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- Nafamostat Mesylate(FUT-175)
Nafamostat Mesylate(FUT-175)
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 Kivalue 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
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
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)
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 539.59 |
| Cas No. | 82956-11-4 |
| Formula | C19H17N5O2·2CH4O3S |
| Synonyms | Nafamostat Mesylate,FUT-175,Futhan |
| Solubility | ≥27 mg/mL in DMSO; ≥54 mg/mL in H2O; insoluble in EtOH |
| Chemical Name | (6-carbamimidoylnaphthalen-2-yl) 4-(diaminomethylideneamino)benzoate;methanesulfonic acid |
| SDF | Download SDF |
| Canonical 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 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
The human pancreatic tumor cell lines PANC-1 |
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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. |
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Reaction Conditions |
3 h; 160 μg/mL |
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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 |
| Animal experiment [1]: | |
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Animal models |
Five-week-old male nude mice |
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Dosage form |
30 μg/g; thrice a week for 6 weeks; intraperitoneal injection |
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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 |
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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. |
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References: [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. |
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| Description | Nafamostat Mesylate is an anticoagulant. | |||||
| Targets | Serine Protease | |||||
| IC50 | ||||||
Quality Control & MSDS
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Chemical structure
Related Biological Data
Related Biological Data
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