Description: Orally active vasopressin V1 antagonist
Chemical Name:N-[3-[4-[[4-(3,4-Dihydro-2-oxo-1(2H)quinolinyl)-1-piperidinyl]carbonyl]phenoxy]propyl]-acetamide
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
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.
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
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Yamamuraet al (1991) OPC-21268, an orally effective, nonpeptide vasopressin V1 receptor antagonist. Science 252 572 PMID: 1850553
Imaizumiet al (1992) Effects of OPC-21268, an orally effective vasopressin V1 receptor antagonist in humans. Hypertension 20 54 PMID: 1319959
Thibonnieret 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