Nafamostat free base
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MedKoo CAT#: 330245

CAS#: 81525-10-2 (free base)

Description: Nafamostat, also known as FUT-175, is a serine protease inhibitor and an anticoagulant. Nafamostat promotes endothelium-dependent vasorelaxation via the Akt-eNOS dependent pathway. Nafamostat Attenuates Ischemia-Reperfusion-Induced Renal Injury. 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. Researchers have identified the drug as a potential therapy for COVID-19,[ with clinical trials in Japan possibly set to begin in March 2020.

Chemical Structure

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Nafamostat free base
CAS# 81525-10-2 (free base)
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 330245
Name: Nafamostat free base
CAS#: 81525-10-2 (free base)
Chemical Formula: C19H17N5O2
Exact Mass: 347.14
Molecular Weight: 347.378
Elemental Analysis: C, 65.69; H, 4.93; N, 20.16; O, 9.21

Price and Availability

Size Price Availability Quantity
100mg USD 950 2 Weeks
250mg USD 2050 2 Weeks
1g USD 2950 1-2 months
2g USD 5250 1-2 months
5g USD 8950 1-2 months
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Related CAS #: 81525-10-2 (free base)   82956-11-4 (mesylate)   80251-32-7 (HCl)  

Synonym: Nafamostat free base; Nafamostat; FUT-175; FUT 175; FUT175.

IUPAC/Chemical Name: 6-Amidino-2-naphthyl 4-guanidinobenzoate

InChi Key: MQQNFDZXWVTQEH-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H17N5O2/c20-17(21)14-2-1-13-10-16(8-5-12(13)9-14)26-18(25)11-3-6-15(7-4-11)24-19(22)23/h1-10H,(H3,20,21)(H4,22,23,24)

SMILES Code: O=C(OC1=CC=C2C=C(C(N)=N)C=CC2=C1)C3=CC=C(NC(N)=N)C=C3

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Product Data
Instruction:
View handling instruction
Biological target: Nafamostat, a synthetic serine protease inhibitor, is an anticoagulant.
In vitro activity: Nafamostat mesilate (NM), a serine protease inhibitor that is frequently used in the clinic, potently suppressed interferon-gamma (IFN-gamma)-induced up-regulation of PD-L1 in cultured human lung cancer cells (HLC-1) at both the messenger RNA (mRNA) and protein levels. Reference: Int Immunopharmacol. 2018 Jan;54:39-45. https://pubmed.ncbi.nlm.nih.gov/29100036/
In vivo activity: FUT-175 (6-amidino-2-naphthyl p-guanidinobenzoate dimethanesulphonate), a new synthetic protease inhibitor, was administrated to (NZB x NZB) F1 mice in order to examine its influence on the development of autoimmune diseases. A dose (400 mg/kg of body weight) of FUT-175 has both prophylactic and curative effects on the development of lupus nephritis: mice showed a significantly low percentage of proteinuria, a marked decrease in BUN levels, and the lowest degree of glomerular damages. Reference: Immunology. 1985 Aug;55(4):595-600. https://pubmed.ncbi.nlm.nih.gov/4018844/

Preparing Stock Solutions

The following data is based on the product molecular weight 347.38 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Morimoto M, Toyoda H, Niwa K, Hanaki R, Okuda T, Nakato D, Amano K, Iwamoto S, Hirayama M. Nafamostat mesylate prevents metastasis and dissemination of neuroblastoma through vascular endothelial growth factor inhibition. Mol Clin Oncol. 2022 Jul 21;17(3):138. doi: 10.3892/mco.2022.2571. PMID: 35949892; PMCID: PMC9353881. 2. Homma S, Hayashi K, Yoshida K, Sagawa Y, Kamata Y, Ito M. Nafamostat mesilate, a serine protease inhibitor, suppresses interferon-gamma-induced up-regulation of programmed cell death ligand 1 in human cancer cells. Int Immunopharmacol. 2018 Jan;54:39-45. doi: 10.1016/j.intimp.2017.10.016. Epub 2017 Oct 28. PMID: 29100036. 3. Matsubara H, Imai T, Tsuji S, Oka N, Egashira Y, Enomoto Y, Nakayama N, Nakamura S, Shimazawa M, Iwama T, Hara H. Nafamostat protects against early brain injury after subarachnoid hemorrhage in mice. J Pharmacol Sci. 2022 Jan;148(1):65-72. doi: 10.1016/j.jphs.2021.10.007. Epub 2021 Oct 23. Erratum in: J Pharmacol Sci. 2022 Feb;148(2):279. PMID: 34924132. 4. Ikehara S, Shimamura K, Aoyama T, Fujii S, Hamashima Y. Effect of FUT-175, a new synthetic protease inhibitor, on the development of lupus nephritis in (NZB x NZW) F1 mice. Immunology. 1985 Aug;55(4):595-600. PMID: 4018844; PMCID: PMC1453784.
In vitro protocol: 1. Morimoto M, Toyoda H, Niwa K, Hanaki R, Okuda T, Nakato D, Amano K, Iwamoto S, Hirayama M. Nafamostat mesylate prevents metastasis and dissemination of neuroblastoma through vascular endothelial growth factor inhibition. Mol Clin Oncol. 2022 Jul 21;17(3):138. doi: 10.3892/mco.2022.2571. PMID: 35949892; PMCID: PMC9353881. 2. Homma S, Hayashi K, Yoshida K, Sagawa Y, Kamata Y, Ito M. Nafamostat mesilate, a serine protease inhibitor, suppresses interferon-gamma-induced up-regulation of programmed cell death ligand 1 in human cancer cells. Int Immunopharmacol. 2018 Jan;54:39-45. doi: 10.1016/j.intimp.2017.10.016. Epub 2017 Oct 28. PMID: 29100036.
In vivo protocol: 1. Matsubara H, Imai T, Tsuji S, Oka N, Egashira Y, Enomoto Y, Nakayama N, Nakamura S, Shimazawa M, Iwama T, Hara H. Nafamostat protects against early brain injury after subarachnoid hemorrhage in mice. J Pharmacol Sci. 2022 Jan;148(1):65-72. doi: 10.1016/j.jphs.2021.10.007. Epub 2021 Oct 23. Erratum in: J Pharmacol Sci. 2022 Feb;148(2):279. PMID: 34924132. 2. Ikehara S, Shimamura K, Aoyama T, Fujii S, Hamashima Y. Effect of FUT-175, a new synthetic protease inhibitor, on the development of lupus nephritis in (NZB x NZW) F1 mice. Immunology. 1985 Aug;55(4):595-600. PMID: 4018844; PMCID: PMC1453784.

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14: Ammendola M, Leporini C, Marech I, Gadaleta CD, Scognamillo G, Sacco R, Sammarco G, De Sarro G, Russo E, Ranieri G. Targeting mast cells tryptase in tumor microenvironment: a potential antiangiogenetic strategy. Biomed Res Int. 2014;2014:154702. doi: 10.1155/2014/154702. Epub 2014 Sep 11. PMID: 25295247; PMCID: PMC4177740.

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16: Tauchi R, Imagama S, Ito Z, Ando K, Hirano K, Ukai J, Kobayashi K, Shinjo R, Muramoto A, Nakashima H, Matsumoto T, Ishiguro N. Acute pancreatitis after spine surgery: a case report and review of literature. Eur J Orthop Surg Traumatol. 2014 Jul;24 Suppl 1:S305-9. doi: 10.1007/s00590-013-1390-z. Epub 2013 Dec 8. PMID: 24318308.

17: Akshintala VS, Hutfless SM, Colantuoni E, Kim KJ, Khashab MA, Li T, Elmunzer BJ, Puhan MA, Sinha A, Kamal A, Lennon AM, Okolo PI, Palakurthy MK, Kalloo AN, Singh VK. Systematic review with network meta-analysis: pharmacological prophylaxis against post-ERCP pancreatitis. Aliment Pharmacol Ther. 2013 Dec;38(11-12):1325-37. doi: 10.1111/apt.12534. Epub 2013 Oct 20. PMID: 24138390.

18: Dhand A, Aminoff MJ. The neurology of itch. Brain. 2014 Feb;137(Pt 2):313-22. doi: 10.1093/brain/awt158. Epub 2013 Jun 22. PMID: 23794605.

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20: Yuhara H, Ogawa M, Kawaguchi Y, Igarashi M, Shimosegawa T, Mine T. Pharmacologic prophylaxis of post-endoscopic retrograde cholangiopancreatography pancreatitis: protease inhibitors and NSAIDs in a meta-analysis. J Gastroenterol. 2014 Mar;49(3):388-99. doi: 10.1007/s00535-013-0834-x. Epub 2013 May 30. PMID: 23720090.