| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Oxytocin parallel dimer TFA targets both oxytocin receptors (OTR) and vasopressin receptors (V1aR, V1bR, and V2R). The dimeric structure allows it to interact with these G protein-coupled receptors (GPCRs) through the same binding determinants as the native monomer. The parallel dimer configuration may influence receptor selectivity and signaling bias compared to the monomer. Activation of OTR and vasopressin receptors leads to distinct downstream signaling cascades through Gq/11 and Gs pathways, resulting in smooth muscle contraction, water reabsorption, and other physiological effects characteristic of neurohypophyseal peptides.
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| ln Vitro |
The dicystine dimers of oxytocin and deaminated oxytocin, whether homogeneous or heterogeneous, have biological activity ranging from 0.2% to 6% of oxytocin [1].
In vitro studies have characterized the biological activity of oxytocin parallel dimer TFA. The dimer's biological activity, including both oxytocin and vasopressin-like effects, ranges from 0.2% to 6% of that of native oxytocin. This reduced potency is consistent with observations that dimeric forms generally exhibit lower receptor binding affinity compared to the monomer, likely due to steric hindrance affecting optimal interaction with the receptor binding pocket. The parallel and antiparallel homodimers and heterodimers of oxytocin and deamino-oxytocin have been systematically evaluated to define how oligomerization impacts bioactivity. |
| ln Vivo |
In comparison to oxytocin (LD50=43 mg/kg vs. 25 mg/kg), oxytocin dimer (intravenous injection; single dose) is less immediately hazardous to rats [2].
Oxytocin parallel dimer TFA shows reduced acute toxicity compared to oxytocin. In intravenous administration studies in rats, the dimer exhibits an LD50 of 43 mg/kg, whereas native oxytocin has an LD50 of 25 mg/kg under comparable conditions. This indicates a nearly 2-fold improvement in safety margin for the dimeric analog. The compound also maintains vasopressin-like activity, including antidiuretic and pressor effects, with similar potency reduction relative to the monomer. The reduced toxicity may be attributed to altered pharmacokinetics or decreased off-target receptor interactions. |
| Enzyme Assay |
Cell-free receptor binding assays can be performed using membrane preparations from cells expressing recombinant oxytocin or vasopressin receptors. For competition binding, membranes (10-20 microg/well) are incubated with a radiolabeled tracer (e.g., [3H]-oxytocin or [3H]-vasopressin, 0.1-1 nM) and increasing concentrations of unlabeled oxytocin parallel dimer TFA (1 pM-100 microM) in binding buffer (50 mM Tris-HCl, pH 7.4, 5 mM MgCl2, 0.1% BSA) for 60-90 minutes at 25degC. Bound and free radioligand are separated by rapid filtration through GF/B filters presoaked in 0.3% PEI. Filters are washed three times with ice-cold buffer, dried, and counted. Ki values are calculated from IC50 using the Cheng-Prusoff equation.
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| Cell Assay |
Cell-based functional assays using CHO or HEK293 cells stably expressing oxytocin or vasopressin receptors are standard. Cells seeded in 96-well plates are loaded with Fluo-4 AM (2 microM, 60 min, 37degC). After washing, varying concentrations of oxytocin parallel dimer TFA (1 pM-10 microM) are added. Intracellular calcium mobilization is measured using a fluorescence plate reader (ex/em 494/516 nm). For cAMP assays, cells are treated with 3-isobutyl-1-methylxanthine (IBMX, 0.5 mM) for 10 minutes, followed by compound addition. After 30 minutes at 37degC, cAMP levels are quantified using a competitive ELISA or HTRF detection kit. EC50 values are determined from dose-response curves.
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| Animal Protocol |
In vivo toxicity studies of oxytocin parallel dimer TFA are conducted in male Wistar rats (200-250 g). The compound is dissolved in sterile saline and administered as a single intravenous injection via the tail vein at escalating doses (10, 25, 50, 100 mg/kg). Rats are observed continuously for 4 hours post-dosing and daily for 14 days for signs of toxicity (behavioral changes, respiratory distress, convulsions). Mortality is recorded to determine the LD50. For vasopressin-like activity assessment, water-loaded rats (5% body weight water load) are anesthetized, and the compound (0.1-100 microg/kg) is injected intravenously. Urine flow is measured over a 60-minute period to evaluate antidiuretic activity. Blood pressure changes are monitored via carotid artery cannulation to measure pressor response.
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| ADME/Pharmacokinetics |
The TFA salt form has a molecular weight of 2128.4 g/mol with formula C88H133F3N24O26S4. The peptide sequence comprises two copies of CYIQNCPLG (disulfide bridges: chain1 Cys1 to chain2 Cys1; chain1 Cys6 to chain2 Cys6). The lyophilized powder should be stored at -20degC, protected from moisture, where it is stable for up to 3 years. For solution storage, it should be kept at -80degC for up to 1 year. The compound is soluble in DMSO and can be formulated for in vivo administration using vehicles such as 10% DMSO + 40% PEG300 + 5% Tween80 + 45% saline.
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| Toxicity/Toxicokinetics |
Oxytocin parallel dimer TFA is for research use only and not for human therapeutic applications. The TFA counterion is generally non-toxic at concentrations used in peptide research but may interfere with some cell-based assays at high concentrations (>0.1%). Standard laboratory safety practices, including the use of gloves, lab coats, and eye protection, should be followed when handling the compound. The compound is not intended for in vivo dosing in humans and should be used only for preclinical research under appropriate animal welfare guidelines.
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| References |
[1]. Chen L, et al. Syntheses and biological activities of parallel and antiparallel homo and hetero bis-cystine dimers of oxytocin and deamino-oxytocin. Pept Res. 1996;9(3):114-121.
[2]. Berde B, et al. Some pharmacological properties of oxytocin-dimers (α+ β)[J]. Experientia, 1971, 27: 1304-1305. |
| Additional Infomation |
The dimer represents a class of neurohypophyseal hormone analogs with modified oligomerization states. Native oxytocin is a 9-amino acid peptide (CYIQNCPLG-NH2) with a single disulfide bridge. Dimerization through additional disulfide bonds alters the spatial presentation of receptor-interacting residues. The reduced toxicity of oxytocin dimers compared to the monomer makes them potentially useful for structure-activity relationship studies. This compound is not a clinically approved drug and is intended solely for research applications in endocrinology, receptor pharmacology, and peptide chemistry. Supplier information must not be included.
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| Molecular Formula |
C88H133F3N24O26S4
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| Related CAS # |
Oxytocin parallel dimer;19645-28-4
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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.) |
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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