Atosiban

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Cat.No. 6332 - Atosiban | Mpr-D-Tyr(OEt)-Ile-Thr-Asn-Cys-Pro-Orn-Gly-NH2 | CAS No. 90779-69-4
Description: Potent oxytocin receptor antagonist
Datasheet
Citations
Reviews
Literature

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

References

References are publications that support the biological activity of the product.

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


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