| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Glucagon-like peptide-1 receptor (GLP-1R). The parent compound, Exendin-4, is a pure GLP-1 receptor agonist (incretin mimetic). {Val1}-Exendin-3/4 is a fragment of Exendin-4 and retains activity at the GLP-1 receptor. This receptor is the primary target for treating type 2 diabetes and obesity, as its activation enhances insulin secretion (glucose-dependent) and promotes satiety.
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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 and its derivatives, including {Val1}-Exendin-3/4, act as GLP-1 receptor agonists. Structurally derived from exendin-4, exendin-4 peptide derivatives may have a connection to dual GLP-1/glucagon receptor agonists. These dual agonists show reduced activity on the GIP receptor to reduce the risk of hypoglycemia. The peptide is used to study incretin signaling in beta-cell lines.. |
| ln Vivo |
In vivo, Exendin-4 peptide derivatives, like {Val1}-Exendin-3/4, are used to treat metabolic syndrome disorders, including diabetes and obesity, as well as for reduction of excess food intake. They are being studied as dual GLP-1/glucagon receptor agonists to maximize weight loss and glycemic control while minimizing gastrointestinal side effects.
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| Enzyme Assay |
A non-cell binding assay, such as surface plasmon resonance (SPR), is performed to confirm GLP-1R binding. Recombinant human GLP-1R protein is immobilized on a sensor chip. Varying concentrations of {Val1}-Exendin-3/4 are flowed over the chip to measure the binding affinity (Kd). Alternatively, a radioactive ligand competition assay using [125I]-GLP-1 is used.
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| Cell Assay |
A functional cAMP accumulation assay is performed using HEK293 cells stably expressing the human GLP-1 receptor. Cells are seeded in 96-well plates and treated with varying concentrations of the peptide (0.001-1000 nM) in the presence of 1 mM IBMX. After 30 minutes, cAMP levels are measured by HTRF or ELISA. The EC50 for cAMP stimulation is calculated from the dose-response curve.
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| Animal Protocol |
In vivo efficacy for metabolic indications is studied in rodent models. For an acute glucose-lowering test, male C57BL/6J mice are fasted overnight. The peptide is administered subcutaneously (SC) at doses of 10-100 ug/kg. An oral glucose tolerance test (OGTT) is performed 30 minutes later, and blood glucose is measured at intervals. Chronic administration studies in diet-induced obesity (DIO) mice monitor body weight and food intake.
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| ADME/Pharmacokinetics |
The peptide has a molecular weight of 3241.70. It is soluble in water (H2O) and DMSO. For in vivo administration, the peptide is formulated in sterile saline or PBS (pH 7.4). Peptides generally have short plasma half-lives (30-60 minutes) due to rapid proteolytic degradation and renal clearance. Stability is improved by the acetate salt form. Storage: -80degC.
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| Toxicity/Toxicokinetics |
The toxicity of {Val1}-Exendin-3/4 is not well-documented. GLP-1 agonists as a class are generally well-tolerated. Common side effects of GLP-1 agonists include gastrointestinal disturbances (nausea, vomiting, diarrhea) and potential risk of pancreatitis. The peptide is for research use only and not for human therapeutic use.
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| References |
[1]. US20150315260 A1
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| Additional Infomation |
{Val1}-Exendin-3/4 is a research-grade peptide used as a GLP-1 receptor agonist. It is not a drug and has no FDA approval for human therapy. It is used to study incretin mimetics and dual GLP-1/glucagon receptor agonists for treating metabolic syndrome illnesses like diabetes and obesity. This product is for research use only (RUO).
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| Molecular Weight |
3241.70
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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 | 0.3085 mL | 1.5424 mL | 3.0848 mL | |
| 5 mM | 0.0617 mL | 0.3085 mL | 0.6170 mL | |
| 10 mM | 0.0308 mL | 0.1542 mL | 0.3085 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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