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82956-11-4 (Nafamostat (mesylate))

1

Identification

Nafamostat (mesylate) Nafamostat (mesylate)
Name Nafamostat (mesylate)
Formula C21H25N5O8S2
MW 539.58
CAS No. 82956-11-4
EINECS
Smiles CS(=O)(O)=O.CS(=O)(O)=O.O=C(OC1=CC=C2C=C(C(N)=N)C=CC2=C1)C3=CC=C(NC(N)=N)C=C3
Synonyms 6-Amidino-2-naphthyl 4-guanidino-benzoate dimethanesulphonate; 6-carbamimidoylnaphthalen-2-yl 4-guanidinobenzoate dimethanesulfonate
InChI 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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Introduction

Nafamostat mesylate, a synthetic serine protease inhibitor, is an anticoagulant. Target: Serine Protease Tranilast (FUT-175) is an antiallergic drug for bronchial asthma.

Background Information

Nafamostat is an anticoagulant. Broad spectrum serine protease inhibitor. Reduces eosinophil infiltration, mast cell activation and airway responsiveness in a murine model of asthma. ......by AdooQ BioScience, LLC
Description ......by Apexbio Technology LLC
Nafamostat Mesylate is a synthetic serine protease inhibitor and an anticoagulant. It is a fast-acting proteolytic inhibitor and used during hemodialysis to prevent the proteolysis of fibrinogen into fibrin. ......by BOC Sciences
A broad-spectrum, synthetic serine protease inhibitor and an inhibitor of the classical and alternative ways of complement activation. Displays selectivity for human tryptase when used at relatively low concentrations. Reduces eosinophil infiltration, mast cell activation and airway responsiveness in a murine model of asthma. ......by BioVision, Inc.,
Nafamostat, also known as FUT-175, is a serine protease inhibitor and an anticoagulant. Nafamostat promotes endothelium-dependent vasorelaxation via the Akt-eNOS dependent pathway. Nafamostat Attenuates Ischemia-Reperfusion-Induced Renal Injury. Nafamostat Attenuates Ischemia-Reperfusion-Induced Renal Injury. Nafamostat protects against acute cerebral ischemia via blood-brain barrier protection. Nafamostat Inhibits TNF-α-Induced Vascular Endothelial Cell Dysfunction by Inhibiting Reactive Oxygen Species Production. ......by MedKoo Biosciences, Inc.
Nafamostat mesilate is a synthetic serine protease inhibitor, used as an anticoagulant during hemodialysis. ......by Selleck Chemicals LLC
Nafamostat mesilate is a synthetic serine protease inhibitor, used as an anticoagulant during hemodialysis. ......by Target Molecule Corp.
Broad spectrum serine protease inhibitor. Displays selectivity for human tryptase when used at relatively low concentrations. Reduces eosinophil infiltration, mast cell activation and airway responsiveness in a murine model of asthma. ......by Tocris Bioscience Inc.
3

Protocol(Only for Reference)

Cell Experiment

Cell lines The human pancreatic tumor cell lines PANC-1
Conditions 3 h; 160 μg/mL
Method In assessment of the NF- κB activation by ELISA, concentration of NF- κB p65 in the nuclear extracts of PANC-1 cells in combination group was statistically lower than those in oxaliplatin group (p<0.0001). Like nuclear NF-κB levels, phosphorylated IκBa levels by Western blot analysis in combination group were significantly lower than those in oxaliplatin group (p=0.037). In other words, FUT-175 inhibits oxaliplatin-induced NF- κB activation by suppressing IκBa phosphorylation in vitro.
Source Apexbio Technology LLC

Animal Experiment

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Physical and Chemical Properties

Appearance:Light yellow to yellow Solid EBNumber:EB000012835

Storage condition

Store at -20°C by Apexbio Technology LLC
Desiccate at +4°C by Tocris Bioscience Inc.

Solubility

Soluble in DMSO > 10 mM by Apexbio Technology LLC
DMSO 20 mg/mL (37 mM); Water 53 mg/mL (98 mM) by MedChemexpress Co., Ltd.
(25°C) * In vitro DMSO 20 mg/mL (37.06 mM); Water53 mg/mL (98.22 mM); Ethanol<1 mg/mL (<1 mM) by Selleck Chemicals LLC
Soluble to 100 mM in water and to 100 mM in DMSO by Tocris Bioscience Inc.
5

Mechanism and Indication

Signaling Pathways Metabolic Enzyme/Protease
Target Ser/Thr Protease
Research Area Cardiovascular Disease
Indications
6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Nafamostat (mesylate) - Launched
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Safety Data of Nafamostat (mesylate)

RTECS : DG2736000
8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AdooQ BioScience, LLC USA
Apexbio Technology LLC USA
Ark Pharm, Inc. USA
BOC Sciences
Beijing Mesochem Technology Co., Ltd. China
BioVision, Inc., USA
Biochempartner Co., Ltd China
CHEMSCENE, LLC 10mg/USD60();50mg/USD180() USA
Cayman Chemical Company USA
Changzhou Hangyu Pharmaceutical Technology Co., Ltd. China
MedChemexpress Co., Ltd. 10mg/USD60();50mg/USD180() USA
MedKoo Biosciences, Inc. USA
Selleck Chemicals LLC 10mg/USD97(In stock);10mM/1mLIn DMSO/USD130(In stock);50mg/USD310(In stock) USA
Shaanxi Dasheng Chemical Tech Co., Ltd. China
Shanghai Haoyuan Chemexpress Co., Ltd. 10mg/USD60();50mg/USD180() China
Target Molecule Corp. 10mg/USD38();25mg/USD70();50mg/USD118();100mg/USD218() USA
Tocris Bioscience Inc. USA
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Related Products

Other Forms of 82956-11-4

Name CAS No Formula MW
Nafamostat (hydrochloride) 80251-32-7 C19H19Cl2N5O2 420.29
Nafamostat 81525-10-2 C19H17N5O2 347.37

Recommended Compounds in Ser/Thr Protease

Name CAS No Formula MW
Nafamostat (hydrochloride) 80251-32-7 C19H19Cl2N5O2 420.29
Nafamostat 81525-10-2 C19H17N5O2 347.37
UK-371804 256477-09-5 C14H16ClN5O4S 0.0
Nα-Tosyl-Lphenylalanine chloromethyl ketone 402-71-1 C17H18ClNO3S 351.85
LP-922761 1454556-82-1 C21H26N6O3 410.47
LP-935509 1454555-29-3 C20H24N6O3 396.44
IPR-2260 2097143-82-1 C31H21ClFNO5 541.95
STOCK1S-50699 393540-75-5 C29H31N2S2 471.7
GCN2iB 2183470-12-2 C18H12ClF2N5O3S 451.83

Recommended Compounds in Same Indication

Name CAS No Formula MW
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Route of Synthesis

12

References

[1]. Ikehara S, et al. Effect of FUT-175, a new synthetic protease inhibitor, on the development of lupus nephritis in (NZB x NZW) F1 mice. Immunology. 1985 Aug;55(4):595-600.

[2]. Pak K, et al. Effectiveness of FUT-175, protease inhibitor, as an anticoagulant to hemodialysis. Hinyokika Kiyo. 1988 Jun;34(6):1077-81.

Protocol Reference

[1] Gocho T, Uwagawa T, Furukawa K, et al. Combination chemotherapy of serine protease inhibitor nafamostat mesilate with oxaliplatin targeting NF-κB activation for pancreatic cancer[J]. Cancer letters, 2013, 333(1): 89-95.

......by Apexbio Technology LLC
Mori et al (2003) Nafamostat mesilate is an extremely potent inhibitor of human tryptase. J.Pharmacol.Sci. 92 420. PMID: 12939527.

Sendo et al (2003) A potent tryptase inhibitor nafamostat mesilate dramatically suppressed pulmonary dysfunction induced in rats by a radiographic contrast medium. Br.J.Pharmacol. 138 959. PMID: 12642398.

Chen et al (2006) Serine protease inhibitors nafamostat mesilate and gabexate mesilate attenuate allergen-induced airway inflammation and eosinophilia in a murine model of asthma. J.Allergy Clin.Immunol. 118 105. PMID: