切换导航

Exendin-4

现货
Catalog No.
A3408
GLP-1激活剂
组合的产品项目
规格价格库存 数量
20mg
¥ 2,000.00
现货
50mg
¥ 4,180.00
现货
100mg
¥ 6,790.00
现货
500mg
¥ 16,720.00
Ship with 10-15 days

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

Background

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].

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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt4186.57
Cas No.141758-74-9
FormulaC184H282N50O60S
SynonymsExenatide
Solubility≥145 mg/mL in DMSO, <2.44 mg/mL in EtOH, ≥52 mg/mL in H2O with gentle warming
SDFDownload SDF
Canonical SMILESCCC(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(
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

小鼠胰岛瘤细胞系(beta TC-1)

溶解方法

在无菌水中的溶解度可达到1 mg/ml。为了获得更高浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

0.1 nM到1 μM孵育2小时

应用

与GLP-1类似,在分离的大鼠胰岛中,Exendin-4可以剂量依赖地刺激葡萄糖诱导的胰岛素分泌,并且在小鼠胰岛瘤βTC-1细胞中,两种肽都能够刺激胰岛素原基因在转录水平的表达。

动物实验 [2]:

动物模型

ob/ob小鼠模型

剂量

10 μg/kg或20 μg/kg,一天一次持续14天

应用

用Exendin-4 [10 μg / kg或20 μg / kg]处理Ob / ob小鼠60天。 结果发现Ob / ob小鼠净重在Exendin-4治疗期间持续减少。 Exendin-4治疗的ob / ob小鼠血清葡萄糖和肝脂肪变性显著降低。 此外,通过体内平衡模型评估计算,Exendin-4可以改善ob / ob小鼠的胰岛素敏感性。 同时还发现在Exendin-4治疗的ob / ob小鼠中,作为氧化应激标志物的硫代巴比妥反应物质水平显著降低。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

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.

质量控制

化学结构

Exendin-4