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Submit ReviewConivaptan hydrochloride
Description: Very high affinity vasopressin V1A and V2 antagonist; orally bioavailable
Chemical Name: N-[4-[(4,5-Dihydro-2-methylimidazo[4,5-d][benzazepin-6(1H)-yl)carbonyl]phenyl-[1,1'-biphenyl]-2-carboxamide hydrochloride
Purity: ≥98% (HPLC)
Biological Activity for Conivaptan hydrochloride
Conivaptan hydrochloride is a very high affinity vasopressin V1A and V2 antagonist (Ki values are 0.61 and 0.66 - 3.04 nM, respectively). Inhibits vasopressin-induced pressor responses in rats without altering blood pressure, and increases urine flow while decreasing urine osmolality. Orally bioavailable.
Compound Libraries for Conivaptan hydrochloride
Conivaptan hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for Conivaptan hydrochloride
| M. Wt | 535.04 |
| Formula | C32H26N4O2.HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 168626-94-6 |
| PubChem ID | 151171 |
| InChI Key | IKENVDNFQMCRTR-UHFFFAOYSA-N |
| Smiles | CC1=NC2=C(C3=CC=CC=C3N(C(C4=CC=C(C=C4)NC(C5=C(C6=CC=CC=C6)C=CC=C5)=O)=O)CC2)N1 |
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 Conivaptan hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 53.5 | 100 | |
| ethanol | 10.7 | 20 with gentle warming |
Preparing Stock Solutions for Conivaptan hydrochloride
The following data is based on the product molecular weight 535.04. 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 | 1.87 mL | 9.35 mL | 18.69 mL |
| 5 mM | 0.37 mL | 1.87 mL | 3.74 mL |
| 10 mM | 0.19 mL | 0.93 mL | 1.87 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.37 mL |
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Product Datasheets for Conivaptan hydrochloride
References for Conivaptan hydrochloride
References are publications that support the biological activity of the product.
Tahara et al (1997) Pharmacological profile of YM087, a novel potent nonpeptide vasopressin V1A and V2 receptor antagonist, in vitro and in vivo. J.Pharmacol.Exp.Ther. 282 301 PMID: 9223568
Yatsu et al (1997) Pharmacological profile of YM087, a novel nonpeptide dual vasopressin V1A and V2 receptor antagonist, in dogs. Eur.J.Pharmacol. 321 225 PMID: 9063692
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Citations for Conivaptan hydrochloride
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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.