Biological Activity
Nonpeptide vasopressin V1 receptor antagonist. Displays greater affinity for rat V1 than human V1 (Ki values are 25 and 8800 nM respectively). Exhibits 1000-fold selectivity for V1 receptors over V2 receptors. Orally active.
Compound Libraries
OPC 21268 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 449.54 |
| Formula | C26H31N3O4 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 131631-89-5 |
| PubChem ID | 114904 |
| InChI Key | KSNUCNRMDYJBKT-UHFFFAOYSA-N |
| Smiles | O=C2N(C3CCN(C(C4=CC=C(OCCCNC(C)=O)C=C4)=O)CC3)C1=CC=CC=C1CC2 |
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 | 44.95 | 100 | |
| ethanol | 11.24 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 449.54. 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 | 2.22 mL | 11.12 mL | 22.24 mL |
| 5 mM | 0.44 mL | 2.22 mL | 4.45 mL |
| 10 mM | 0.22 mL | 1.11 mL | 2.22 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Yamamura et al (1991) OPC-21268, an orally effective, nonpeptide vasopressin V1 receptor antagonist. Science 252 572 PMID: 1850553
Imaizumi et al (1992) Effects of OPC-21268, an orally effective vasopressin V1 receptor antagonist in humans. Hypertension 20 54 PMID: 1319959
Thibonnier et al (2000) A molecular model of agonist and nonpeptide antagonist binding to the human V1 vascular vasopressin receptor. J.Pharmacol.Exp.Ther. 294 195 PMID: 10871312
Keywords: OPC 21268, supplier, OPC21268, vasopressin, v1, v1r, avp, arginine, Vasopressin, Receptors, Vasopressin, Receptors, Tocris Bioscience
