| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
FOY-251 targets TMPRSS2, a host cell protease that cleaves the viral spike protein to facilitate entry. By inhibiting TMPRSS2, FOY-251 prevents viral entry and replication. It also inhibits trypsin-like serine proteases including prostasin. The compound has an IC50 of 33.3 nM for TMPRSS2.
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| ln Vitro |
FOY-251 is a potent TMPRSS2 inhibitor with an IC50 of 33.3 nM. It inhibits trypsin with an IC50 of ~55 nM, plasma kallikrein with an IC50 of 2.32 µM, and plasmin with an IC50 of 12.5 µM. It inhibits SARS-CoV-2 infection in cell assays with EC50 values in the low micromolar range.
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| ln Vivo |
In vitro, FOY-251 inhibits SARS-CoV-2 infection in cell culture. As the active metabolite of camostat mesilate, it contributes to the in vivo efficacy of the parent drug in animal models of viral infection. Its TMPRSS2 inhibition is thought to be the primary mechanism of antiviral action.
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| Enzyme Assay |
The in vitro enzyme assay measures TMPRSS2 activity using a fluorogenic peptide substrate. The compound is incubated with the enzyme and substrate, and the release of fluorophore is measured to determine IC50. Similar assays are used for other serine proteases.
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| Cell Assay |
The in vitro cellular assay involves culturing cells permissive to SARS-CoV-2 infection and treating with compound. Viral replication is measured by plaque assay or qPCR. Cytotoxicity is assessed to determine selectivity. The compound's effect on spike protein cleavage can be evaluated by Western blotting.
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| Animal Protocol |
In vivo studies use animal models of SARS-CoV-2 infection, such as transgenic mice expressing human ACE2. Animals are administered the compound orally or intraperitoneally, and viral load in lungs and other tissues is measured. Efficacy is assessed by reduction in viral titer and improvement in clinical scores.
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| ADME/Pharmacokinetics |
FOY-251 has a molecular weight of 409.41 g/mol and a molecular formula of C17H19N3O7S. It is soluble in water and DMSO. The compound is stable at -20°C. Pharmacokinetic data from camostat studies indicate that FOY-251 reaches micromolar concentrations in plasma after oral dosing.
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| Toxicity/Toxicokinetics |
Specific toxicology data are limited. The compound is for research use only. Camostat has a known safety profile in humans, but FOY-251 itself requires further toxicological evaluation for clinical use.
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| References |
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| Additional Infomation |
FOY-251 is the active metabolite of camostat mesilate and a potent TMPRSS2 inhibitor. It has been studied for COVID-19 therapy and is strictly a research compound, not yet clinically approved.
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| Related CAS # |
71079-09-9 (mesylate);71079-08-8
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| Appearance |
Typically exists as solid at room temperature
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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.
Products are for research use only; We do not sell to patients
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