L-371,257

Key Product Details

Product Description

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.

Product Specifications for L-371,257

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 24 publications citing the usage of this 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

Product Documents for L-371,257