info

product name:

Nafamostat mesilate

cas No. :

82956-11-4

MF :

C21H25N5O8S2

MW :

539.58

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Detail

Quick Details

Synonyms:

Futhan;

Ronastat;

FUT 175;

Coahibitor;

Nafamastat;

Nafamostatum;

Nafamostat mesylate;

p-Guanidinobenzoic acid ester with 6-hydroxy-2-naphthamidine;

6-Amidino-2-naphthyl 4-guanidino-benzoate dimethanesulphonate;

6-Carbamimidoyl-2-naphthyl 4-carbamimidamidobenzoate methanesulfonate (1:2)

Molecular structure:

Properties

Item

Specifications

Results

Appearance

White crystalline powder

Conforms

Identification

IR corresponds to that of reference standard

Conforms

Rt corresponds to that of reference standard

Conforms

pH

4.7~5.7

5.3

Clarity and color of solution

Colorless and clear

Conforms

Loss on drying

≤0.5%

0.12%

Heavy metals

≤10ppm

5ppm

Residue on ignition

≤0.1%

0.05%

Chloride

≤0.02%

0.007%

Sulfate

≤0.008%

0.004%

Related substance

Individual impurity

<0.1%

0.05%

Total impurities

<0.5%

0.2%

Assay

98.5~101.5%

99.63%

Residual solvents

Methanol

≤3000ppm

<3000ppm

Ethanol

≤5000ppm

<5000ppm

Conclusion

The results conforms with enterprise standards

 

Description

Nafamostat mesilate, also known as nafamostat mesylate, is a potent, synthetic, broad-spectrum, serine protease inhibitor. It aids in proteomic preservation & stabilization. Although it was originally developed as an inhibitor of complements, Nafamostat mesilate has been widely used for the treatment of inflammation (such as acute pancreatitis) and disseminated intravascular coagulation (DIC). Nafamostat mesilate exhibits extremely potent inhibition against human tryptase as well as tryptase-catalyzed hydrolysis of Boc-Phe-Ser-Arg-MCA with inhibition constant Kivalue of 95.3 pM. Besides its protease-inhibiting activity, Nafamostat mesilate, in a recent study, displayed its antimicrobial activity by dose-dependently inhibiting the proliferation of chlamydial in vitro. Nafamostat mesilate has the ability to promote synthesis of tumor necrosis factor-α, IL-12, and IL-18. Additionally, Nafamostat mesilate can induce production of intercellular adhesion molecules-1, B7.1, B7.2, CD40 and CD40 ligand in human blood mononuclear cells. Nafamostat mesilate is an anticoagulant and has been shown to decrease levels of plasma myeloperoxidase, and has also been used in ERCP pancreatitis studies. Nafamostat mesilate is an inhibitor of Factor X, Factor XII, granzyme A and KLK.

Usage

Nafamostat mesylate inhibits fibrinolysis.

Nafamostat mesylate inhibits serine proteases such as F.VIIa, F.XIIa, kallikrein, thrombin, components of the complement system and trypsin.

Nafamostat mesylate promotes endothelium-dependent vasorelaxation via the Akt-eNOS dependent pathway.

Nafamostat mesylate attenuates ischemia-reperfusion-induced renal injury.

Nafamostat mesylate protects against acute cerebral ischemia via blood-brain barrier protection.

Nafamostat mesylate inhibits TNF-α-Induced vascular endothelial cell dysfunction by inhibiting reactive oxygen species production.

Nafamostat mesylate prevents not only coagulation abnormalities, but also organ failure induced by complement-activated leukocytes in animal models of disseminated intravascular coagulation.

Nafamostat mesylate has been used in treating acute pancreatitis because of its inhibitory effect on trypsin and other proteases that produce inflammation and alter hemodynamics.

Nafamostat mesylate has been used effectively and safely as an anticoagulant in patients receiving hemodialysis or plasmapheresis and in those subjected to extracorporeal circulation. Its benefits were most apparent in patients at a high risk of bleeding. NM prevents postoperative cerebral vasospasm in patients with subarachnoid hemorrhage, perhaps by inhibiting the inflammatory response in the vessel wall.

The hyperkalemia that is associated with continuous nafamostat mesylate administration, and which is due to the inhibition of K excretion from the renal collecting duct by Nafamostat mesylate and its metabolites, may be prevented by the intermittent administration of nafamostat mesylate.

Market Outlook and Forecast

Acute pancreatitis (AP) is one of the common abdominal conditions, which is more common in young adults, and its mortality is high, accounting for 30-50%. There are many unresolved problems in the etiology, pathogenesis, and clinical prevention and treatment of AP. At present, AP's unlimited activation of trypsin in the lesions locally causes the pancreatic tissue to digest itself and deteriorate the disease. Even a small amount of protease in the patient's pancreatic juice-when activated, becomes the strongest digestive enzyme. At the same time, it plays a role in initiating a variety of enzyme activation cascades, enabling multiple pancreatic digestive enzymes to be activated at the same time to cooperate with each other to strengthen the pancreas Digest itself. Therefore, it is particularly important to develop drugs that inhibit trypsin activity, and this variety must have broad market prospects.

Nafamostat mesilate is a synthetic protease inhibitor. Protease inhibitors are used to treat acute pancreatitis, acute exacerbation of chronic pancreatitis, postoperative pancreatitis, and anticoagulation during open heart surgery and extracorporeal blood circulation, early treatment of DIC, shock, and treatment of autoimmune diseases. .

In the past, the main treatment principles for acute pancreatitis were symptomatic treatment and prevention of complications. Nafamostat mesilate has the following advantages compared with gabexate:

It has a wide spectrum of enzyme inhibition, strong effect, long half-life and good stability.

Is nafamostat mesilate safe?

Long-term clinical application in Japan has shown that nafamostat mesilate is a safe and effective protease inhibitor. nafamostat mesilate is a non-peptide protease inhibitor developed by Japan's Tobacco Company. It was launched in Japan in October 1986. The dosage form is a lyophilized powder injection, the specification is 10mg, and the sales price is 24670 yen per 10 bottles. The first approved indications were acute pancreatitis, acute exacerbation of chronic pancreatitis, acute pancreatitis after pancreatography, traumatic pancreatitis, postoperative acute pancreatitis, and then increased diffuse intravascular coagulation (DIC) and It is used to prevent indications such as blood coagulation during extracorporeal circulation. At present, the domestic drugs for the treatment of acute pancreatitis are mainly ulinastatin, and gabexate mesylate. There has been no report on the development of nafamostat mesilate. Therefore, the nafamlast mesylate API has been developed. And preparations (freeze-dried needles) can provide a new therapeutic drug for patients with acute pancreatitis, DIC and need extracorporeal blood circulation and fill domestic gaps.

Packaging

25kg/drum

Storage

Store in a dry, well-ventilated place away from direct sunlight.

COA,