Apraglutide TFA (Synonyms: FE 203799 TFA) |
Catalog No.GC35376
One-Click Copy Product Info
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Apraglutide TFA is a potent and highly selective GLP-2 agonist with EC50 values of 0.03 nM and 0.07nM for hGLP-2 receptor and rGLP-2 receptor, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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Apraglutide TFA is a potent and highly selective GLP-2 agonist with EC50 values of 0.03 nM and 0.07nM for hGLP-2 receptor and rGLP-2 receptor, respectively[1]. Apraglutide TFA decreases the rate of absorption, reduce the clearance rate, and increases the protein binding rate, thereby reducing DPP-IV degradation[2]. Apraglutide TFA has been widely used to increase plasma citrulline levels and improve intestinal function in animal models[3].
In vivo, Apraglutide TFA treatment via subcutaneous injection of Apraglutide TFA (3.3mg/kg/day) for 17 days alleviated cytarabine-induced intestinal injury and improved survival in mice[4]. Subcutaneous injection of a 20mg/kg dose of Apraglutide TFA three times a week for three weeks significantly increased gut weight and length in mice[5]. Subcutaneous injection of Apraglutide TFA at a dose of 5mg/kg on days 0 and 4 of 75% intestinal resection with jejunocolic anastomosis, respectively, increased intestinal growth and resulted in reduced nutritional losses in Duroc newborn piglets[6].
References:
[1] Hargrove D M, Alagarsamy S, Croston G, et al. Pharmacological characterization of Apraglutide TFA, a novel long-acting peptidic glucagon-like peptide-2 agonist, for the treatment of short bowel syndrome[J]. The Journal of Pharmacology and Experimental Therapeutics, 2020, 373(2): 193-203.
[2] Verbiest A, Hvistendahl M K, Bolognani F, et al. Efficacy and safety of Apraglutide TFA in short bowel syndrome with intestinal failure and colon–in–continuity: A multicenter, open-label, metabolic balance study[J]. Clinical Nutrition, 2024, 43(12): 158-166.
[3] Bolognani F, Kruithof A C, Schulthess P, et al. Characterization of the pharmacokinetic and pharmacodynamic profile of Apraglutide TFA, a glucagon-like peptide-2 analog, in healthy volunteers[J]. The Journal of Pharmacology and Experimental Therapeutics, 2023, 386(2): 129-137.
[4] Eliasson J, Hvistendahl M K, Freund N, et al. Apraglutide TFA, a novel glucagon‐like peptide‐2 analog, improves fluid absorption in patients with short bowel syndrome intestinal failure: findings from a placebo‐controlled, randomized phase 2 trial[J]. Journal of Parenteral and Enteral Nutrition, 2022, 46(4): 896-904.
[5] Martchenko S E, Sweeney M E, Dimitriadou V, et al. Site-specific and temporal effects of Apraglutide TFA, a novel long-acting glucagon-like peptide-2 receptor agonist, on intestinal growth in mice[J]. The Journal of Pharmacology and Experimental Therapeutics, 2020, 373(3): 347-352.
[6] Slim G M, Lansing M, Wizzard P, et al. Novel long‐acting GLP‐2 analogue, FE 203799 (Apraglutide TFA), enhances adaptation and linear intestinal growth in a neonatal piglet model of short bowel syndrome with total resection of the ileum[J]. Journal of Parenteral and Enteral Nutrition, 2019, 43(7): 891-898.
| Animal experiment [1]: | |
Animal models | Male BALB/c mice |
Preparation Method | Male BALB/c mice (12-week-old) were housed in well-ventilated cages with no more than four mice per cage and access to diet and water ad libitum. Environmental conditions in the feeding chamber were controlled with a temperature of 23.5±2°C, humidity of 60±12%, and a 12h light/dark cycle. The mice were divided into 2 groups, 18 mice in each group, and all mice were intraperitoneally injected with cytarabine (30mg/kg) twice daily for 5 consecutive days. Apraglutide TFA was administered subcutaneously at a dose of 3.3mg/kg/day on the 4 days before and on the day of cytarabine application and 12 days after. Mice's intestinal tissues were collected for analysis. |
Dosage form | 100mg/kg/day for 17 days; s.c. |
Applications | Apraglutide TFA treatment protected intestinal function and improved survival following chemotherapy with cytarabine in mice. |
References: | |
| Cas No. | SDF | ||
| Synonyms | FE 203799 TFA | ||
| Formula | C172H263N43O52.C2HF3O2 | M.Wt | 3879.27 |
| Solubility | H2O : 66.67 mg/mL (ultrasonic and adjust pH to 11 with NaOH) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 257.8 μL | 1.2889 mL | 2.5778 mL |
| 5 mM | 51.6 μL | 257.8 μL | 515.6 μL |
| 10 mM | 25.8 μL | 128.9 μL | 257.8 μL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)