L-371,257

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Cat.No. 2410 - L-371,257 | C28H33N3O6 | CAS No. 162042-44-6
Description: Potent and selective oxytocin receptor antagonist
Chemical Name: 1-[4-[(1-Acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]-4-(2-oxo-2H-3,1-benzoxazin-1(4H)-yl)piperidine
Purity: ≥99% (HPLC)
Datasheet
Citations (2)
Reviews
Literature

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
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 162042-44-6
PubChem ID 6918320
InChI Key WDERJSQJYIJOPD-UHFFFAOYSA-N
Smiles CC(N(CC3)CCC3OC(C=C2)=CC(OC)=C2C(N1CCC(N4C(OCC5=C4C=CC=C5)=O)CC1)=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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 5.08 10mM with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 507.59. 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 1.97 mL 9.85 mL 19.7 mL
5 mM 0.39 mL 1.97 mL 3.94 mL
10 mM 0.2 mL 0.99 mL 1.97 mL
50 mM 0.04 mL 0.2 mL 0.39 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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

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

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


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

2 Citations for L-371,257

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


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