Nafamostat Mesylate

Catalog No.S1386

Nafamostat mesilate is a synthetic serine protease inhibitor, used as an anticoagulant during hemodialysis.

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Nafamostat Mesylate Chemical Structure

Nafamostat Mesylate Chemical Structure
Molecular Weight: 539.58

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Nafamostat Mesylate is available in the following compound libraries:

Product Information

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Product Description

Biological Activity

Description Nafamostat mesilate is a synthetic serine protease inhibitor, used as an anticoagulant during hemodialysis.
Targets serine protease [1]
In vitro Nafamostat mesilate significantly inhibits the release of platelet beta-thromboglobulin (beta TG) at 60 and 120 min. Nafamostat mesilate (NM) prevents any significant release of neutrophil elastase; at 120 min, plasma elastase-alpha 1-antitrypsin complex is 0.16 mg/mL in the NM group and 1.24 mg/mL in the control group. Nafamostat mesilate completely inhibits formation of complexes of C1 inhibitor with kallikrein and FXIIa. [1] Nafamostat mesilate inhibits several proteases which may be importantly involved in the pathophysiology of disseminated intravascular coagulation (DIC).Nafamostat mesilate inhibits extrinsic pathway activity (TF-F.VIIa mediated-F.Xa generation) in a concentration dependent manner with IC50 of 0.1 μM. [2] Nafamostat mesilate produces concentration-dependent inhibition of the initial-phase transient component of biphasic ASIC3 currents with an IC50 value of approximately 2.5 mM. [3]
In vivo Nafamostat mesilate (10 mg/kg) inhibits scratching induced by tryptase but not by histamine and serotonin. Nafamostat mesilate (1-10 mg/kg) produces the dose-dependent inhibition of scratching induced by intradermal compound 48/80 (10 mg/site). Nafamostat mesilate (10 mg/kg) suppresses tryptase activity in the mouse skin. [4] Nafamostat mesilate inhibits gemcitabine-induced NF-kappaB activation, enhances apoptosis by gemcitabine and suppresses pancreatic tumor growth. Nafamostat mesilate combined with Gemcitabine improves the body weight loss of mice induced by Gemicitabine. [5]
Features

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Sundaram S, et al. Thromb Haemost, 1996, 75(1), 76-82.

[2] Uchiba M, et al. Thromb Res, 1994, 74(2), 155-161.

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Chemical Information

Download Nafamostat Mesylate SDF
Molecular Weight (MW) 539.58
Formula

C19H17N5O2.2CH4O3S

CAS No. 82956-11-4
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms FUT-175
Solubility (25°C) * In vitro DMSO 20 mg/mL (37.06 mM)
Water 53 mg/mL (98.22 mM)
Ethanol <1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 6-carbamimidoylnaphthalen-2-yl 4-guanidinobenzoate dimethanesulfonate

Tech Support & FAQs

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