![[Arg8]-Vasotocin TFA](/upload/1124/V77346.png)
| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Vasopressin (V1a, V1b, V2) and oxytocin receptors. [Arg8]-Vasotocin is a non-selective agonist that activates multiple receptors within the vasopressin/oxytocin family. In mammals, it binds to and activates the V1a (vascular), V1b (pituitary), V2 (renal), and oxytocin receptors, regulating osmoregulation, reproductive behaviors, and stress responses. It also activates a unique subset of dorsal vagal complex neurons not responsive to vasopressin, suggesting action through novel CNS receptors.
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| ln Vitro |
[Arg8]-Vasotocin is a substance found in all vertebrate phyla, including birds. It is found in cyclostomes, primitive fish, and other vertebrates. In vitro, neurones in the dorsal vagal complex are stimulated by [Arg8]-vasotocin[2].
In vitro, [Arg8]-Vasotocin (TFA) excites neurones in the dorsal vagal complex. This effect is not completely blocked by standard V1a or oxytocin receptor antagonists, providing evidence for an action through novel class(es) of CNS receptors. It is used to study the electrophysiological properties of neurons in the suprachiasmatic nucleus (SCN) and other brain regions, helping to elucidate the neural circuits controlling circadian rhythms and autonomic function. |
| ln Vivo |
In vivo, [Arg8]-Vasotocin is used as a pharmacological tool to study osmoregulation, social behaviors, and stress responses in non-mammalian vertebrates as well as in mammals. In fish and amphibians, it plays a critical role in water balance and spawning behavior. In rodents, administration can mimic the effects of vasopressin, increasing blood pressure (via V1a), stimulating ACTH release (via V1b), and promoting water reabsorption (via V2), with some unique effects due to incomplete selectivity for the oxytocin receptor.
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| Enzyme Assay |
A non-cell radioligand binding assay is performed to determine receptor affinity. Membranes from CHO cells expressing human V1a, V1b, V2, or oxytocin receptors are incubated with the appropriate radioligand (e.g., [3H]-AVP for V1a/V2, [125I]-OVTA for OTR) and varying concentrations of [Arg8]-Vasotocin TFA. After incubation at 25degC for 60 minutes, the mixture is filtered through GF/B filters, and bound radioactivity is counted. The Ki values for each receptor subtype are calculated and compared.
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| Cell Assay |
For cellular electrophysiology studies, brain slices containing the dorsal vagal complex (DVC) or suprachiasmatic nucleus (SCN) are prepared from juvenile rats or mice. Whole-cell patch-clamp recordings are performed on identified neurons. [Arg8]-Vasotocin TFA is applied to the perfusate at concentrations ranging from 1-1000 nM. The firing rate of neurons is measured before, during, and after washout of the peptide. An increase in firing rate indicates neuronal excitation, which is not completely blocked by standard vasopressin and oxytocin receptor antagonists, confirming a novel mechanism.
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| Animal Protocol |
In vivo studies to investigate the effects on blood pressure and osmoregulation are performed in anesthetized rats. The carotid artery is cannulated for blood pressure measurement via a pressure transducer. [Arg8]-Vasotocin TFA is administered intravenously (IV) at doses of 0.1-10 ug/kg as a bolus injection. The pressor response (increase in mean arterial pressure) is recorded. To study antidiuretic effects, the peptide can be administered to water-loaded rats, and urine output is measured over several hours using a metabolic cage.
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| ADME/Pharmacokinetics |
[Arg8]-Vasotocin TFA is soluble in water (50 mg/mL) and DMSO. As a nonapeptide, it has a short plasma half-life (minutes) due to rapid degradation by peptidases in the blood and tissues. For in vivo studies, it is typically formulated in sterile saline or PBS. The TFA salt enhances water solubility, allowing for easy preparation of stock solutions. Storage: lyophilized powder at -80degC; in solvent at -80degC for 6 months, sealed and protected from moisture and light.
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| Toxicity/Toxicokinetics |
Toxicity data for [Arg8]-Vasotocin TFA is not documented. As a neuropeptide analogue of vasopressin, it is well-tolerated at the low doses used for research (e.g., 0.1-10 ug/kg). At very high systemic doses, it could cause severe hypertension, water retention (hyponatremia, cerebral edema), and mesenteric ischemia due to potent V1a receptor-mediated vasoconstriction. However, these effects are not observed at standard research doses. The TFA salt is non-toxic.
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| References |
[1]. Ingram CD, et al [Arg8]vasotocin excites neurones in the dorsal vagal complex in vitro: evidence for an action through novel class(es) of CNS receptors. J Neuroendocrinol. 1994 Aug;6(4):415-22.
[2]. Mihai R, et al. The effects of [Arg8]vasotocin on the firing rate of suprachiasmatic neurons in vitro. Neuroscience. 1994 Oct;62(3):783-92. |
| Additional Infomation |
[Arg8]-Vasotocin TFA is a research-grade chemical used for comparative endocrinology and neuropharmacology. It is the ancestral hormone from which both vasopressin and oxytocin evolved in mammals. It has been used extensively in studies of the CNS to identify novel classes of receptors in the dorsal vagal complex and suprachiasmatic nucleus. Key references include Ingram CD, et al. (1994) and Mihai R, et al. (1994). This product is for research use only (RUO) and is not a clinical drug.
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| Molecular Formula |
C45H68F3N15O14S2
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| Molecular Weight |
1164.24
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| Related CAS # |
[Arg8]-Vasotocin;113-80-4
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| Appearance |
Typically exists as solid at room temperature
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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 (~42.95 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 | 0.8589 mL | 4.2946 mL | 8.5893 mL | |
| 5 mM | 0.1718 mL | 0.8589 mL | 1.7179 mL | |
| 10 mM | 0.0859 mL | 0.4295 mL | 0.8589 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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