Home>>Peptides>>Exendin-4

Exendin-4 Sale

(Synonyms: 艾塞那肽; Exenatide) 目录号 : GC13391

Exendin-4是由39个氨基酸(48-86)组成的多肽,是一种长效的胰高血糖素样肽-1(GLP-1)受体激动剂,IC50为3.22 nM。

Exendin-4 Chemical Structure

Cas No.:141758-74-9

规格 价格 库存 购买数量
5mg
¥550.00
现货
10mg
¥900.00
现货
20mg
¥1,460.00
现货
50mg
¥3,087.00
现货
100mg
¥5,009.00
现货
500mg
¥11,729.00
现货

电话:400-920-5774 Email: sales@glpbio.cn

Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

101

客户使用产品发表文献 1

产品文档

Quality Control & SDS

View current batch:

实验参考方法

Cell experiment [1]:

Cell lines

HUVEC cell lines

Preparation method

HUVECs were seeded at a density of 106/dish and incubated overnight for attachment. The cells were incubated with Exendin-4 at various concentrations (0–50nM) for 15 min.

Reaction Conditions

0-50 nM ; 15 min

Applications

Incubation with exendin-4 (≤20nM) for 15 minutes induced a dose-dependent increase in intracellular cAMP concentration.

Animal experiment [2]:

Animal models

ob/ob mice

Preparation method

The Exendin-4 treated group received 10 μg/kg every 24 hours for the first 14 days. This treatment was the induction phase. After 14 days, the mice treated with Exendin-4 were randomly divided into two groups: one group received a high dose of Exendin-4 (20 μg/kg) every 12 hours; the second group continued to receive a low dose of Exendin-4 (10 μg/kg) every 12 hours. The mice were weighed every day during the 60-day treatment period.

Dosage form

10μg/kg、20μg/kg; s.c.

Applications

Low-dose Exendin-4 treated ob/ob mice sustained a reduction of 7% body weight; high-dose treated animals sustained a net weight reduction of 14%.

References:

[1]Wei R, Ma S, Wang C, et al. Exenatide exerts direct protective effects on endothelial cells through the AMPK/Akt/eNOS pathway in a GLP-1 receptor-dependent manner[J]. American Journal of Physiology-Endocrinology and Metabolism, 2016, 310(11): E947-E957.

[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.

产品描述

Exendin-4 is a 39-amino-acid polypeptide (48-86) and a long-acting glucagon-like peptide-1 (GLP-1) receptor agonist with an IC50 of 3.22 nM[1]. The mechanism of action of Exendin-4 is by binding to the GLP-1 receptor, activating adenylyl cyclase, increasing intracellular cAMP levels, and ultimately promoting insulin secretion while inhibiting glucagon secretion [2]. Exendin-4 has the effect of lowering blood pressure and inducing aortic vasodilation [3].

In vitro, Exendin-4 (0-20nM) incubated HUVEC cells for 15 minutes, which induced a dose-dependent increase in intracellular cAMP concentration, and Exendin-4 (20nM) increased the production of NO in HUVEC cells and increased p-eNOS and GTPCH1 levels [4]. Exendin-4 (0-10μM) treated MCF-7 cells for 48 hours, which had a significant cytotoxic effect with an IC50 of 5μM and reduced the expression of caspase-9, Akt and MMP2 in the cells [5].

In vivo, exendin-4 (10μg/kg or 20μg/kg) was used to treat obese mice via subcutaneous injection for 60 days, which improved serum ALT, reduced serum glucose and insulin levels, and mice in the low-dose group lost weight. 7%, and the body weight of mice in the high-dose group decreased by 14%[6]. Exendin-4 (10 μg/kg) treated SD rats by subcutaneous injection for 75 days, reduced body weight by approximately 30%, significantly reduced insulin, adiponectin, and leptin levels, but caused pancreatic acinar inflammation and pus toxicosis[7].

References:
[1] Doyle M E, Theodorakis M J, Holloway H W, et al. The importance of the nine-amino acid C-terminal sequence of exendin-4 for binding to the GLP-1 receptor and for biological activity[J]. Regulatory peptides, 2003, 114(2-3): 153-158.
[2] Doyle M E, Egan J M. Mechanisms of action of glucagon-like peptide 1 in the pancreas[J]. Pharmacology & therapeutics, 2007, 113(3): 546-593.
[3] Sélley E, Kun S, Szijártó I A, et al. Exenatide induces aortic vasodilation increasing hydrogen sulphide, carbon monoxide and nitric oxide production[J]. Cardiovascular Diabetology, 2014, 13: 1-9.
[4]Wei R, Ma S, Wang C, et al. Exenatide exerts direct protective effects on endothelial cells through the AMPK/Akt/eNOS pathway in a GLP-1 receptor-dependent manner[J]. American Journal of Physiology-Endocrinology and Metabolism, 2016, 310(11): E947-E957.
[5]Fidan-Yaylalı G, Dodurga Y, Seçme M, et al. Antidiabetic exendin-4 activates apoptotic pathway and inhibits growth of breast cancer cells[J]. Tumor Biology, 2016, 37: 2647-2653.
[6]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.
[7]Nachnani J S, Bulchandani D G, Nookala A, et al. Biochemical and histological effects of exendin-4 (exenatide) on the rat pancreas[J]. Diabetologia, 2010, 53: 153-159.

Exendin-4是由39个氨基酸(48-86)组成的多肽,是一种长效的胰高血糖素样肽-1(GLP-1)受体激动剂,IC50为3.22 nM[1]。Exendin-4的作用机制是通过与GLP-1受体结合,激活腺苷酸环化酶,增加细胞内cAMP水平,最终促进胰岛素的分泌,同时抑制胰高血糖素的分泌[2]。Exendin-4具有降低血压,诱导主动脉血管舒张的作用[3]

在体外,Exendin-4(0-20nM)孵育HUVEC细胞15分钟,诱导了细胞内cAMP浓度呈剂量依赖性增加,且Exendin-4(20nM)增加了HUVEC细胞内NO的产生,升高了p-eNOS和GTPCH1水平[4]。Exendin-4(0-10μM)处理MCF-7细胞48 h,具有显著的细胞毒性作用,IC50为5μM,且降低了细胞中caspase-9、Akt和MMP2的表达[5]

在体内,Exendin-4(10 μg/kg或20 μg/kg)通过皮下注射治疗肥胖小鼠,持续60天,均改善了血清ALT,降低了血清葡萄糖和胰岛素水平,低剂量组小鼠体重减少7%,高剂量组小鼠体重减少14%[6]。Exendin-4(10μg/kg)通过皮下注射处理SD大鼠,持续75天,体重减轻了约30%,显著降低了胰岛素、脂联素和瘦素水平,但会导致胰腺腺泡炎症和脓毒症[7]

Chemical Properties

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。
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。

溶解性数据

制备储备液
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
  • 摩尔浓度计算器

  • 稀释计算器

  • 分子量计算器

质量
=
浓度
x
体积
x
分子量
 
 
 
*在配置溶液时,请务必参考产品标签上、MSDS / COA(可在Glpbio的产品页面获得)批次特异的分子量使用本工具。

计算

动物体内配方计算器 (澄清溶液)

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
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