Exendin-4
(Synonyms: 艾塞那肽; Exenatide) 目录号 : GC13391
Exendin-4 (Exenatide) 是一种 39 个氨基酸的肽，是一种长效胰高血糖素样肽-1 受体激动剂，IC50 为 3.22 nM。
Cas No.:141758-74-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
Mouse insulinoma beta TC-1 cell line |
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Preparation method |
Soluble to 1 mg/ml in sterile water. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
0.1 nM to 1 μM for 2 h |
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Applications |
Exendin-4, like GLP-1, could stimulate dose dependently the glucose-induced insulin secretion in isolated rat islets, and, in mouse insulinoma beta TC-1 cells, both peptides were able to stimulate the proinsulin gene expression at the level of transcription. |
| Animal experiment [2]: | |
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Animal models |
Ob/ob mice model |
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Dosage form |
10 μg/kg or 20 μg/kg, qd for 14 days |
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Application |
Ob/ob mice were treated with Exendin-4 [10 μg/kg or 20 μg/kg] for 60 days. It was found that Ob/ob mice sustained a reduction in the net weight gained during Exendin-4 treatment. Serum glucose and hepatic steatosis was significantly reduced in Exendin-4 treated ob/ob mice. Moreover, Exendin-4 improved insulin sensitivity in ob/ob mice, as calculated by the homeostasis model assessment. The measurement of thiobarbituric reactive substances as a marker of oxidative stress was significantly reduced in ob/ob-treated mice with Exendin-4. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Gke R, Fehmann H C, Linn T, et al. Exendin-4 is a high potency agonist and truncated exendin-(9-39)-amide an antagonist at the glucagon-like peptide 1-(7-36)-amide receptor of insulin-secreting beta-cells[J]. Journal of Biological Chemistry, 1993, 268(26): 19650-19655. [2] Ding X, Saxena N K, Lin S, et al. Exendin‐4, a glucagon‐like protein‐1 (GLP‐1) receptor agonist, reverses hepatic steatosis in ob/ob mice[J]. Hepatology, 2006, 43(1): 173-181. |
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Exendin-4, a glucagon-like protein-1 (GLP-1) receptor agonist, mimics the activity of mammalian incretin hormone glucagon-like peptide 1 (GLP-1), and thus, promotes insulin secretion and functions in the control of glucose [1].
In vitro: Exendin-4 showed a pronounced effect on intracellular cAMP generation. Treatment of GLP-1 in combination with exendin-4 showed additive action on the generation of cAMP. In isolated rat islets and in mouse insulinoma beta TC-1 cells, Exendin-4 stimulated the glucose-induced insulin secretion in a dose dependent manner [2]. In basal forebrain cholinergic neurons, exendin-4 greatly reduced ibotenic acid-induced depletion of choline acetyltransferase immunoreactivity [3].
In vivo: In ob/ob mice, administration of Exendin-4 (10 μg/kg or 20 μg/kg) improved insulin sensitivity and significantly reduced serum glucose and hepatic steatosis. Exendin-4 appeared to effectively reverse hepatic steatosis in ob/ob mice by improving insulin sensitivity [1]. In athymic mice, 63% of exendin-4-treated mice achieved graft function compared with 21% of untreated mice (p = 0.033) in the short-term study. 88% of treated mice had functioning grafts compared with 22% of controls (p = 0.015) in the long-term study. Exendin-4-treated mice gained significantly more weight than the untreated counterparts [4].
艾塞格琳-4（Exendin-4）是一种类胰高血糖素样肽1（GLP-1）受体激动剂，可以模拟哺乳动物胰高血糖素样肽1（GLP-1）的活性，从而促进胰岛素分泌和控制葡萄糖水平的功能[1]。
体外：Exendin-4对细胞内环磷酸腺苷（cAMP）生成有显著的影响。GLP-1和Exendin-4联合处理对cAMP的生成具有叠加作用。在离体大鼠胰岛和小鼠胰岛素瘤细胞系β TC-1中，Exendin-4剂量依赖性地刺激葡萄糖诱导的胰岛素分泌[2]。在基底前脑胆碱能神经元中，Exendin-4极大地减少了依博酸引起的胆碱乙酰转移酶免疫反应物的丢失[3]。
体内：在ob/ob小鼠中，给予Exendin-4（10 μg/kg或20 μg/kg）可以改善胰岛素敏感性，显著降低血清葡萄糖和肝脏脂肪变性。Exendin-4似乎通过改善胰岛素敏感性有效地逆转了ob/ob小鼠的肝脏脂肪变性[1]。在无胸腺小鼠中，短期研究中，63％的接受Exendin-4治疗的小鼠达到移植功能，而未接受治疗的小鼠只有21％（p = 0.033）。长期研究中，88％的治疗小鼠具有功能性移植物，而对照组只有22％（p = 0.015）。接受Exendin-4治疗的小鼠体重显著增加[4]。
References:
Ding X, Saxena N K, Lin S, et al. Exendin‐4, a glucagon‐like protein‐1 (GLP‐1) receptor agonist, reverses hepatic steatosis in ob/ob mice[J]. Hepatology, 2006, 43(1): 173-181.
Gke R, Fehmann H C, Linn T, et al. Exendin-4 is a high potency agonist and truncated exendin-(9-39)-amide an antagonist at the glucagon-like peptide 1-(7-36)-amide receptor of insulin-secreting beta-cells[J]. Journal of Biological Chemistry, 1993, 268(26): 19650-19655.
Perry T A, Haughey N J, Mattson M P, et al. Protection and reversal of excitotoxic neuronal damage by glucagon-like peptide-1 and exendin-4[J]. Journal of Pharmacology and Experimental Therapeutics, 2002, 302(3): 881-888.
Sharma A, Srenby A, Wernerson A, et al. Exendin-4 treatment improves metabolic control after rat islet transplantation to athymic mice with streptozotocin-induced diabetes[J]. Diabetologia, 2006, 49(6): 1247-1253.
| Cas No. | 141758-74-9 | SDF | |
| 别名 | 艾塞那肽; Exenatide | ||
| Canonical SMILES | CCC(C)C(C(=O)NC(CCC(=O)O)C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)NC(CC(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NCC(=O)NCC(=O)N3CCCC3C(=O)NC(CO)C(=O)NC(CO)C(=O)NCC(=O)NC(C)C(=O)N4CCCC4C(=O)N5CCCC5C(=O)N6CCCC6C(=O)NC(CO)C(=O)N)NC(=O)C(CC7=CC=CC=C7)NC(=O)C(CC(C)C)NC( | ||
| 分子式 | C184H282N50O60S | 分子量 | 4186.57 |
| 溶解度 | ≥ 145 mg/mL in DMSO, ≥ 52 mg/mL in Water with gentle warming | 储存条件 | Store at -20°C,protect from light |
| 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 | 0.2389 mL | 1.1943 mL | 2.3886 mL |
| 5 mM | 0.0478 mL | 0.2389 mL | 0.4777 mL |
| 10 mM | 0.0239 mL | 0.1194 mL | 0.2389 mL |
| 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。