![[Asp5]-Oxytocin](/upload/1124/V74427.png)
| Size | Price | Stock | Qty |
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| 5mg |
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| Other Sizes |
| Targets |
Oxytocin receptor. [Asp5]-Oxytocin is a potent analog of the neurohypophyseal hormone oxytocin that acts as an agonist at the oxytocin receptor. It maintains a high affinity for uterine tone receptors and shares the same intrinsic activity as oxytocin. By binding to and activating the oxytocin receptor, it induces uterine contractions and mediates other physiological effects associated with oxytocin signaling.
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| ln Vitro |
[Asp5]-Oxytocin shares the same intrinsic activity as oxytocin and has a strong affinity for uterine tone receptors [1]. One millimolar magnesium dioxide can increase the contractile action of [Asp5]-Oxytocin on the uterus [1]. [Asp5]-Oxytocin, at doses of 20.3, 41, and 0.14 units/mg, respectively, had the same effects as a rat antidiuretic, avian vasodilator, and uterine dilatation [1].
[Asp5]-Oxytocin induces rat uterine contractions in vitro, with its contractile action enhanced by magnesium ions. It exhibits potent uterotonic activity and also demonstrates avian vasostatic and rat antidiuretic capabilities. The compound shares the same intrinsic activity as oxytocin and maintains a strong affinity for uterine tone receptors. These in vitro activities make it a useful tool for studying oxytocin receptor-mediated signaling. |
| ln Vivo |
In vivo, [Asp5]-Oxytocin exhibits rat antidiuretic and avian vasostatic activities. As a neurohypophyseal hormone analog, it would be expected to mediate effects similar to oxytocin, including uterine contraction and antidiuretic effects, when administered in appropriate animal models. Its in vivo effects are mediated through activation of the oxytocin receptor and subsequent downstream signaling pathways.
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| Enzyme Assay |
In vitro receptor binding assays are used to characterize the interaction of [Asp5]-Oxytocin with the oxytocin receptor. Typically, radioligand binding assays are performed using membranes from cells expressing the oxytocin receptor, and the compound's ability to displace a labeled oxytocin ligand is measured to determine its binding affinity. These assays confirm that [Asp5]-Oxytocin maintains high affinity for uterine tone receptors.
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| Cell Assay |
Cellular assays for [Asp5]-Oxytocin involve treating uterine smooth muscle cells or oxytocin receptor-expressing cell lines with the compound and measuring receptor activation. Functional readouts include intracellular calcium mobilization, which is a key downstream signal following oxytocin receptor activation. The compound's ability to induce uterine contractions can be assessed in isolated uterine tissue preparations.
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| Animal Protocol |
In vivo studies with [Asp5]-Oxytocin would be performed in animal models to study its effects on uterine contractility and antidiuretic function. The compound would be administered via injection, and its effects on uterine tone, blood pressure, and urine output would be measured. Its rat antidiuretic and avian vasostatic capabilities have been documented, confirming its in vivo activity as a neurohypophyseal hormone analog.
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| ADME/Pharmacokinetics |
[Asp5]-Oxytocin is a peptide with molecular formula C43H65N11O13S2 and molecular weight of 1008.17. As a peptide hormone analog, its pharmacokinetic properties are characteristic of this class, including a short half-life due to rapid degradation by peptidases. It is typically administered via injection for in vivo studies. The compound is stable as a powder and should be stored desiccated at -20°C.
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| Toxicity/Toxicokinetics |
No specific toxicity data is available for [Asp5]-Oxytocin. As a peptide hormone analog, its toxicity profile would be related to its pharmacological effects, with potential for off-target effects at high doses. Standard preclinical safety studies would be required to evaluate its safety for potential therapeutic applications. The compound is for research use only and not intended for human therapeutic use.
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| References | |
| Additional Infomation |
[Asp5]-Oxytocin (CAS#: 65907-78-0) is a potent 5-position neurohypophyseal hormone analog of oxytocin. It has a molecular formula of C43H65N11O13S2 and a molecular weight of 1008.17. The compound maintains high affinity for uterine tone receptors and shares the same intrinsic activity as oxytocin. It induces rat uterine contractions in vitro, enhanced by magnesium ions, and exhibits rat antidiuretic and avian vasostatic activities. It is a research tool for studying oxytocin receptor pharmacology.
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| Molecular Formula |
C43H65N11O13S2
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| Molecular Weight |
1008.17
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| Exact Mass |
1007.42
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| CAS # |
65907-78-0
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| Related CAS # |
[Asp5]-Oxytocin acetate
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| PubChem CID |
191785
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| Appearance |
White to off-white solid powder
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| LogP |
1.455
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| Hydrogen Bond Donor Count |
12
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| Hydrogen Bond Acceptor Count |
16
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| Rotatable Bond Count |
17
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| Heavy Atom Count |
69
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| Complexity |
1870
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| Defined Atom Stereocenter Count |
8
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| SMILES |
CC[C@H](C)C1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@H](C(=O)N1)CC2=CC=C(C=C2)O)N)C(=O)N3CCC[C@H]3C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N)CC(=O)O)CCC(=O)N
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| InChi Key |
BKQNCZBCEMVEEP-OMTOYRQASA-N
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| InChi Code |
InChI=1S/C43H65N11O13S2/c1-5-22(4)35-42(66)48-26(12-13-32(45)56)38(62)50-29(17-34(58)59)39(63)52-30(20-69-68-19-25(44)36(60)49-28(40(64)53-35)16-23-8-10-24(55)11-9-23)43(67)54-14-6-7-31(54)41(65)51-27(15-21(2)3)37(61)47-18-33(46)57/h8-11,21-22,25-31,35,55H,5-7,12-20,44H2,1-4H3,(H2,45,56)(H2,46,57)(H,47,61)(H,48,66)(H,49,60)(H,50,62)(H,51,65)(H,52,63)(H,53,64)(H,58,59)/t22-,25-,26-,27-,28-,29-,30-,31-,35?/m0/s1
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| Chemical Name |
2-[(4R,7S,10S,16S,19R)-19-amino-4-[(2S)-2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicos-7-yl]acetic acid
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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 | 0.9919 mL | 4.9595 mL | 9.9190 mL | |
| 5 mM | 0.1984 mL | 0.9919 mL | 1.9838 mL | |
| 10 mM | 0.0992 mL | 0.4959 mL | 0.9919 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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