Apraglutide TFA (Synonyms: FE 203799 TFA) |
カタログ番号GC35376
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Apraglutide TFAは有力で高度に選択的なGLP-2作動剤であり、hGLP-2受容体とrGLP-2受容体に対するEC50値はそれぞれ0.03nMと0.07nMである。
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は有力で高度に選択的なGLP-2作動剤であり、hGLP-2受容体とrGLP-2受容体に対するEC50値はそれぞれ0.03nMと0.07nMである[1]。Apraglutide TFAは、吸収速度を低下させ、クリアランス速度を減らし、タンパク質の結合速度を増やし、よってDPP-IVの分解を減らす[2]。Apraglutide TFAは動物モデルで、血漿シトルリンのレベルの上昇、腸機能の改善に広く使われている[3]。
In vivo（体内）実験で、Apraglutide TFA（3.3mg/kg/日）を17日間皮下注射したところ、マウスで、シタラビン誘発性腸損傷を軽減し、生存率を改善した[4]。20mg/kgのApraglutide TFAを三週間、週に三回皮下注射したところ、マウスで腸の重量と長さを著しく増やした[5]。Duroc新生子豚に、75%の腸切除と空腸結腸吻合後の0日目と4日目に、それぞれ5mg/kgのApraglutide TFAを皮下注射したところ、腸の成長が促進され、その結果、栄養の損失が減少した[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.
| 動物実験 [1]: | |
動物モデル | 雄のBALB/cマウス |
準備方法 | 雄のBALB/cマウス（12週齢）を、最多4匹のマウス/ケージを、換気が良好なケージで飼育し、飼料と水を自由に摂取させた。飼育チャンバーにおける環境条件を、23.5±2°Cの室温、60±12%の湿度、12時間の昼夜循環に管理した。マウスを18匹ごとに2つのグループに分け、全てのマウスに、シタラビン（30mg/kg）を5日間連続で、毎日二回腹腔内注射した。シタラビン投与の4日前、当日、そして12日後に、3.3mg/kg/日のApraglutide TFAを皮下投与した。マウスの腸組織を分析のために採取した。 |
投与形態 | 100mg/kg/日、17日間；皮下投与 |
アプリケーション | マウスで、Apraglutide TFAの処理は、腸機能を保護し、シタラビンの化学療法後の生存率を改善した。 |
References: | |
| Cas No. | SDF | ||
| 同義語 | FE 203799 TFA | ||
| Formula | C172H263N43O52.C2HF3O2 | M.Wt | 3879.27 |
| 溶解度 | 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 |
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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
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- 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.)