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Purity: ≥98%
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.
Targets |
Serine Protease; Granzyme
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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.
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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. |
Molecular Formula |
C21H25N5O8S2
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Molecular Weight |
539.58
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Exact Mass |
539.11445512
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Elemental Analysis |
C, 46.75; H, 4.67; N, 12.98; O, 23.72; S, 11.88
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CAS # |
82956-11-4
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Appearance |
Solid powder
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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
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InChi Key |
SRXKIZXIRHMPFW-UHFFFAOYSA-N
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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)
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Chemical Name |
(6-carbamimidoylnaphthalen-2-yl) 4-(diaminomethylideneamino)benzoate;methanesulfonic acid
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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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.
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.
(2) Be sure to add the solvent(s) in order.
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 |