Exendin-4 (Exenatide), a 39 amino acid peptide, is a long-acting glucagon-like peptide-1 receptor agonist with an IC50 of 3.22 nM.
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Custom Peptide Synthesis
Exendin-4 Chemical Structure
CAS No. : 141758-74-9
This product is a controlled substance and not for sale in your territory.
Based on 47 publication(s) in Google Scholar
Other Forms of Exendin-4:
Exendin-4 acetate
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Exendin-4 (Standard)
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Exendin-4 purchased from MedChemExpress. Usage Cited in:
Front Pharmacol. 2019 Oct 25;10:1230.
[Abstract]
INS-1 cells are incubated with THAP (0.5 μM), H89, with Exendin-4 or FSK at indicated concentration for 24 h, then the IL-1β level is analyzed by qRT-PCR (n = 3).
Exendin-4 purchased from MedChemExpress. Usage Cited in:
Front Pharmacol. 2019 Oct 25;10:1230.
[Abstract]
Exendin-4 or FSK treatment reduces ER stress-induced β-cell viability. INS-1 cells are incubated with THAP (0.5 μM), with Eexendin-4.
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Description
Exendin-4 (Exenatide), a 39 amino acid peptide, is a long-acting glucagon-like peptide-1 receptor agonist with an IC50 of 3.22 nM.
In human umbilical vein endothelial cells, exendin-4 significantly increases NO production, endothelial NO synthase (eNOS) phosphorylation, and GTP cyclohydrolase 1 (GTPCH1) level in a dose-dependent manner[2]. Exendin-4 shows cytotoxic effects to MCF-7 breast cancer cells with IC50 of 5 μM at 48 hour[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Exendin-4 Related Antibodies
In Vivo
Both low- and high-dose exendin-4 treatment in ob/ob mice improve serum ALT and reduce serum glucose, and calculated HOMA scores compared with control. Exendin-4-treated ob/ob mice sustain a marked reduction in the net weight gain in the final 4 weeks of the study period[4]. Animals treated with exendin-4 have more pancreatic acinar inflammation, more pyknotic nuclei and weigh significantly less than control rats. Exendin-4 treatment is associated with lower leptin levels as well as lower HOMA values in rats[5]. Exenatide causes dose-dependent relaxation of rat thoracic aorta, which is evoked via the GLP-1 receptor and is mediated mainly by H2S but also by NO and CO[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Room temperature in continental US; may vary elsewhere.
Storage
Sealed storage, away from moisture and light, under nitrogen
Powder
-80°C
2 years
-20°C
1 year
*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light, under nitrogen)
Solvent & Solubility
In Vitro:
H2O : 33.33 mg/mL (7.96 mM; Need ultrasonic)
DMSO : ≥ 32 mg/mL (7.64 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : < 1 mg/mL (insoluble)
*"≥" means soluble, but saturation unknown.
Preparing Stock Solutions
ConcentrationSolventMass
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
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View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
*
Note: If you choose water as the stock solution, please dilute it to the working solution,
then filter and sterilize it with a 0.22 μm filter before use.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (0.60 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3
Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (0.60 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 900 μLCorn oil, and mix evenly.
For the following dissolution methods, please prepare the working solution directly.
It is recommended to prepare fresh solutions and use them promptly within a short period of time. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution.
If precipitation or phase separation occurs during preparation,
heat and/or sonication can be used to aid dissolution.
Protocol 1
Add each solvent one by one: PBS
Solubility: 100 mg/mL (23.89 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration:
mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
[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.
[Content Brief]
[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.
[Content Brief]
[3]. 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.
[Content Brief]
[4]. 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.
[Content Brief]
[5]. Nachnani JS, et al. Biochemical and histological effects of exendin-4 (exenatide) on the rat pancreas. Diabetologia. 2010 Jan;53(1):153-9.
[Content Brief]
[6]. Selley E, et al. Exenatide induces aortic vasodilation increasing hydrogen sulphide, carbon monoxide and nitric oxide production. Cardiovasc Diabetol. 2014 Apr 2;13:69.
[Content Brief]
Animal Administration
[4][5]
Rats: 20 Sprague-Dawley male rats, ten of which are treated with exendin-4 (10 μg/kg) and ten of which are used as controls. The study period is 75 days. Serum and pancreatic tissue are removed for biochemical and histological study. Blood glucose, amylase, lipase and adipocytokines are compared between the two groups[5].
Mice: The exendin-4 treatment groups are treated with 10 μg/kg every 24 hours for the first 14 days. This treatment is the induction phase. Respective control mice (lean and ob/ob) receive saline every 24 hours. After 14 days Exendin-4-treated mice are randomly divided into two groups: one group receives high dose exendin-4 (20 μg/kg) every 12 hours, while the second group continues with low dose exendin-4 (10 μg/kg) every 12 hours. The control mice continue to receive saline every 12 hours. The mice are weighed daily for the 60-day treatment period[4].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References
[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.
[Content Brief]
[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.
[Content Brief]
[3]. 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.
[Content Brief]
[4]. 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.
[Content Brief]
[5]. Nachnani JS, et al. Biochemical and histological effects of exendin-4 (exenatide) on the rat pancreas. Diabetologia. 2010 Jan;53(1):153-9.
[Content Brief]
[6]. Selley E, et al. Exenatide induces aortic vasodilation increasing hydrogen sulphide, carbon monoxide and nitric oxide production. Cardiovasc Diabetol. 2014 Apr 2;13:69.
[Content Brief]
[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]. 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.
[4]. 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.
[5]. Nachnani JS, et al. Biochemical and histological effects of exendin-4 (exenatide) on the rat pancreas. Diabetologia. 2010 Jan;53(1):153-9.
[6]. Selley E, et al. Exenatide induces aortic vasodilation increasing hydrogen sulphide, carbon monoxide and nitric oxide production. Cardiovasc Diabetol. 2014 Apr 2;13:69.
Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Optional Solvent
ConcentrationSolventMass
1 mg
5 mg
10 mg
25 mg
DMSO / H2O
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
*
Note: If you choose water as the stock solution, please dilute it to the working solution,
then filter and sterilize it with a 0.22 μm filter before use.
Exendin-4 Related Classifications
Metabolic Disease
GPCR/G Protein
GCGR
Help & FAQs
Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
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