820957-38-8
Chemical Structure
Retosiban
Synonym(s): GSK 221149; GSK 221149A
- CAS No.: 820957-38-8
- Formula:C27H34N4O5
- Molecular Weight:494.58
IUPAC Name: (3R,6R)-6-((S)-sec-butyl)-3-(2,3-dihydro-1H-inden-2-yl)-1-((R)-1-(2-methyloxazol-4-yl)-2-morpholino-2-oxoethyl)piperazine-2,5-dione
InChIKey: PLVGDGRBPMVYPB-FDUHJNRSSA-N
SMILES: O=C([C@@H](C1CC2=C(C=CC=C2)C1)N3)N([C@H](C4=COC(C)=N4)C(N5CCOCC5)=O)[C@H]([C@H](CC)C)C3=O
Biological Activity: Retosiban (GSK221149A) is a potent, selective, and orally active oxytocin receptor antagonist (Ki (hOT) = 0.65 nM, Ki (rOT) = 4.1 nM) with no detectable agonist activity. Retosiban has nanomolar affinity for the oxytocin receptor with >1400-fold selectivity over the closely related vasopressin receptors. Retosiban inhibits spontaneous and induces uterine contractions. Retosiban can be studied in research for preterm labour[1][2][4].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Retosiban | 98.95% | Retosiban (GSK221149A) is a potent, selective, and orally active oxytocin receptor antagonist (Ki (hOT) = 0.65 nM, Ki (rOT) = 4.1 nM) with no detectable agonist activity. Retosiban has nanomolar affinity for the oxytocin receptor with >1400-fold selectivity over the closely related vasopressin receptors. Retosiban inhibits spontaneous and induces uterine contractions. Retosiban can be studied in research for preterm labour. | ||||||||||||||||||||
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- [1]. Liddle J, et al. The discovery of GSK221149A: a potent and selective oxytocin antagonist. Bioorg Med Chem Lett. 2008 Jan 1;18(1):90-4. [Content Brief]
- [2]. Thornton, S., et al., (2015). Treatment of spontaneous preterm labour with retosiban: a phase 2 proof-of-concept study. British journal of clinical pharmacology, 80(4), 740-749. [Content Brief]
- [4]. McCafferty, G. P., et al., (2007). Use of a novel and highly selective oxytocin receptor antagonist to characterize uterine contractions in the rat. American journal of physiology. Regulatory, integrative and comparative physiology, 293(1), R299–R305. [Content Brief]
Keywords
