Apraglutide TFA (Synonyms: FE 203799 TFA) |
Catalog No.GC35376
One-Click Copy Product Info
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Apraglutide TFA는 강력하고 고선택적인 GLP-2 작용제로 hGLP-2 수용체와 rGLP-2 수용체에 대한 EC50 값이 각각 0.03 nM과 0.07 nM이다.
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 TFA는 강력하고 고선택적인 GLP-2 작용제로 hGLP-2 수용체와 rGLP-2 수용체에 대한 EC50 값이 각각 0.03 nM과 0.07 nM이다. Apraglutide TFA는 흡수 속도를 감소시키고 청소율을 줄이고 단백질 결합률을 증가시켜 DPP-IV 분해를 감소시킨다[2]. Apraglutide TFA는 동물 모델에서 혈장 시트룰린 수치를 증가시키고 장 기능을 개선하기 위해 일반적으로 사용되고 있다[3].
체내 실험에서 Apraglutide TFA (3.3mg/kg/일)를 피하 주사해서 17일간 처리하면 사이타라빈 유도 쥐의 장 손상을 완화하고 생존율을 개선하였다[4]. 20mg/kg 용량의 Apraglutide TFA를 일주일에 세 번씩 3주간 피하 주사하면 쥐의 장 중량과 길이가 현저하게 증가하였다[5]. 75% 장 절제 및 공장결장 문합술을 받은 듀로크 신생 자돈에서 제0일과 제4일에 각각 5mg/kg 용량의 Apraglutide TFA를 피하 주사하면 장 성장이 증가하고 영양 손실이 감소하였다[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.
| 동물 실험 [1]: | |
동물 모형 | 수컷 BALB/c 쥐 |
제조 방법 | 수컷 BALB/c 쥐(12주령)를 환기가 잘 되는 케이지에 사육하였고 케이지당 4마리 이하, 사료와 물을 자유롭게 섭취할 수 있도록 하였습니다. 사육실 환경 조건은 온도 23.5±2°C, 습도 60±12%, 12시간 광명/암흑 주기로 조절하였습니다. 쥐를 2그룹으로 나누었고 각 그룹당 18마리, 모든 쥐에게 5일 연속으로 하루 두 번 사이타라빈(30mg/kg)을 복강 내 주사하였습니다. Apraglutide TFA를 사이타라빈 투여 4일 전에 투여 당일 및 투여 후 12일 동안 3.3mg/kg/일의 용량으로 피하 투여하였습니다. 쥐의 장 조직을 채취해서 분석하였습니다. |
제형 | 100mg/kg/일, 17 일 동안; s.c. |
응용 분야 | Apraglutide TFA 처리는 쥐에서 사이타라빈 화학요법 후 장 기능을 보호하고 생존율을 개선하였습니다. |
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 | |||
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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)
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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.)