product name Nafamostat Mesylate
Description: Nafamostat mesylate, also known as FUT-175, is a synthetic serine protease inhibitor, which is used as an anticoagulant during hemodialysis. Nafamostat promotes endothelium-dependent vasorelaxation via the Akt-eNOS dependent pathway. 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.
References: Thromb Haemost. 1996 Jan;75(1):76-82; Eur J Pharmacol. 2006 Jan 13;530(1-2):172-8.
539.58
Formula
C19H17N5O2.2CH4O3S
CAS No.
82956-11-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 20 mg/mL (37.1 mM)
Water: 53 mg/mL (98.2 mM)
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
FUT-175
other peoduct :
| In Vitro |
In vitro activity: 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. 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. 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. Kinase Assay: Cell Assay: 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. |
|---|---|
| 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. 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. |
| Animal model | Five-week-old male nude mice |
| Formulation & Dosage | 30 μg/g; i.p. injection |
| References | Thromb Haemost. 1996 Jan;75(1):76-82; Eur J Pharmacol. 2006 Jan 13;530(1-2):172-8. |
6-Deazaneplanocin A (hydrochloride)
