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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
GLP-2 receptor (GLP-2R), a G protein-coupled receptor expressed primarily in the gastrointestinal tract. Apraglutide acts as a GLP-2R agonist, promoting intestinal epithelial proliferation, reducing apoptosis, enhancing nutrient absorption, and decreasing gastric emptying.
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| ln Vitro |
Apraglutide binds to and activates the GLP-2 receptor with high potency. In vitro studies using GLP-2R-expressing cells demonstrate increased cAMP production upon treatment. The peptide is resistant to dipeptidyl peptidase-4 (DPP-4) degradation due to amino acid substitutions at positions 2 and 10-11.
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| ln Vivo |
Piglets given aprageluteide (FE 203799; 5 mg/kg/dose, administered subcutaneously twice on days 0 and 4 postsurgery) show signs of improvement by day 7, including intestinal lengthening, increased small-intestinal weight, longer villus height, and greater crypt depth. These piglets are in good health.
In a neonatal piglet model with total ileal resection (mimicking human short bowel syndrome), apraglutide enhances intestinal adaptation and linear intestinal growth. In healthy volunteers, it exhibits dose-dependent increases in plasma citrulline (a marker of enterocyte mass). |
| Enzyme Assay |
GLP-2 receptor binding assays: Membranes from GLP-2R-transfected cells are incubated with radiolabeled GLP-2 and varying concentrations of apraglutide. Bound radioactivity is measured by filtration. cAMP accumulation assays in GLP-2R-expressing cells measure receptor activation via competition immunoassay or FRET-based biosensors.
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| Cell Assay |
Caco-2 or other intestinal epithelial cell lines expressing GLP-2R are treated with apraglutide (0.1-100 nM). cAMP levels are measured by ELISA. Cell proliferation is assessed by BrdU incorporation or by counting viable cells. Apoptosis is measured by caspase-3/7 activity or Annexin V staining.
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| Animal Protocol |
Animal/Disease Models: NewbornDuroc piglets, 2-5 days old and weighing between 2-2.6 kg[1].
Doses: 5 mg/kg/dose. Route of Administration: subcutaneously (sc), twice on days 0 and 4 postsurgery. Experimental Results: On day 7, treated piglets were healthy, had significant lower fecal fat and energy losses and demonstrated intestinal lengthening, greater small-intestinal weight, longer villus height, and greater crypt depth. In preclinical models of short bowel syndrome (SBS), apraglutide is administered subcutaneously once weekly due to its extended half-life. Endpoints include intestinal length and weight, villus height, crypt depth, epithelial cell proliferation (Ki67 staining), and nutrient absorption measurements (e.g., plasma citrulline). |
| ADME/Pharmacokinetics |
Apraglutide has an extended plasma half-life (approximately 60-100 hours in humans) due to Ahx (aminocaproic acid) substitution at position 10, which reduces degradation by lysine-targeting proteases. It is administered subcutaneously and exhibits high bioavailability. Steady state is reached after 2-3 weekly doses.
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| Toxicity/Toxicokinetics |
In Phase I clinical trials, apraglutide has shown a favorable safety and tolerability profile with no serious adverse events reported. In preclinical studies, no significant toxicity or off-target effects have been observed. Long-term safety is being evaluated in Phase III extension trials.
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| References | |
| Additional Infomation |
Apraglutide is currently in Phase III clinical development (STARS trial) for short bowel syndrome with intestinal failure (SBS-IF). It has orphan drug designation for graft-versus-host disease (GvHD) and is also being investigated for chemotherapy-induced intestinal dysfunction. Not FDA-approved as of 2026.
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| Molecular Formula |
C172H263N43O52.C2HF3O2
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| Molecular Weight |
3879.27
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| Related CAS # |
Apraglutide;1295353-98-8
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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 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)
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| Solubility (In Vitro) |
H2O :~66.67 mg/mL (~17.19 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 | 0.2578 mL | 1.2889 mL | 2.5778 mL | |
| 5 mM | 0.0516 mL | 0.2578 mL | 0.5156 mL | |
| 10 mM | 0.0258 mL | 0.1289 mL | 0.2578 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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