NafaMostat (hydrochloride)

Product NameNafaMostat (hydrochloride)
CAS80251-32-7
MFC19H18ClN5O2
MW383.84
EINECS
MOL File80251-32-7.mol

Chemical Properties

Melting point	264-266 °C
storage temp.	Store at -20°C
solubility	Soluble in DMSO
form	Powder

Usage And Synthesis

Uses

Nafamostat hydrochloride, an anticoagulant, is a synthetic serine protease inhibitor. Nafamostat hydrochloride has anticancer and antivirus effect. Nafamostat hydrochloride induces apoptosis by up-regulating the expression of tumor necrosis factor receptor-1 (TNFR1). Nafamostat hydrochloride can be used in the development of the pathological thickening of the arterial wall[1][2][3][4].

in vivo

Nafamostat hydrochloride (10 mg/kg, Intraperitoneal injection, once a day for 18 days) exhibits favourable antiviral effects against Zika virus (ZIKV) infection in A129 mice^[3].
Nafamostat hydrochloride (0.5-2.0 mg/mL (dissolved in saline), Intraperitoneal injection, once a day for 7 consecutive days) has inhibitory effect on neointimal formation after balloon injury of the rat carotid wall^[4].

Animal Model:	A129 mice^[3]
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection (i.p.)
Result:	Exhibit delayed lethality and improved survival (40%).

Animal Model:	Balloon injury of the rat carotid wall ^[4]
Dosage:	0.5 mg/mL, 1 mg/mL, 2 mg/mL (dissolved in saline)
Administration:	Intraperitoneal injection (i.p.)
Result:	Showed smaller ratios of the neointima/medial area. Showed positive but reduced immunoreactivity of the cells in the neointimal.

IC 50

I-kappaBalpha

References

[1] Uwagawa T, et al. Mechanisms of synthetic serine protease inhibitor (FUT‐175)‐mediated cell death [J]. Cancer: Interdisciplinary International Journal of the American Cancer Society, 2007, 109(10): 2142-2153. DOI:10.1016/j.bmc.2023.117467
[2] Tajima H, et al. Enhanced invasiveness of pancreatic adenocarcinoma cells stably transfected with cationic trypsinogen cDNA [J]. International journal of cancer, 2001, 94(5): 699-704. DOI:10.1002/ijc.1531
[3] Yan Y, et al. Nafamostat mesylate as a broad-spectrum candidate for the treatment of flavivirus infections by targeting envelope proteins [J]. Antiviral research, 2022, 202: 105325. DOI:10.1016/j.antiviral.2022.105325
[4] Sawada M, et al. Prevention of neointimal formation by a serine protease inhibitor, FUT-175, after carotid balloon injury in rats [J]. Stroke, 1999, 30(3): 644-650. DOI:10.1161/01.str.30.3.644

NafaMostat (hydrochloride)

Chemical Properties

Usage And Synthesis

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