| Size | Price | Stock | Qty |
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| 10mg |
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| Other Sizes |
| Targets |
Des His1, Glu8 Exendin-4 specifically targets the glucagon-like peptide-1 receptor (GLP-1-R), acting as a potent antagonist. By blocking the GLP-1 receptor, it prevents the binding of endogenous GLP-1 and exogenous GLP-1 receptor agonists, thereby inhibiting GLP-1-mediated signaling. This allows researchers to study the effects of GLP-1 receptor signaling by blocking it and observing the resulting changes in insulin secretion, glucose production, and other metabolic processes.
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| ln Vitro |
In vitro, Des His1, Glu8 Exendin-4 functions as a GLP-1-R antagonist. Specific in vitro activity data, such as IC50 or Ki values, are not detailed in the available sources. However, its ability to bind to the GLP-1 receptor and block agonist-induced signaling has been characterized. It is typically used in cell-based assays to study GLP-1 receptor function, such as measuring cAMP production or assessing insulin secretion from pancreatic beta cells.
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| ln Vivo |
Des His1, Glu8 Exendin-4 (dH-EX) (i3vt injection; 50 μg, 2 μL/15 s) controls the synthesis of glucose and the secretion of insulin to maintain glucose homeostasis[1].
In vivo, Des His1, Glu8 Exendin-4 (50 μg, 2 μL/15 s, i3vt injection) has been shown to improve glucose homeostasis in rats by regulating insulin secretion and glucose production. It has been used to study the role of arcuate GLP-1 receptors in regulating glucose homeostasis but not food intake. In these studies, the antagonist is administered via intracerebroventricular (i3vt) injection to specifically target GLP-1 receptors in the brain. |
| Enzyme Assay |
Non-cellular receptor binding assays for Des His1, Glu8 Exendin-4 involve measuring its binding affinity to the GLP-1 receptor. These assays typically use radioligand binding techniques, where the peptide is incubated with membranes expressing the GLP-1 receptor and a labeled, high-affinity ligand. The ability of the peptide to displace the radioligand is measured, and binding parameters such as the dissociation constant (Kd) are determined.
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| Cell Assay |
In vitro cellular assays for Des His1, Glu8 Exendin-4 are performed using cells that express the GLP-1 receptor, such as pancreatic beta cell lines or recombinant cells. The compound's ability to inhibit GLP-1 or Exendin-4-induced signaling is measured. Typically, the production of cyclic AMP (cAMP), a downstream second messenger of GLP-1 receptor activation, is quantified. The antagonist's potency is determined by measuring the shift in the agonist dose-response curve.
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| Animal Protocol |
Animal/Disease Models: Rat[1]
Doses: 50 μg, 2 μl/15 s Route of Administration: i3vt injection Experimental Results: demonstrated hyperglycemic for the first 45 min after the intraperitoneal (ip)glucose load. Dramatically increased insulin levels and insulin area under the curve (AUC) during the IVGTT. In vivo animal experiments for Des His1, Glu8 Exendin-4 are typically conducted in rats or mice. The compound is administered via various routes, including intracerebroventricular (i3vt) injection to study central effects, or peripherally to study systemic effects. Endpoints include measurements of blood glucose, insulin levels, and glucose tolerance during intraperitoneal glucose tolerance tests (IPGTT) or intravenous glucose tolerance tests (IVGTT). |
| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties for Des His1, Glu8 Exendin-4 are not detailed in the available sources. As a peptide with a molecular weight of 4063.46, its PK would be influenced by factors such as proteolytic degradation, renal clearance, and potential binding to plasma proteins. It is typically administered via injection to bypass first-pass metabolism. The stability and half-life of the peptide in vivo would be key determinants of its experimental utility.
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| Toxicity/Toxicokinetics |
Toxicological data for Des His1, Glu8 Exendin-4 are not provided in the available sources. As a research peptide, its safety profile has not been extensively characterized. It is intended for research use only and not for human consumption.
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| References |
[1]. Darleen A Sandoval, et al. Arcuate glucagon-like peptide 1 receptors regulate glucose homeostasis but not food intake. Diabetes. 2008 Aug;57(8):2046-54.
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| Additional Infomation |
Des His1, Glu8 Exendin-4 has a molecular weight of 4063.46 and a sequence of GEGTFTSELSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2. It is a potent GLP-1 receptor antagonist used for research on diabetes and obesity. It is a valuable tool for studying the role of GLP-1 receptors in glucose homeostasis and other physiological processes. It is not approved for clinical use.
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| Molecular Formula |
C179H277N47O59S
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| Molecular Weight |
4063.46
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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 |
| 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 | 0.2461 mL | 1.2305 mL | 2.4610 mL | |
| 5 mM | 0.0492 mL | 0.2461 mL | 0.4922 mL | |
| 10 mM | 0.0246 mL | 0.1230 mL | 0.2461 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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