Nafamostat Mesylate(FUT-175)

A serine protease inhibitor

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10mg

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货号: ajci5468
CAS: 82956-11-4
别名: 甲磺酸萘莫司他; FUT-175
分子式: C19H17N5O2.2CH4O3S
分子量: 539.59
纯度: >98%
溶解度: ≥ 27mg/mL in DMSO, ≥ 54mg/mL in Water
储存: 4°C, protect from light
库存: 现货

Background

Nafamostat mesylate, previously known as FUT-175, is an inhibitor of serine protease that inhibits a variety of serine proteases, including trypsin and several proteases in the coagulation cascade. Although it was originally developed as an inhibitor of complements, Nafamostat mesylate has been widely used for the treatment of inflammation (such as acute pancreatitis) and disseminated intravascular coagulation (DIC). Nafamostat mesylate exhibits extremely potent inhibition against human tryptase as well as tryptase-catalyzed hydrolysis of Boc-Phe-Ser-Arg-MCA with inhibition constant K_ivalue of 95.3 pM. Besides its protease-inhibiting activity, nafamostat mesylate, in a recent study, displayed its antimicrobial activity by dose-dependently inhibiting the proliferation of chlamydial in vitro.

Reference

[1].Robert D Inman and Basil Chiu. Nafamostat mesylate, a serine protease inhibitor, demonstrates novel antimicrobial properties and effectiveness in Chlamydia-induced arthritis. Arthritis Rsearch & Therapy 2012, 13:R150
[2].Shuji Mori, Yoshinori Itoh, Ryoko Shinohata, Toshiaki Sendo, Ryozo Oishi and Masahiro Nishibori. Nafamostat mesilate is an extremely potent inhibitor of human tryptase. J Pharmacol Sci 92, 420-423 (2003)

Protocol

Cell experiment [1]:
Cell lines	The human pancreatic tumor cell lines PANC-1
Preparation method	The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.
Reaction Conditions	3 h; 160 μg/mL
Applications	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.
Animal experiment [1]:
Animal models	Five-week-old male nude mice
Dosage form	30 μg/g; thrice a week for 6 weeks; intraperitoneal injection
Applications	A pancreatic cancer model was established by injection of PANC-1 cells (5×10-6cells) in 200 μM of PBS subcutaneously into the right side of the back of the animals. In vivo, the tumor growth in combination group (oxaliplatin and nafamostat mesilate) was significantly slower than that of oxaliplatin group (p<0.0001). Tumor volume in combination group was significantly smaller than that of oxaliplatin group (p=0.048).
Other notes	Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
参考文献: [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.