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FOY-251 mesylate

Alias: FOY-251 mesylate; FOY 251; FOY-251; FOY251
Cat No.:V2211 Purity: ≥98%
FOY 251 mesylate is a Camostat metabolite with anti-proteolytic activity, and acts as a proteinase inhibitor.
FOY-251 mesylate
FOY-251 mesylate Chemical Structure CAS No.: 71079-09-9
Product category: Serine Protease
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
250mg
Other Sizes

Other Forms of FOY-251 mesylate:

  • FOY-251 free base
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description

FOY 251 mesylate is a Camostat metabolite with anti-proteolytic activity, and acts as a proteinase inhibitor. It was found to be successful in the cellullar assay in combating SARS-CoV-2 infection. The management and avoidance of allergies are further uses for it.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
FOY-251 inhibits prostasin's protease activity and dose-dependently reduces equivalent current (Ieq) in M-1 cells in vitro.[1]
ln Vivo
FOY-251 increases the plasma and circulating levels of FGF21 of transcription are maintained with the induction of liver integrated stress response (ISR) transcription target genes up to one week of treatment in both ob/ob and lean mice; when administered to DIO mice, the levels of FGF21 in the plasma also increase.[3]
Enzyme Assay
M-1 cells were cultivated on a semi-permeable membrane, subjected to a 24-hour serum deprivation, and treated from the apical side with either 0.01–10 μM FOY-251 or 0.01–1 μM camostat mesilate. Transepithelial voltage (Vte) and resistance (Rte) were measured using a volt-ohm meter following a 24-hour incubation period. Ieq was calculated as the ratio of Vte to Rte and was normalized by dividing it by the active membrane's surface area (113 mm2).
Animal Protocol
Male ob/ob mice, lean and diet-induced obese (DIO) C57BL/6 mice
0.8 mg/g food
p.o.
References

[1]. J Hypertens . 2009 Jan;27(1):181-9.

[2]. bioRxiv . 2020 Aug 5:2020.08.05.237651.

[3]. Published online 2019 Mar 28.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C17H19N3O7S
Molecular Weight
409.41366
Exact Mass
409.094
Elemental Analysis
C, 49.87; H, 4.68; N, 10.26; O, 27.35; S, 7.83
CAS #
71079-09-9
Related CAS #
FOY 251 free base;71079-08-8
PubChem CID
130394
Appearance
Off-white to light yellow solid powder
Density
1.36g/cm3
Boiling Point
592.6ºC at 760 mmHg
Melting Point
194-198ºC
Flash Point
312.2ºC
Index of Refraction
1.632
LogP
3.296
Hydrogen Bond Donor Count
4
Hydrogen Bond Acceptor Count
8
Rotatable Bond Count
6
Heavy Atom Count
28
Complexity
539
Defined Atom Stereocenter Count
0
SMILES
CS(=O)(=O)O.C1=CC(=CC=C1CC(=O)O)OC(=O)C2=CC=C(C=C2)N=C(N)N
InChi Key
JXMOPIDYHUYOED-UHFFFAOYSA-N
InChi Code
InChI=1S/C16H15N3O4.CH4O3S/c17-16(18)19-12-5-3-11(4-6-12)15(22)23-13-7-1-10(2-8-13)9-14(20)21;1-5(2,3)4/h1-8H,9H2,(H,20,21)(H4,17,18,19);1H3,(H,2,3,4)
Chemical Name
2-[4-[4-(diaminomethylideneamino)benzoyl]oxyphenyl]acetic acid;methanesulfonic acid
Synonyms
FOY-251 mesylate; FOY 251; FOY-251; FOY251
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~20 mg/mL (~48.85 mM)
Solubility (In Vivo)
Solubility in Formulation 1: 2 mg/mL (4.89 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: 2 mg/mL (4.89 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2 mg/mL (4.89 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.4425 mL 12.2127 mL 24.4254 mL
5 mM 0.4885 mL 2.4425 mL 4.8851 mL
10 mM 0.2443 mL 1.2213 mL 2.4425 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

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  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • Camostat mesylate and FOY-251 inhibit the activity of recombinant TMPRSS2. bioRxiv . 2020 Aug 5:2020.08.05.237651.
  • Camostat mesylate and FOY-251 inhibit SARS-2-S-driven cell entry with comparable efficiency. bioRxiv . 2020 Aug 5:2020.08.05.237651.
  • Camostat mesylate and FOY-251 inhibit SARS-CoV-2 infection with comparable efficiency. bioRxiv . 2020 Aug 5:2020.08.05.237651.
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