafamostat Mesylate
  • Nafamostat Mesylate
  • Effect of mast cell deficiency on the inhibitory action of nafamostat mesilate ...
    Eur J Pharmacol.2006 Jan 13;530(1-2):172-8.
  • Effects of nafamostat mesilate (NFM) and terfenadine (TRF) on plasma ...
    Eur J Pharmacol.2006 Jan 13;530(1-2):172-8.
  • Effect of nafamostat mesilate (NFM) on the activity of tryptase in the skin. The ...
    Eur J Pharmacol. 2006 Jan 13;530(1-2):172-8.
  • PAR-2 involvement in tryptase- and compound 48/80-induced scratching. (A) ...
    Eur J Pharmacol. 2006 Jan 13;530(1-2):172-8.
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