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Exendin-4

Exendin-4

产品编号 T3967   CAS 141758-74-9
别名: 艾塞那肽, Exenatide, Exenatide Acetate

Exendin-4 (Exenatide) 是一种长效的 glucagon-likepeptide-1 受体激动剂(IC50: 3.22 nM),是一种由 39 个氨基酸组成的多肽。

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Exendin-4 Chemical Structure
Exendin-4, CAS 141758-74-9
规格 价格/CNY 货期 数量
1 mg ¥ 747 现货
2 mg ¥ 1,060 现货
5 mg ¥ 1,630 现货
10 mg ¥ 2,420 现货
25 mg ¥ 3,390 现货
50 mg ¥ 4,860 现货
100 mg ¥ 6,750 现货
其他形式的 Exendin-4:
产品目录号及名称: Exendin-4 (T3967)
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纯度: 99.72%
纯度: 97.84%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Exendin-4 (Exenatide) is a glucagon-like peptide-1 receptor (GLP-1) agonist (IC50: 3.22 nM). Exenatide is a 39 amino acid peptide. Compared to GLP-1, exenatide has a longer half-life of 2.4 hours.
靶点活性 GLP-1:3.22 nM
体外活性 In HUVECs, exendin-4 dose-dependently significantly increases NO production, eNOS phosphorylation and GTPCH1 level[2]. Exendin-4 shows cytotoxic effects to MCF-7 breast cancer cells (IC50 5 μM) at 48 hours [3].
体内活性 In ob/ob mice, the treatment of exendin-4 improve serum ALT and reduce serum glucose, insulin levels and calculated HOMA scores compared with control. In the final 4 weeks of the study period, exendin-4-treated ob/ob mice sustain an obvious reduction in the net weight gain[4]. Animals treated with exendin-4 have more pyknotic nuclei, more pancreatic acinar inflammation and weigh significantly less than control rats[5]. Exenatide leads to dose-dependent relaxation of rat thoracic aorta, which is evoked via the GLP-1 receptor and is mediated mainly by H2S but also by CO and NO[6].
别名 艾塞那肽, Exenatide, Exenatide Acetate
分子量 4186.57
分子式 C184H282N50O60S
CAS No. 141758-74-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 10 mM

H2O: 1.23 mg/mL), sonification/heating is recommended.

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.2389 mL 1.1943 mL 2.3886 mL 5.9715 mL
5 mM 0.0478 mL 0.2389 mL 0.4777 mL 1.1943 mL
10 mM 0.0239 mL 0.1194 mL 0.2389 mL 0.5971 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Doyle ME, 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. Regul Pept. 2003 Jul 15;114(2-3):153-8. 2. Wei R, et al. Exenatide exerts direct protective effects on endothelial cells through the AMPK/Akt/eNOS pathway in a GLP-1 receptor-dependent manner. Am J Physiol Endocrinol Metab. 2016 Jun 1; 310(11):E947-57. 3. Ding X, et al. Exendin-4, a glucagon-like protein-1 (GLP-1) receptor agonist, reverses hepatic steatosis in ob/obmice. Hepatology. 2006 Jan;43(1):173-81. 4. Nachnani JS, et al. Biochemical and histological effects of exendin-4 (exenatide) on the rat pancreas. Diabetologia. 2010 Jan;53(1):153-9. 5. Sélley, E., Kun, S., Szijártó, I., Laczy, B., Kovács, T., & Fülöp, F. et al. (2014). Exenatide induces aortic vasodilation increasing hydrogen sulphide, carbon monoxide and nitric oxide production. Cardiovascular Diabetology, 13(1), 69. doi: 10.1186/1475-2840-13-69 6. Fidan-YaylalI G, et al. Antidiabetic exendin-4 activates apoptotic pathway and inhibits growth of breast cancer cells. Tumour Biol. 2016 Feb;37(2):2647-53. 7. Huang L, Ma R, Lin T, et al. Glucagon-like peptide-1 receptor pathway inhibits extracellular matrix production by mesangial cells through store-operated Ca2+ channel[J]. Experimental Biology and Medicine. 2019: 1535370219876531.

文献引用

1. Huang L, Ma R, Lin T, et al. Glucagon-like peptide-1 receptor pathway inhibits extracellular matrix production by mesangial cells through store-operated Ca2+ channel. Experimental Biology and Medicine. 2019: 1535370219876531. 2. Ren W, Chen J, Wang W, et al.Sympathetic nerve-enteroendocrine L cell communication modulates GLP-1 release, brain glucose utilization, and cognitive function.Neuron.2024
V-0219 PF-06291874 Avexitide GLP-1R agonist 3 Shanzhiside methyl ester Lotiglipron Semaglutide Acetate Tirzepatide

相关化合物库

该产品包含在如下化合物库中:
NO PAINS 化合物库 ReFRAME 相关化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Exendin-4 141758-74-9 GPCR/G Protein Glucagon Receptor inhibit GCGR 艾塞那肽 Inhibitor Exenatide Exenatide Acetate Exendin 4 Exendin4 inhibitor

 

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