| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Atosiban acetate, the acetate salt of Atosiban (RW-22164; Tractocile; RWJ22164), is a novel and potent peptide-based oxytocin and vasopressin antagonist with the potential to be used for spontaneous preterm labor. It is a desamino-oxytocin analogue that is nonapeptide and a competitive antagonist of the vasopressin/oxytocin receptor (VOTra). Atosiban blocks the release of inositol trisphosphate from the myometrial cell membrane, which is mediated by oxytocin.
| ln Vitro |
Atosiban prevents IP3 from being released from the myometrial cell membrane through the action of oxytocin. Reduced Ca2+ inflow from the extracellular space via voltage-gated channels and decreased release of intracellular, stored calcium from the sacroplasmic reticulum of myometrial cells are the results. Furthermore, atosiban inhibits the release of PGE and PGF from the decidua mediated by oxytocin[1].
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|---|---|
| ln Vivo |
Atosiban prevents IP3 from being released from the myometrial cell membrane through the action of oxytocin. Reduced Ca2+ inflow from the extracellular space via voltage-gated channels and decreased release of intracellular, stored calcium from the sacroplasmic reticulum of myometrial cells are the results[1].
Atosiban inhibits the activation of neurons that express oxytocin receptors in the parabrachial nucleus of mice[2]. |
| References | |
| Additional Infomation |
See also: Atosiban (annotation moved to).
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| Molecular Formula |
C45H71N11O14S2
|
|---|---|
| Molecular Weight |
1054.246
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| Exact Mass |
1053.462
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| Elemental Analysis |
C, 51.27; H, 6.79; N, 14.61; O, 21.25; S, 6.08
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| CAS # |
914453-95-5
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| Related CAS # |
Atosiban; 90779-69-4
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| PubChem CID |
87665603
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| Appearance |
White to off-white solid powder
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| LogP |
3.044
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| Hydrogen Bond Donor Count |
12
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| Hydrogen Bond Acceptor Count |
17
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| Rotatable Bond Count |
18
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| Heavy Atom Count |
72
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| Complexity |
1810
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| Defined Atom Stereocenter Count |
9
|
| SMILES |
C(=O)(O)C.C([C@@H]1CSSCCC(=O)N[C@H](CC2C=CC(OCC)=CC=2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@H](O)C)C(=O)N[C@@H](CC(=O)N)C(=O)N1)(N1CCC[C@H]1C(=O)N[C@@H](CCCN)C(=O)NCC(=O)N)=O
|
| InChi Key |
SVDWBHHCPXTODI-QIWYXCRTSA-N
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| InChi Code |
InChI=1S/C43H67N11O12S2.C2H4O2/c1-5-23(3)35-41(63)53-36(24(4)55)42(64)50-29(20-32(45)56)38(60)51-30(43(65)54-17-8-10-31(54)40(62)49-27(9-7-16-44)37(59)47-21-33(46)57)22-68-67-18-15-34(58)48-28(39(61)52-35)19-25-11-13-26(14-12-25)66-6-2;1-2(3)4/h11-14,23-24,27-31,35-36,55H,5-10,15-22,44H2,1-4H3,(H2,45,56)(H2,46,57)(H,47,59)(H,48,58)(H,49,62)(H,50,64)(H,51,60)(H,52,61)(H,53,63);1H3,(H,3,4)/t23-,24+,27-,28+,29-,30-,31-,35-,36-;/m0./s1
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| Chemical Name |
acetic acid;(2S)-N-[(2S)-5-amino-1-[(2-amino-2-oxoethyl)amino]-1-oxopentan-2-yl]-1-[(4R,7S,10S,13S,16R)-7-(2-amino-2-oxoethyl)-13-[(2S)-butan-2-yl]-16-[(4-ethoxyphenyl)methyl]-10-[(1R)-1-hydroxyethyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]pyrrolidine-2-carboxamide
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| Synonyms |
ORF-22164; RWJ 22164; ORF 22164; RWJ22164; ORF22164; RWJ-22164; Atosiban; trade names: Tractocile; Antocin
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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) |
DMSO: ~100 mg/mL (~94.9 mM)
H2O: ~50 mg/mL (~47.4 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.37 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.37 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.37 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (94.86 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9485 mL | 4.7427 mL | 9.4854 mL | |
| 5 mM | 0.1897 mL | 0.9485 mL | 1.8971 mL | |
| 10 mM | 0.0949 mL | 0.4743 mL | 0.9485 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05693688 | Recruiting | Drug: Atosiban | Preterm Birth | Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA) |
December 1, 2017 | Phase 4 |
| NCT05382143 | Recruiting | Drug: Atosiban | Endometriosis | Radboud University Medical Center | February 1, 2022 | Phase 2 |
| NCT03570294 | Completed | Drug: Atosiban | Premature Birth | Polish Mother Memorial Hospital Research Institute |
February 1, 2014 | Not Applicable |
| NCT01501214 | Completed | Drug: Atosiban Drug: Normal saline |
Subfertility | The University of Hong Kong | December 2011 | Phase 4 |
| NCT00599898 | Completed | Drug: Atosiban Drug: Nifedipine |
Labor, Premature | Raed Salim | January 2008 | Phase 4 |
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