Nafamostat (mesylate) | 甲磺酸萘莫司他

MCE 国际站：Nafamostat (mesylate)

中文名：甲磺酸萘莫司他

CAS：82956-11-4

品牌：MedChemExpress (MCE)

存储条件：4°C, sealed storage, away from moisture and light

生物活性： Nafamostat mesylate 是一种合成的丝氨酸蛋白酶抑制剂，是一种抗凝剂。 Nafamostat mesylate 通过降低颗粒酶活性和 CTL 细胞溶解来抑制 T 细胞自身反应性。萘莫司他甲磺酸盐可阻断 SARS-CoV-2 的激活。^[1][2][3][4]。 IC50 和目标：丝氨酸蛋白酶^[1][2]。颗粒酶^[3]。

体外：Nafamostat mesylate (10-80 μg/mL, 3-48 h) 通过阻断 IκBα 磷酸化抑制 MDAPanc-28 细胞 NF-κB 活性[1]。 Nafamostat mesylate (80 μg/mL, 24-48 h) 通过上调肿瘤坏死因子受体 1 (TNFR1) 的表达诱导 MDAPanc-28 细胞凋亡[1]。 Nafamostat mesylate (0.1-10 μM, 24 h) 对 Panc-1 细胞的侵袭能力有抑制作用[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内：Nafamostat mesylate (10 mg/kg，腹腔注射，一天一次，持续 18 天) 对寨卡病毒 (ZIKV) 感染的 A129 小鼠具有良好的抗病毒作用[3]。 Nafamostat mesylate (0.5-2.0 mg/mL (溶于生理盐水中)，腹腔注射，一天一次，连续 7 天) 对大鼠颈动脉壁球囊损伤后新生内膜形成有抑制作用[4]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. Clinical Trial

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研究领域：Anti-infection  |  Apoptosis  |  NF-κB  |  Metabolic Enzyme/Protease

作用靶点：Flavivirus  |  TNF Receptor  |  NF-κB  |  Apoptosis  |  Ser/Thr Protease

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参考文献：[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.

[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.

[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.

[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.