| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
This peptide targets the Glucagon Receptor (GCGR) and is part of the GPCR/G Protein signaling pathway. As an Exendin-4 peptide derivative, it may relate to dual GLP-1/glucagon receptor agonists. Exendin-4 is a pure GLP-1 receptor agonist, and this derivative likely interacts with the glucagon-like peptide-1 receptor (GLP-1R) which is a key target for metabolic research.
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| ln Vitro |
Exendin-4 is a pure agonist of the GLP-1 receptor. Structurally generated from exendin-4, exendin-4 peptide derivatives may have a connection to dual GLP-1/glucagon receptor agonists. Their usage in medicine, for instance, includes reducing excessive food consumption and treating metabolic syndrome illnesses like diabetes and obesity. In order to lower the risk of hypoglycemia, these dual GLP-1/glucagon receptor agonists exhibit decreased action on the GIP receptor[1].
In vitro, Exendin-4 is a pure GLP-1 receptor agonist. Exendin-4 peptide derivatives, including this compound, are structurally derived from Exendin-4 and may be related to dual GLP-1/glucagon receptor agonists. Their medical use includes the treatment of metabolic syndrome disorders such as diabetes and obesity. Dual GLP-1/glucagon receptor agonists show reduced activity on the GIP receptor to lower the risk of hypoglycemia. |
| ln Vivo |
In vivo studies have not been specifically reported for this fragment. However, as an Exendin-4 derivative and potential dual GLP-1/glucagon receptor agonist, it may be studied in animal models of metabolic syndrome for applications including reducing excessive food intake and treating diabetes and obesity. Further in vivo characterization is needed to confirm its activity.
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| Enzyme Assay |
For GLP-1 receptor binding assays: Coat 96-well plates with purified GLP-1R protein (0.5-1 ug/well) overnight at 4degC. Block with 1% BSA for 1 hour. Add increasing concentrations of the test peptide (1 pM-1 uM) in binding buffer (50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA, pH 7.4) and incubate for 2 hours at 25degC. Wash three times, add HRP-conjugated secondary antibody, incubate, and measure absorbance at 450 nm. Determine IC50 using nonlinear regression.
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| Cell Assay |
Culture GLP-1R-expressing cells (e.g., INS-1 pancreatic beta cells) in RPMI-1640 with 10% FBS. For cAMP assays, treat cells with the peptide at concentrations ranging from 0.1 nM to 10 uM for 15-30 minutes. Lyse cells and measure intracellular cAMP levels using a homogeneous time-resolved fluorescence (HTRF) assay kit. For insulin secretion, incubate cells in Krebs-Ringer buffer with 2.8 mM or 16.7 mM glucose and peptide (1 nM-1 uM) for 1 hour. Collect supernatant and measure insulin by ELISA.
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| Animal Protocol |
For glucose tolerance studies, dissolve the peptide in sterile saline and administer to C57BL/6 mice or STZ-induced diabetic rats via intraperitoneal injection at doses of 1-100 nmol/kg, 30 minutes before an oral glucose load (2 g/kg). Collect blood from the tail vein at 0, 15, 30, 60, 90, and 120 minutes post-glucose. Measure blood glucose using a glucometer and plasma insulin by ELISA. Assess glucose tolerance by calculating area under the curve (AUC).
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| ADME/Pharmacokinetics |
Pharmacokinetic data for this specific peptide are limited. As a synthetic peptide derivative of Exendin-4, it is expected to have improved stability and resistance to DPP-4 degradation compared to native GLP-1, which has a half-life of only 2 minutes. Exendin-4 has a plasma half-life of approximately 2.4 hours in humans. The TFA salt form enhances water solubility and stability for research applications. The peptide should be stored as a lyophilized powder at -20degC, protected from light and moisture.
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| Toxicity/Toxicokinetics |
Specific toxicity data are not available for this peptide. As a research-grade peptide derivative, it is not intended for human use. The peptide is expected to have low toxicity at typical research concentrations (nM to uM range). Standard laboratory precautions should be used when handling. The TFA salt may cause irritation to eyes and respiratory tract. Perform risk assessment before use and handle with appropriate personal protective equipment.
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| References |
[1]. US20150315260 A1
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| Additional Infomation |
This peptide is designated for research use only. It is not approved for clinical or diagnostic applications. The compound is an Exendin-4 peptide derivative as described in patent US20150315260 A1. It may be used in studies of dual GLP-1/glucagon receptor agonism for the treatment of metabolic syndrome. The peptide sequence is Phe-Thr-Ser-Asp-Val-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser.
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| Molecular Weight |
3692.15
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| Appearance |
Typically exists as solid at room temperature
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.2708 mL | 1.3542 mL | 2.7084 mL | |
| 5 mM | 0.0542 mL | 0.2708 mL | 0.5417 mL | |
| 10 mM | 0.0271 mL | 0.1354 mL | 0.2708 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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