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 |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
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
Keywords: L-371,257, supplier, Potent, selective, oxytocin, receptors, antagonists, OT, Receptors, L371257, Oxytocin, Receptors, Oxytocin, Receptors, Tocris Bioscience
