![[Glu4]-Oxytocin acetate](/upload/1124/V77341.png)
| 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 |
Oxytocin receptor (OTR). Oxytocin receptors are class A G-protein-coupled receptors (GPCRs) involved in social bonding, reproduction, lactation, and metabolic regulation. The modification at position 4 is designed to alter receptor binding properties and potentially enhance metabolic stability compared to the native hormone, allowing researchers to investigate the precise conformational requirements for receptor activation and signaling specificity.
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| ln Vitro |
In vitro, [Glu4]-Oxytocin is used as a tool for the comprehensive investigation of the conformation of oxytocin-like molecules in aqueous solution by a variety of methods, including NMR spectroscopy. By substituting glutamine with glutamic acid, researchers can study the effect of a negative charge at this position on peptide folding and receptor binding affinity. It is an appropriate derivative for conducting structure-activity relationship (SAR) studies of the oxytocin family of peptides.
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| ln Vivo |
Although specific in vivo pharmacological activity data for [Glu4]-Oxytocin is limited, it is designed to interact with oxytocin receptors. The modified structure may enhance receptor binding or alter signaling pathways compared to the native hormone. It is used to understand how single amino acid substitutions impact biological activity in animal models of social behavior, reproduction, and metabolic regulation (e.g., glucose uptake in adipose tissue).
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| Enzyme Assay |
A non-cell radioligand binding assay is performed to determine receptor affinity. Membranes from HEK-293 cells expressing the human oxytocin receptor are incubated with the radioligand [125I]-OVTA (a selective oxytocin antagonist) or [3H]-oxytocin. Varying concentrations of [Glu4]-Oxytocin acetate (0.01 nM to 10 uM) are added to compete for binding. After incubation at 25degC for 60-90 minutes, bound and free radioligand are separated by rapid filtration through GF/B filters pre-treated with 0.3% PEI. Bound radioactivity is counted to calculate the Ki.
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| Cell Assay |
A functional intracellular calcium mobilization assay is used. Cells expressing the oxytocin receptor (e.g., HEK-293-OTR) are loaded with a calcium-sensitive fluorescent dye, such as Fluo-4 AM. The cells are then stimulated with varying concentrations of [Glu4]-Oxytocin acetate (0.01-1000 nM). The change in fluorescence (ex/em 490/525 nm) is measured using a fluorescence plate reader (e.g., FLIPR). The EC50 for intracellular calcium release is calculated, and the maximal response is compared to that of native oxytocin to determine the intrinsic efficacy.
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| Animal Protocol |
For in vivo pharmacological studies, [Glu4]-Oxytocin acetate would be administered to laboratory rats or mice via intracerebroventricular (ICV) injection (1-10 ug/mouse) or intraperitoneally (IP, 100-1000 ug/kg). Behavioral tests to assess social recognition or maternal behavior could be performed following administration. Alternatively, it could be used to study metabolic effects, such as measuring glucose uptake in adipose tissue or skeletal muscle. The peptide's effects would be compared to those of native oxytocin to determine the impact of the Glu4 substitution.
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| ADME/Pharmacokinetics |
As a synthetic peptide, the acetate salt is soluble in water and most organic solvents. The plasma half-life of oxytocin derivatives is typically short (a few minutes) due to rapid degradation by oxytocinase (a placental leucine aminopeptidase). The [Glu4] modification may improve resistance to enzymatic hydrolysis, potentially increasing its bioavailability compared to the native hormone. For stability, the peptide should be stored as a lyophilized powder at -80degC.
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| Toxicity/Toxicokinetics |
The toxicity of [Glu4]-Oxytocin acetate is not documented beyond the known effects of oxytocin. As a derivative of a naturally occurring hormone, acute toxicity is expected to be low. The primary risks are related to its pharmacological activity at the oxytocin receptor, which at high doses could lead to potentiated uterine contractions (in pregnant animals) or hyponatremia (water retention). No off-target toxicity has been reported for this derivative.
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| References |
[1]. Walter R, et al. H N.M.R. study of the conformation of [Glu4] oxytocin and its lanthanide complexes in aqueous solution. Int J Pept Protein Res. 1981;17(1):56-64.
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| Additional Infomation |
[Glu4]-Oxytocin acetate is a research-grade chemical used exclusively for studying the conformation of oxytocin-like molecules. It is not a drug and has no FDA approval. It was first described in the literature as a tool to comprehensively investigate the conformation of oxytocin-like molecules in aqueous solution. This product is an appropriate derivative for conducting such SAR studies of the oxytocin family of peptides. It is for research use only (RUO).
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| Molecular Formula |
C45H69N11O15S2
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| Molecular Weight |
1068.22
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| Related CAS # |
[Glu4]-Oxytocin;4314-67-4
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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 | 0.9361 mL | 4.6807 mL | 9.3614 mL | |
| 5 mM | 0.1872 mL | 0.9361 mL | 1.8723 mL | |
| 10 mM | 0.0936 mL | 0.4681 mL | 0.9361 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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