製品番号: HY-B0190A

Nafamostat (mesylate)

(別名: FUT-175; ナファモスタットメシル酸塩)

19 Cited Publications

カスタマーレビュー

Based on 19 publication(s) in Google Scholar

Nafamostat mesylate (FUT-175), an anticoagulant, is a synthetic serine protease inhibitor. Nafamostat mesylate has anticancer and antivirus effect. Nafamostat mesylate induce apoptosis by up-regulating the expression of tumor necrosis factor receptor-1 (TNFR1). Nafamostat mesylate can be used in the development of the pathological thickening of the arterial wall.

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 99.94%
CAS 番号: 82956-11-4
分子式: C₂₁H₂₅N₅O₈S₂
分子量:539.58

保管条件:

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture and light)

Nafamostat mesylate 構造式

CAS 番号: 82956-11-4

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
- 臨床実験
化学情報
Publications (19)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

I-kappaBalpha

TNF Receptor アイソフォーム固有の製品をすべて表示 :

NF-κB アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
Caco-2	CC₅₀	>20 μM Compound: NAFAMOSTAT	Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay	10.21203/rs.3.rs-23951/v1
Caco-2	IC₅₀	0.04 μM Compound: NAFAMOSTAT	Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging	10.21203/rs.3.rs-23951/v1

体外実験

Nafamostat mesylate (10-80 μg/mL, 3-48 h) inhibits NF-κB activity by blocking IκBα phosphorylation in MDAPanc-28 cells^[1].
Nafamostat mesylate (80 μg/mL, 24-48 h) induces apoptosis by up-regulating the expression of tumor necrosis factor receptor-1 (TNFR1) in MDAPanc-28 cells^[1].
Nafamostat mesylate (0.1-10 μM, 24 h) has suppressive effect on invasiveness in Panc-1 cells^[2].

MedChemExpress (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:

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 NF-κB DNA-binding activity and the degradation of IκBα in a dose-dependent manner as well as in a time-dependent manner.
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.

体内実験

Nafamostat mesylate (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 mesylate (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].

MedChemExpress (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.

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 82956-11-4
性状 Solid
分子量 539.58
分子式 C₂₁H₂₅N₅O₈S₂
Color White to light yellow
SMILES

CS(=O)(O)=O.O=C(OC1=CC=C2C=C(C(N)=N)C=CC2=C1)C3=CC=C(NC(N)=N)C=C3.CS(=O)(O)=O
別名

FUT-175; ナファモスタットメシル酸塩
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture and light)

Publications (19)

All Bio/Physico-chemical AssayIF

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Journal Impact Factor

Cell Res

Remdesivir and chloroquine effectively inhibit the recently emerged novel coronavirus (2019-nCoV) in vitro. [Abstract]

2020 Mar;30(3):269-271. PMID: 32020029
Nat Commun

Structural basis for potent neutralization of human respirovirus type 3 by protective single-domain camelid antibodies. [Abstract]

2024 Jun 27;15(1):5458. PMID: 38937429
Exp Mol Med

Distribution and impact of p16INK4A+ senescent cells in elderly tissues: a focus on senescent immune cell and epithelial dysfunction. [Abstract]

2024 Dec;56(12):2631-2641. PMID: 39617789
Nat Chem Biol

Structure and activity of human TMPRSS2 protease implicated in SARS-CoV-2 activation. [Abstract]

2022 Sep;18(9):963-971. PMID: 35676539
Nucleic Acids Res

COVID19 Drug Repository: text-mining the literature in search of putative COVID19 therapeutics. [Abstract]

2021 Jan 8;49(D1):D1113-D1121. PMID: 33166390
Adv Healthc Mater

Self-Assembling Multi-Antigen T Cell Hybridizers for Precision Immunotherapy of Multiple Myeloma. [Abstract]

2025 Aug 1:e02156. PMID: 40747784

Nafamostat mesylate purchased from MedChemExpress. Usage Cited in: Adv Healthc Mater. 2025 Aug 1:e02156. [Abstract]

Targeted inhibition of granzyme B with Z‐AAD‐CMK and granzyme A with Nafamostat mesylate (NFM) attenuates cell death.
Cells

Assessment of FDA-Approved Drugs as a Therapeutic Approach for Niemann-Pick Disease Type C1 Using Patient-Specific iPSC-Based Model Systems. [Abstract]

2022 Jan 18;11(3):319. PMID: 35159129
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
Eur J Pharmacol

Mechanisms of acid-sensing ion channels inhibition by nafamostat, sepimostat and diminazene. [Abstract]

2023 Jan 5:938:175394. PMID: 36403685

Nafamostat mesylate purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2023 Jan 5:938:175394. [Abstract]

Concentration-inhibition curves for Nafamostat mesylate, sepimostat and diminazene aceturate.

Nafamostat mesylate purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2023 Jan 5:938:175394. [Abstract]

Representative examples of current inhibition by 1 μM Nafamostat mesylate.
Eur J Pharmacol

Mechanisms of NMDA receptor inhibition by nafamostat, gabexate and furamidine. [Abstract]

2022 Mar 15:919:174795. PMID: 35122868
Biomolecules

The Rabep1-Mediated Endocytosis and Activation of Trypsinogen to Promote Pancreatic Stellate Cell Activation. [Abstract]

2022 Jul 31;12(8):1063. PMID: 36008957
Sci Rep

Production and characterization of gigastasin, a leech-derived inhibitor of complement and coagulation pathways. [Abstract]

2026 May 16. PMID: 42143157
Antiviral Res

Omicsynin B4 potently blocks coronavirus infection by inhibiting host proteases cathepsin L and TMPRSS2. [Abstract]

2023 Jun:214:105606. PMID: 37076089

Nafamostat mesylate purchased from MedChemExpress. Usage Cited in: Antiviral Res. 2023 Jun:214:105606. [Abstract]

Huh7.5 cells was infected with HCoV-229E (MOI = 3.5) and treated with omicsynin B4 (10 μM), E−64d (1 μM) or nafamostat mesylate (40 μM) at the indicated times. Immunofluorescence staining of the dsRNA (green) were merged with the nuclear Hoechst 33342 dye (blue) using a fluorescence microscopy (200 × ). Mock, the cell control. Veh, the vehicle control. Cpd, compound. NH4Cl, ammonium chloride. B4, omicsynin B4. NM, nafamostat mesylate. hpi, hour post infection.
Viruses

Molecular Analyses of Clinical Isolates and Recombinant SARS-CoV-2 Carrying B.1 and B.1.617.2 Spike Mutations Suggest a Potential Role of Non-Spike Mutations in Infection Kinetics. [Abstract]

2022 Sep 12;14(9):2017. PMID: 36146823

Nafamostat mesylate purchased from MedChemExpress. Usage Cited in: Viruses. 2022 Sep 12;14(9):2017. [Abstract]

Efficacy of small molecule inhibitors Remdesivir, Nafamostat mesylate, Nirmatrelvir, and Molnupiravir against B.1^BAC-V (green), B.1.617.2^BAC-V (orange), and corresponding clinical isolates (CI, grey).
ChemMedChem

2026 Mar 31;21(7):e202501099.
bioRxiv

2026 Jan 24.
Res Sq

2025 Apr 07.
bioRxiv

2024 October 09.
Patent

US20230210807A1.

溶剤 & 溶解度

体外:

DMSO : 50 mg/mL (92.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 33.33 mg/mL (61.77 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8533 mL

9.2665 mL

18.5329 mL

5 mM

0.3707 mL

1.8533 mL

3.7066 mL

10 mM

0.1853 mL

0.9266 mL

1.8533 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture and light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.63 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.63 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.63 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact

MedChemExpress (MCE) .

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
元素分析報告書 (2659 KB)
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取扱説明書 (2659 KB)

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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	1.8533 mL	9.2665 mL	18.5329 mL	46.3323 mL
	5 mM	0.3707 mL	1.8533 mL	3.7066 mL	9.2665 mL
	10 mM	0.1853 mL	0.9266 mL	1.8533 mL	4.6332 mL
	15 mM	0.1236 mL	0.6178 mL	1.2355 mL	3.0888 mL
	20 mM	0.0927 mL	0.4633 mL	0.9266 mL	2.3166 mL
	25 mM	0.0741 mL	0.3707 mL	0.7413 mL	1.8533 mL
	30 mM	0.0618 mL	0.3089 mL	0.6178 mL	1.5444 mL
	40 mM	0.0463 mL	0.2317 mL	0.4633 mL	1.1583 mL
	50 mM	0.0371 mL	0.1853 mL	0.3707 mL	0.9266 mL
	60 mM	0.0309 mL	0.1544 mL	0.3089 mL	0.7722 mL
DMSO	80 mM	0.0232 mL	0.1158 mL	0.2317 mL	0.5792 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

Nafamostat mesylate

19 Cited Publications

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Nafamostat (mesylate)

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MedChemExpress（MCE）の使用を引用している文献 Nafamostat mesylate

TNF Receptor アイソフォーム固有の製品をすべて表示

NF-κB アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (19)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Nafamostat mesylate 関連分類

HY-B0190A 関連分類