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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 for OPC 21268
OPC 21268 is a 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 for OPC 21268
OPC 21268 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for OPC 21268
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for OPC 21268
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 44.95 | 100 | |
| ethanol | 11.24 | 25 |
Preparing Stock Solutions for OPC 21268
The following data is based on the product molecular weight 449.54. 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 |
|---|---|---|---|
| 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 for OPC 21268
References for OPC 21268
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for OPC 21268, please let us know.
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Keywords: OPC 21268, OPC 21268 supplier, OPC21268, vasopressin, v1, v1r, avp, arginine, Vasopressin, Receptors, 3924, Tocris Bioscience
3 Citations for OPC 21268
Citations are publications that use Tocris products. Selected citations for OPC 21268 include:
Amita et al (2018) Asymmetric vasopressin signaling spatially organizes the master circadian clock. J Comp Neurol 526 2048-2067 PMID: 29931690
Gallia et al (2022) Evidence for a Prehypertensive Water Dysregulation Affecting the Development of Hypertension: Results of Very Early Treatment of Vasopressin V1 and V2 Antagonism in Spontaneously Hypertensive Rats. Front Cardiovasc Med 9 897244 PMID: 35722114
Harshida et al (2020) Reduced VIP Expression Affects Circadian Clock Function in VIP-IRES-CRE Mice (JAX 010908). J Biol Rhythms 35 340-352 PMID: 32460660
Do you know of a great paper that uses OPC 21268 from Tocris? Please let us know.
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Literature in this Area
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Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.