| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Exendin derivative 1 targets the glucagon-like peptide-1 receptor (GLP-1R), a G-protein coupled receptor (GPCR) expressed in pancreatic beta cells, as well as in the brain, heart, kidney, and gastrointestinal tract. Activation of GLP-1R stimulates adenylyl cyclase, leading to increased cAMP production and downstream signaling through PKA and Epac, resulting in glucose-dependent insulin secretion.
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| ln Vitro |
In vitro, exendin derivative 1 binds to GLP-1R with high affinity and activates receptor-mediated signaling pathways. It stimulates cAMP production, activates ERK/MAPK signaling, and induces insulin secretion from pancreatic beta-cell lines. The structural modifications present in this derivative offer enhanced stability and unique functional properties, supporting its utility in peptide research focused on metabolic regulation and receptor pharmacology.
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| ln Vivo |
In vivo, exendin derivative 1 improves glucose tolerance, enhances insulin secretion, and reduces blood glucose levels in diabetic animal models. Its engineered modifications increase resistance to enzymatic degradation (particularly DPP-4) and extend biological half-life compared to native exendin-4. It serves as a valuable research tool for studying incretin signaling, glucose regulation, and diabetes therapeutics.
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| Enzyme Assay |
For GLP-1 receptor binding assays: coat 96-well plates with GLP-1R protein (0.5-1 ug/well) overnight at 4degC. Block with 1% BSA in PBS for 1 hour at room temperature. Add varying concentrations of exendin derivative 1 (1 pM-1 uM) in binding buffer, incubate for 2 hours at 25degC. Wash, add HRP-labeled secondary antibody or use FITC-labeled competitor, and measure absorbance or fluorescence. Calculate IC50 using nonlinear regression.
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| Cell Assay |
Culture GLP-1R-expressing cells (e.g., INS-1 832/13 rat insulinoma cells, or transfected HEK293-GLP-1R cells) in RPMI-1640 with 10% FBS, 10 mM HEPES, 1 mM sodium pyruvate, and 50 uM beta-mercaptoethanol. For cAMP assays, treat cells with exendin derivative 1 (0.1 pM-1 uM) for 15-30 minutes, lyse, and measure cAMP levels using an ELISA kit or HTRF assay (Cisbio). For insulin secretion, incubate cells in Krebs-Ringer bicarbonate buffer with 2.8 mM or 16.7 mM glucose and peptide (1 nM-1 uM) for 1 hour, then collect supernatant for insulin ELISA.
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| Animal Protocol |
For glucose tolerance studies, dissolve exendin derivative 1 in sterile saline or PBS. Administer to C57BL/6 mice or diabetic models (db/db mice or STZ-induced diabetic rats) via intraperitoneal injection at doses of 1-100 nmol/kg, 30-60 minutes before an oral or intraperitoneal glucose load (2 g/kg). Collect blood from tail vein at 0, 15, 30, 60, 90, and 120 minutes post-glucose for glucose measurement by glucometer and plasma insulin by ELISA. For pharmacokinetic studies, collect plasma at multiple time points for LC-MS/MS analysis.
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| ADME/Pharmacokinetics |
The engineered modifications provide improved metabolic stability, resulting in an extended half-life compared to native exendin-4, which has a half-life of 2-4 hours in rodents. Resistance to DPP-4 degradation is enhanced. The compound has a molecular weight of 4187.56 g/mol and is soluble in water (up to 50 mg/mL). Storage at -20degC is recommended.
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| Toxicity/Toxicokinetics |
Toxicity data specific to exendin derivative 1 are limited. The general safety profile of exendin-based peptides includes potential for gastrointestinal disturbances (nausea, vomiting, diarrhea) at high doses, as observed with exenatide and other GLP-1 receptor agonists. No significant acute toxicity is expected at research doses (nanomolar to low micromolar ranges in vitro, nmol/kg in vivo).
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| Additional Infomation |
Exendin derivative 1 has a molecular weight of 4187.56 and formula C184H281N49O61S. It is a research-grade peptide with sequence HAEGTFTSDVSKQMEEEAVRLFIEWLKNGGPSSGAPPPSLMNPQRSTVWY (one-letter code) or His-Ala-Glu-Gly-Thr-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-Leu-Met-Asn-Pro-Gln-Arg-Ser-Thr-Val-Trp-Tyr (three-letter code). The compound is exclusively for research use and not intended for clinical or medical purposes.
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| Molecular Formula |
C184H281N49O61S
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| Molecular Weight |
4187.56
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| Appearance |
White to off-white solid powder
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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, avoid exposure to moisture. |
| 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) |
H2O :~50 mg/mL (~11.94 mM)
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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 | 0.2388 mL | 1.1940 mL | 2.3880 mL | |
| 5 mM | 0.0478 mL | 0.2388 mL | 0.4776 mL | |
| 10 mM | 0.0239 mL | 0.1194 mL | 0.2388 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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