L-371,257

Cat. No. 2410

L-371,257 C28H33N3O6 [162042-44-6]

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Chemical Name: 1-[4-[(1-Acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]-4-(2-oxo-2H-3,1-benzoxazin-1(4H)-yl)piperidine

Biological Activity

Potent, high affinity human oxytocin (OT) receptor antagonist (Ki = 4.6 nM) that displays > 800-fold selectivity over human arginine vasopressin receptors V1a and V2. Antagonizes oxytocin-induced contractions in isolated rat uterine tissue (pA2 = 8.44) and in anesthetised rats following intravenous and intraduodenal administration. Decreases length of U-87MG cell projections induced by retinoic acid (Cat.No.0695). Orally active.

Technical Data

M.Wt:
507.59
Formula:
C28H33N3O6
Solubility:
Soluble to 10 mM in DMSO with gentle warming
Purity:
>99 %
Storage:
Store at RT
CAS No:
162042-44-6

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Tahara et al (2000) Pharmacologic characterization of the oxytocin receptor in human uterine smooth muscle cells. Br.J.Pharmacol. 129 131. PMID: 10694212.

Tahara et al (1999) Comparison of vasopressin binding sites in human uterine and vascular smooth muscle cells. Eur.J.Pharmacol. 378 137. PMID: 10478574.

Williams et al (1995) 1-{1-[4-[N-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]piperidin-4-yl}-4H-3,1-benzoxazin-2(1H)-one (L-371,257): a new, orally bioavailable, non-peptide oxytocin antagonist. J.Med.Chem. 38 4634. PMID: 7473590.

If you know of a relevant reference for L-371,257 please let us know.

Citations are publications that use Tocris products. Selected citations for L-371,257 include:

Lestanova et al (2017) Downregulation of oxytocin receptor decreases the length of projections stimulated by retinoic acid in the U-87MG cells. Neurochem.Res. 42 1006. PMID: 27995495.

Ataka et al (2012) Alteration of antral and proximal colonic motility induced by chronic psychological stress involves central urocortin 3 and vasopressin in rats. Am J Physiol Gastrointest Liver Physiol 303 G519. PMID: 22651925.

Do you know of a great paper that uses L-371,257 from Tocris? If so please let us know.

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Keywords: L-371,257, supplier, Potent, selective, oxytocin, receptors, antagonists, OT, Receptors, L371257, Tocris Bioscience, Oxytocin Receptor Antagonist products

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