| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
GLP-1 receptor (glucagon-like peptide-1 receptor). SDV-Exendin-3/4 is a peptide ligand that binds to and activates the GLP-1 receptor, which is expressed on pancreatic beta cells and other tissues. Activation of this receptor stimulates glucose-dependent insulin secretion, suppresses glucagon release, slows gastric emptying, and promotes satiety. This mechanism is used in the treatment of type 2 diabetes.
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| ln Vitro |
In vitro, SDV-Exendin-3/4 is a 32-amino acid peptide that acts as a GLP-1 receptor ligand. It plays a key role in glucose metabolism and insulin secretion. The peptide mimics the action of endogenous GLP-1, stimulating cAMP production and insulin secretion in pancreatic beta cells. It is more stable than native GLP-1 and shows potent glucose-lowering activity in cell-based assays.
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| ln Vivo |
In vivo, GLP-1 receptor agonists derived from exendin-4 (such as exenatide) have demonstrated efficacy in lowering blood glucose and promoting weight loss in patients with type 2 diabetes. As a close analog, SDV-Exendin-3/4 is expected to have similar glucose-lowering and insulinotropic properties. Further in vivo studies are needed to characterize its specific pharmacodynamic profile.
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| Enzyme Assay |
GLP-1 receptor binding assay: Membranes prepared from cells expressing human GLP-1 receptors are incubated with 125I-labeled GLP-1 (0.1 nM) and increasing concentrations of unlabeled SDV-Exendin-3/4 (0.001-1000 nM) in binding buffer (50 mM HEPES pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) for 90 min at 25degC. Bound radioactivity is separated by vacuum filtration through GF/C filters pre-soaked in 0.3% PEI. IC50 values are calculated by non-linear regression analysis from triplicate measurements.
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| Cell Assay |
Insulin secretion assay protocol: INS-1 (rat insulinoma) cells or isolated mouse islets are seeded in 96-well plates. Cells are pre-incubated for 1 hour in Krebs-Ringer bicarbonate buffer (KRB) containing 2.8 mM glucose. SDV-Exendin-3/4 (0-1000 nM) is then added in KRB containing 2.8 mM or 16.7 mM glucose for 1 hour at 37degC. Supernatants are collected for insulin measurement by ELISA. cAMP levels in cell lysates are measured using a cAMP ELISA kit. EC50 for insulin secretion is calculated by non-linear regression.
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| Animal Protocol |
Oral glucose tolerance test (OGTT) protocol: Male C57BL/6 mice (or diabetic model mice) are fasted overnight (12-16 hours). SDV-Exendin-3/4 is administered via subcutaneous injection at doses of 0.1-10 ug/kg, 15-30 min before oral glucose challenge (2 g/kg). Blood glucose levels are measured at baseline (0 min) and at 15, 30, 60, 90, and 120 min post-glucose using a glucometer. Plasma insulin levels are measured by ELISA at selected time points. The AUC for glucose is calculated to evaluate glucose-lowering efficacy.
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| ADME/Pharmacokinetics |
PK data for SDV-Exendin-3/4 are limited. As a 32-amino acid peptide (MW 3443.87), it has poor oral bioavailability due to proteolytic degradation and is typically administered via subcutaneous or intravenous injection. The peptide is stable in solution when stored at -20degC. Subcutaneous administration in rodents results in a Tmax of 1-2 hours and plasma half-life of 2-4 hours. The acetate salt is often used to enhance solubility. Solubility in water is <1 mg/mL (slightly soluble to insoluble).
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| Toxicity/Toxicokinetics |
Toxicity data for SDV-Exendin-3/4 are limited. As a GLP-1 receptor agonist, potential adverse effects may include gastrointestinal disturbances (nausea, vomiting), risk of pancreatitis, and thyroid C-cell tumors in rodents. The compound is intended for research use only and not for human therapeutic applications. Exendin-4-based therapeutics (exenatide) are FDA-approved for type 2 diabetes, but SDV-Exendin-3/4 has not been approved. Standard safety precautions should be observed.
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| Additional Infomation |
SDV-Exendin-3/4 is a research peptide for studying GLP-1 receptor physiology and for evaluating potential diabetes therapeutics. It is an analog of exendin-4, which is the active ingredient in exenatide (brand name Byetta/Bydureon), an FDA-approved drug for type 2 diabetes. SDV-Exendin-3/4 differs from exendin-4 by several amino acid residues and may have altered pharmacokinetic properties. It has not entered clinical trials independently. Store as powder at -20degC. Purity ≥98% by HPLC.
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| Molecular Weight |
3443.87
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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 (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 | 0.2904 mL | 1.4519 mL | 2.9037 mL | |
| 5 mM | 0.0581 mL | 0.2904 mL | 0.5807 mL | |
| 10 mM | 0.0290 mL | 0.1452 mL | 0.2904 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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