Apraglutide是一种强效且高度选择性的GLP-2激动剂，对hGLP-2受体和rGLP-2受体的EC50值分别为0.03nM和0.07nM。
Cas No.:1295353-98-8
Sample solution is provided at 25 µL, 10mM.
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Apraglutide 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 decreases the rate of absorption, reduce the clearance rate, and increases the protein binding rate, thereby reducing DPP-IV degradation[2]. Apraglutide has been widely used to increase plasma citrulline levels and improve intestinal function in animal models[3].
In vivo, Apraglutide treatment via subcutaneous injection of Apraglutide (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 three times a week for three weeks significantly increased gut weight and length in mice[5]. Subcutaneous injection of Apraglutide 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, 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 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, 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, 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, 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), 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.
Apraglutide是一种强效且高度选择性的GLP-2激动剂，对hGLP-2受体和rGLP-2受体的EC50值分别为0.03nM和0.07nM[1]。Apraglutide可降低吸收速率、减少清除率，并提高蛋白结合率，从而减少DPP-IV降解[2]。Apraglutide已被广泛用于动物模型中以提高血浆瓜氨酸水平和改善肠道功能[3]。
在体内，每日皮下注射Apraglutide（3.3mg/kg/day）连续17天，减轻了阿糖胞苷诱导的小鼠肠道损伤并提高了小鼠存活率[4]。每周三次皮下注射20mg/kg剂量的Apraglutide，连续三周，显著增加了小鼠的肠道重量和长度[5]。在杜洛克新生仔猪进行75%肠切除加空肠结肠吻合术后的第0天和第4天，分别皮下注射5mg/kg剂量的Apraglutide，促进了肠道生长，并减少了营养损失[6]。
| 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 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 treatment protected intestinal function and improved survival following chemotherapy with cytarabine in mice. |
References: | |
| Cas No. | 1295353-98-8 | SDF | |
| 别名 | FE 203799 | ||
| 分子式 | C172H263N43O52 | 分子量 | 3765.25 |
| 溶解度 | DMSO : 100 mg/mL (26.56 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 265.6 μL | 1.3279 mL | 2.6559 mL |
| 5 mM | 53.1 μL | 265.6 μL | 531.2 μL |
| 10 mM | 26.6 μL | 132.8 μL | 265.6 μL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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