| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
This peptide fragment may interact with incretin receptors including GLP-1R as part of the exendin peptide family, though the specific binding affinity of the truncated 64-86 fragment is not fully characterized compared to the full-length exendin-4. Full-length exendin-4 (exenatide) acts as a GLP-1R agonist with IC50 of 3.22 nM. The 64-86 region may contribute to receptor interactions or peptide stability.
|
|---|---|
| ln Vitro |
Cellular and biochemical activities of this specific fragment (64-86) are not well-documented in published literature. Full-length exendin-4 promotes glucose-dependent insulin secretion, suppresses glucagon release, slows gastric emptying, and promotes beta-cell proliferation. As a C-terminal fragment, exendin-3/4 (64-86) may serve as a research tool for studying exendin structure-function relationships.
|
| ln Vivo |
In vivo studies specific to exendin-3/4 (64-86) are not reported in major databases. However, full-length exendin-4 is widely used in diabetes research to lower blood glucose levels, improve glycemic control, and reduce body weight in animal models. The 64-86 fragment may be studied for its contribution to the in vivo stability and activity of full-length exendin peptides.
|
| Enzyme Assay |
Due to limited data for this specific fragment, a generic protocol for peptide-receptor binding can be described: coat assay plates with GLP-1 receptor protein, add varying concentrations of FITC-labeled exendin-3/4 (64-86) (1 pM-1 uM) in binding buffer (50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA, pH 7.4), incubate at 25degC for 2 hours, wash, and measure fluorescence or perform competition with unlabeled exendin-4.
|
| Cell Assay |
Culture GLP-1R-expressing cell lines (e.g., INS-1 pancreatic beta cells or transfected HEK293-GLP-1R cells) in appropriate medium with 10% FBS. Treat cells with exendin-3/4 (64-86) at concentrations ranging from 0.1 nM to 10 uM for 15-60 minutes. Measure cAMP accumulation by ELISA or homogeneous time-resolved fluorescence (HTRF) as a readout of GLP-1R activation. Alternatively, assess downstream signaling such as ERK phosphorylation by Western blot or calcium flux using fluorescent indicators.
|
| Animal Protocol |
For in vivo pharmacology studies in rodent models, dissolve exendin-3/4 (64-86) in saline or PBS and administer via intraperitoneal injection at doses of 1-100 nmol/kg to mice or rats. For glucose tolerance testing, perform oral glucose tolerance test (OGTT) or intraperitoneal glucose tolerance test (IPGTT) 30 minutes after peptide administration, collecting blood glucose measurements at 0, 15, 30, 60, and 120 minutes post-glucose load. Collect plasma for insulin measurement by ELISA.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data specific to exendin-3/4 (64-86) are not available. Full-length exendin-4 has a plasma half-life of approximately 2.4 hours in humans (compared to 2 minutes for native GLP-1), primarily due to resistance to dipeptidyl peptidase-4 (DPP-4) degradation due to its N-terminal histidine-alanine sequence. The 64-86 fragment may be subject to proteolytic degradation and rapid renal clearance.
|
| Toxicity/Toxicokinetics |
The toxicity profile of exendin-3/4 (64-86) is not specifically characterized. Full-length exendin-4 is well-tolerated at therapeutic doses, with adverse effects including nausea, vomiting, and diarrhea being the most common in human use. At supra-pharmacological doses, potential pancreatic and renal effects have been reported. The 64-86 fragment is not considered acutely toxic.
|
| References |
[1]. CN 106029087 A
|
| Additional Infomation |
Exendin-3/4 (64-86) is a research-grade peptide. The full-length sequence is also known as exenatide, which is an FDA-approved drug for type 2 diabetes marketed as Byetta/Bydureon. This C-terminal fragment (64-86) has the sequence EAVRLFIEWLKNGGPSSGAPPPS. Molecular weight is 2409.75 g/mol, formula C110H169N29O32. It is soluble in water. Store powder at -20degC, protected from moisture.
|
| Molecular Formula |
C110H169N29O32
|
|---|---|
| Molecular Weight |
2409.75
|
| Appearance |
Typically exists as solid at room temperature
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 0.4150 mL | 2.0749 mL | 4.1498 mL | |
| 5 mM | 0.0830 mL | 0.4150 mL | 0.8300 mL | |
| 10 mM | 0.0415 mL | 0.2075 mL | 0.4150 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
