L-371,257

Name: L-371,257
Brand: Tocris Bioscience
SKU: 2410

Tocris Bioscience, part of Bio-Techne | Catalog # 2410

Citations (19)

COA / SDS

Potent and selective oxytocin receptor antagonist

Key Product Details

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)
Molecular Weight:	507.59

View Full Technical Details for L-371,257

Technical Data
Citations

Biological Activity for L-371,257

L-371,257 is a potent, high affinity human oxytocin (OT) receptor antagonist (K_i = 4.6 nM) that displays > 800-fold selectivity over human arginine vasopressin receptors V_1a 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 for L-371,257

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for L-371,257

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	2.54	5 with gentle warming with sonication

Preparing Stock Solutions for L-371,257

The following data is based on the product molecular weight 507.59.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.05 mM	39.40 mL	197.01 mL	394.02 mL
0.25 mM	7.88 mL	39.40 mL	78.80 mL
0.5 mM	3.94 mL	19.70 mL	39.40 mL
2.5 mM	0.79 mL	3.94 mL	7.88 mL

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References for L-371,257

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

Tahara Comparison of vasopressin binding sites in human uterine and vascular smooth muscle cells. Eur.J.Pharmacol. 1999 PMID: 10478574
Tahara Pharmacologic characterization of the oxyt. receptor in human uterine smooth muscle cells. Br.J.Pharmacol. 2000 PMID: 10694212
Williams 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 oxyt. antagonist. J.Med.Chem. 1995 PMID: 7473590