Biological Activity
Potent oxytocin receptor (OTR) antagonist. Inhibits oxytocin-induced increase in Ca2+ concentration in myometrial cells in vitro (IC50 = 5 nM) Activates NF-κB and MAPK pathways in human amnion via Gαi signaling, resulting in pro-inflammatory effects. Inhibits oxytocin-induced uterine contractions in vivo and in vitro. Effective in a rat preterm labor model.
Technical Data
| M. Wt | 994.19 |
| Formula | C43H67N11O12S2 |
| Sequence |
XYITNCPXG (Modifications: X-1 = Mpr, X-8 = Orn, Tyr-2 = D-Tyr(OEt), Gly-9 = C-terminal amide, Cyclized = X-1 - Cys-6) |
| Storage | Store at -20°C |
| CAS Number | 90779-69-4 |
| PubChem ID | 5311010 |
| InChI Key | VWXRQYYUEIYXCZ-OBIMUBPZSA-N |
| Smiles | [H][C@@]1([C@H](O)C)NC(C([C@H](CC)C)NC([C@H](NC(CCSSC[C@@H](C(N2CCC[C@H]2C(N[C@H](C(NCC(N)=O)=O)CCCN)=O)=O)NC([C@@H](NC1=O)CC(N)=O)=O)=O)CC3=CC=C(C=C3)OCC)=O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solubility | Soluble to 100 mg/ml in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 994.19. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.01 mL | 5.03 mL | 10.06 mL |
| 5 mM | 0.2 mL | 1.01 mL | 2.01 mL |
| 10 mM | 0.1 mL | 0.5 mL | 1.01 mL |
| 50 mM | 0.02 mL | 0.1 mL | 0.2 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Kim et al (2016) The oxytocin receptor antagonist, Atosiban, activates pro-inflammatory pathways in human amnion via Gαi signalling. Mol.Cell.Endocrinol. 420 11 PMID: 26586210
Kim et al (2017) Differential effects of oxytocin receptor antagonists, Atosiban and Nolasiban, on oxytocin receptor-mediated signaling in human amnion and myometrium. Mol.Pharmacol. 91 403 PMID: 28188254
Hahn et al (1987) Evaluation of 1-deamino-[D-Tyr(Oethyl)2, Thr4, Orn8] vasotocin, an oxytocin antagonist, in animal models of uterine contractility and preterm labor: a new tocolytic agent. Am.J.Obstet.Gynecol. 157 977 PMID: 3674173
Maggi et al (1994) Antagonists for the human oxytocin receptor: an in vitro study. J.Reprod.Fertil. 101 345 PMID: 7932368
Keywords: Atosiban, supplier, oxytoxin, receptor, antagonists, antagonism, tocolytics, preterm, labor, labour, OTR, Oxytocin, Receptors, Oxytocin, Receptors, Tocris Bioscience
