GLPBio

FOY 251

Catalog No.: GC60856Purity:>98.50%
COASDSData Sheet
FOY 251 is an anti-proteolytic active metabolite Camostate, acts as a proteinase inhibitor.

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FOY 251
Cas No.: 71079-09-9
10mM (in 1mL DMSO)In Stock
$93.00
1
1mgIn Stock
$40.00
1
5mgIn Stock
$99.00
1
10mgIn Stock
$159.00
1
25mgIn Stock
$267.00
1
50mgIn Stock
$381.00
1
100mgIn Stock
$520.00
1
200mgIn Stock
$690.00
1
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Description

FOY 251 is an anti-proteolytic active metabolite Camostate, acts as a proteinase inhibitor [1]. FOY 251 can reversibly non-covalently bind to the active site of the TMPRSS2 enzyme, forming a covalent bond with serine proteases to inhibit the enzyme activity and prevent the cellular invasion of SARS-CoV-2[2]. FOY 251 has been widely used to prepare novel types of nanoparticles, which can inhibit trypsin activity both in vitro and on the intestinal mucosal surface [3].

In vitro, FOY 251 treatment (10μM) for 2 hours significantly inhibited the activity of SARS-CoV-2 virus in Calu-3 cells, with an IC50 value of 178nM[4]. FOY 251 treatment (10μM) for 24 hours significantly inhibited the equivalent current and the protease activity of prostasin in mouse cortical collecting duct cells (M-1 cells)[5].

In vivo, FOY 251 treatment via oral administration at a dose of 46mg/kg daily for 7 days reduced the food intake and weight gain in ob/ob mice and increased the plasma FGF21 level[6]. A single oral administration of 100mg/kg dose of FOY 251 significantly delayed gastric emptying in diet-induced obese mice within 60 minutes[7].

References:
[1] Beckh K, Göke B, Müller R, et al. Elimination of the low-molecular weight proteinase inhibitor camostate (FOY 305) and its degradation products by the rat liver[J]. Research in experimental medicine, 1987, 187(6): 401-406.
[2] Kosinsky Y, Peskov K, Stanski D R, et al. Semi-Mechanistic pharmacokinetic-pharmacodynamic model of Camostat mesylate-predicted efficacy against SARS-CoV-2 in COVID-19[J]. Microbiology Spectrum, 2022, 10(2): e02167-21.
[3] Chen J, Liu C, Shan W, et al. Enhanced stability of oral insulin in targeted peptide ligand trimethyl chitosan nanoparticles against trypsin[J]. Journal of microencapsulation, 2015, 32(7): 632-641.
[4] Hoffmann M, Hofmann-Winkler H, Smith J C, et al. Camostat mesylate inhibits SARS-CoV-2 activation by TMPRSS2-related proteases and its metabolite GBPA exerts antiviral activity[J]. EBioMedicine, 2021, 65.
[5] Maekawa A, Kakizoe Y, Miyoshi T, et al. Camostat mesilate inhibits prostasin activity and reduces blood pressure and renal injury in salt-sensitive hypertension[J]. Journal of hypertension, 2009, 27(1): 181-189.
[6] Albarazanji K, Jennis M, Cavanaugh C R, et al. Intestinal serine protease inhibition increases FGF21 and improves metabolism in obese mice[J]. American Journal of Physiology-Gastrointestinal and Liver Physiology, 2019, 316(5): G653-G667.
[7] Albarazanji K, Hinke S A, Cavanaugh C, et al. Role of CCK1 receptor in metabolic benefits of intestinal enteropeptidase inhibition in mice[J]. Plos one, 2025, 20(6): e0312927.

Protocol

Cell experiment [1]:

Cell lines

Calu-3 cells

Preparation Method

Calu-3 cells were cultivated in minimum essential medium (MEM) containing 10% fetal bovine serum (FBS), 100U/mL of penicillin and 0.1mg/mL of streptomycin, non-essential amino acid solution and 1mM sodium pyruvate at 37°C in a humidified atmosphere containing 5% CO2. Calu-3 cells were pre-incubated for 2h with different concentrations of Camostat mesylate or FOY 251 (0, 2, 20, and 200µM), or DMSO (control), before inoculating with SARS-CoV-2 at an MOI of 0.01. Following 1h of incubation at 37°C and 5% CO2, the culture supernatant was removed and cells were washed two times with excess PBS before culture medium containing 1-fold concentrated inhibitor was added. Supernatants were harvested at 24h post inoculation and subjected to plaque titration.

Reaction Conditions

0, 2, 20, and 200µM; 48h

Applications

FOY 251 treatment inhibit SARS-CoV-2 infection in Calu-3 cells in a dose-dependent manner.
Animal experiment [2]:

Animal models

Male ob/ob mice

Preparation Method

Male ob/ob mice (6 weeks old) were single housed in a temperature-controlled room with a 12:12h light-dark cycle and allowed ad libitum access to water and food. Mice (ob/ob) were acclimated to powdered chow [Formula B Diet 5008 (16.5% protein; 17.0% fat; 56.5% carbohydrate)] for 5-7 days. Afterward, mice were fed powdered chow formulated with vehicle alone [20% HP-β-cyclodextran (HP-β-CD)] or Camostat (0.08, 0.25 or 0.8mg/g food) or FOY 251 (46mg/kg) for 7 days. At the end of the experiment, mice were euthanized with CO2. Blood was collected by cardiac puncture and centrifuged at 10,000 rpm for 10 min at 4°C to obtain plasma for analysis. Whole livers were dissected and weighed.

Dosage form

46mg/kg/day for 7 days; p.o.

Applications

FOY 251 treatment significantly decreased liver weight and increased plasma FGF21 levels in ob/ob mice.

References:
[1] Hoffmann M, Hofmann-Winkler H, Smith J C, et al. Camostat mesylate inhibits SARS-CoV-2 activation by TMPRSS2-related proteases and its metabolite GBPA exerts antiviral activity[J]. EBioMedicine, 2021, 65.
[2] Albarazanji K, Jennis M, Cavanaugh C R, et al. Intestinal serine protease inhibition increases FGF21 and improves metabolism in obese mice[J]. American Journal of Physiology-Gastrointestinal and Liver Physiology, 2019, 316(5): G653-G667.

Product Documents

Purity:>98.50%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
71079-09-9
SMILES
O=C(O)CC1=CC=C(OC(C2=CC=C(NC(N)=N)C=C2)=O)C=C1.CS(=O)(O)=O
Molecular Formula
C17H19N3O7S
Molecular Weight
409.41
Solubility
DMSO: 20 mg/mL (48.85 mM; ultrasonic and adjust pH to 5 with HCl); Water: < 0.1 mg/mL (insoluble)
Storage
4°C, away from moisture
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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