1. Anti-infection Apoptosis NF-κB Metabolic Enzyme/Protease
  2. Flavivirus TNF Receptor NF-κB Apoptosis Ser/Thr Protease
  3. Nafamostat

Nafamostat  (Synonyms: 萘莫司他)

目录号: HY-B0190
产品使用指南

Nafamostat,一种抗凝剂,是一种人工合成的丝氨酸蛋白酶 (serine protease) 抑制剂。Nafamostat 具有抗癌和抗病毒作用,Nafamostat 通过上调肿瘤坏死因子受体 1 (TNFR1) 的表达诱导凋亡 (apoptosis),可用于动脉壁病理性增厚的发生发展3]

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Nafamostat Chemical Structure

Nafamostat Chemical Structure

CAS No. : 81525-10-2

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生物活性

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

IC50 & Target

I-kappaBalpha

 

体外研究
(In Vitro)

Nafamostat (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 (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 (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.

Cell Viability Assay[1]

Cell Line: MDAPanc-28 cells
Concentration: 80 μg/mL
Incubation Time: 24 h, 48 h
Result: Substantially reduced the cell viability of MDAPanc-28 cells at both 24 hours and 48 hours.

Cell Invasion Assay[2]

Cell Line: Panc-1 cells
Concentration: 0.1 μM, 1 μM, 10 μM
Incubation Time: 24 h
Result: Observed significant inhibition in Panc-1-Try clones at concentrations as low as 0.1 mM.

Western Blot Analysis[1]

Cell Line: MDAPanc-28 cells
Concentration: 10 μg/mL, 20 μg/mL ,40 μg/mL, 80 μg/mL
Incubation Time: 3 h, 8 h, 24 h, 48 h
Result: Inhibited NF-κB DNA-binding activity and the degradation of IκBα in a dose-dependent manner as well as in a time-dependent manner.
Inhibited phosphorylation of IκBα in a time-dependent manner.
体内研究
(In Vivo)

Nafamostat (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 (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
分子量

347.37

Formula

C19H17N5O2

CAS 号
中文名称

萘莫司他

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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