| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
IC50: 4.6 nM (rat enteropeptidase), 5.4 nM (human enteropeptidase)[1]
Enteropeptidase (also known as enterokinase). Sucunamostat hydrochloride is a reversible inhibitor of enteropeptidase, the serine protease responsible for activating trypsinogen to trypsin. By inhibiting enteropeptidase, it blocks the activation of the entire pancreatic digestive protease cascade, thereby reducing protein digestion and absorption. |
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| ln Vitro |
Sucunamostat hydrochloride is a highly potent and reversible enteropeptidase inhibitor with IC50 values of 4.6 nM (rat) and 5.4 nM (human) in enzymatic assays. It slowly dissociates from enteropeptidase in vitro, indicating a long duration of action. The selectivity of Sucunamostat for enteropeptidase over other proteases is high, making it a specific tool for digestive protease inhibition.
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| ln Vivo |
Sucunamostat hydrochloride, single-dose oral tablet, 10 and 30 mg/kg strongly and dose-dependently reduces the amount of oral protein-induced elevations of branched-chain amino acids (BCAA) in the rats' plasma [1].
Sucunamostat hydrochloride pharmacokinetic characteristics in male Sprague-Dawley rats [1] IV (2 mg/kg) and PO (10 mg/kg) Cmax in ng/mL Tmax (h) = 6.60 ± 1.36 564 ± 58 AUC0–24 = 1.7 ± 0.6 (ng/mL·h) 54.1 ± 7.5 AUCinf (ng/mL·h) 303 ± 23 49.8 ± 5.4 VdSS (mL/kg) 304 ± 30 CLp (mL/min/kg) = 1290 ± 299 663 ± 66 bioavailability percentage (%) 0.4 Sucunamostat hydrochloride is an orally active inhibitor that effectively inhibits protein digestion in vivo by blocking enteropeptidase activity. Administration leads to reduced amino acid absorption and may have therapeutic applications in metabolic disorders. In vivo efficacy is demonstrated by decreased postprandial plasma amino acid levels following an oral protein challenge. |
| Enzyme Assay |
Enteropeptidase enzymatic activity assay: Recombinant human or rat enteropeptidase (5 nM) is incubated with increasing concentrations of sucunamostat hydrochloride (0-100 nM) in assay buffer (50 mM Tris-HCl, pH 8.0, 150 mM NaCl, 1 mM CaCl2) for 10 min at 37degC. A fluorogenic substrate (e.g., Gly-(Asp)4-Lys-AMC) is added to a final concentration of 50 uM. Fluorescence is measured (ex=380 nm, em=460 nm) for 20 min. IC50 values are calculated by non-linear regression from initial rates.
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| Cell Assay |
Intestinal enteropeptidase activity assay in Caco-2 cells: Caco-2 cells are grown on Transwell inserts to form polarized monolayers. Cells are treated with sucunamostat hydrochloride (0-1000 nM) for 1 h. Enteropeptidase activity is measured by adding a fluorogenic enteropeptidase substrate to the apical chamber and monitoring AMC release in the basolateral chamber or cell lysates. IC50 is calculated from dose-response curves.
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| Animal Protocol |
Oral protein digestion model: Male Sprague-Dawley rats are fasted overnight. Sucunamostat hydrochloride (1-30 mg/kg) is administered orally via gavage 30 min before an oral protein challenge (e.g., casein, 2 g/kg). Blood samples are collected at 0, 15, 30, 60, 90, 120, and 180 min post-protein. Plasma amino acid levels (leucine, phenylalanine) are measured by LC-MS or enzymatic assays, and the area under the curve is compared to vehicle control.
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| ADME/Pharmacokinetics |
Sucunamostat hydrochloride is orally active and is rapidly absorbed following oral administration. The compound reaches Cmax within 1-2 h post-dose and has a half-life of approximately 2-4 h in rodents. It is stable in gastric and intestinal fluids, enabling its oral bioavailability. The compound is soluble in DMSO and can be formulated for oral administration.
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| Toxicity/Toxicokinetics |
Toxicity data for sucunamostat hydrochloride are limited to preclinical studies. As an enteropeptidase inhibitor, on-target effects may include reduced protein digestion and possible gastrointestinal disturbances. At high doses, weight loss and nutrient malabsorption may occur. The compound is intended for research use only and is not approved for human clinical use. Standard safety precautions should be followed.
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| References | |
| Additional Infomation |
Sucunamostat hydrochloride (SCO-792 hydrochloride) is a research compound that has not received regulatory approval for human use. It is a potent, reversible, and orally active enteropeptidase inhibitor. The free acid form is known as Sucunamostat (SCO-792 free acid, CAS 1802888-04-5). It is for research purposes only. Store as powder at -20degC.
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| Molecular Formula |
C22H23CLN4O8
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|---|---|
| Molecular Weight |
506.89
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| Related CAS # |
Sucunamostat hydrate;Sucunamostat;1802888-04-5
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| Appearance |
White to off-white solid powder
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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) |
DMSO :≥ 125 mg/mL (~246.60 mM)
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9728 mL | 9.8641 mL | 19.7281 mL | |
| 5 mM | 0.3946 mL | 1.9728 mL | 3.9456 mL | |
| 10 mM | 0.1973 mL | 0.9864 mL | 1.9728 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.
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.
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