Tolvaptan-d7

Modify Date: 2024-01-16 08:39:19

Tolvaptan-d7 Structure
Tolvaptan-d7 structure
Common Name Tolvaptan-d7
CAS Number 1246818-18-7 Molecular Weight 455.984
Density 1.3±0.1 g/cm3 Boiling Point 594.4±50.0 °C at 760 mmHg
Molecular Formula C26H18D7ClN2O3 Melting Point N/A
MSDS N/A Flash Point 313.3±30.1 °C

 Use of Tolvaptan-d7


Tolvaptan-D7 (OPC-41061-D7) is the deuterium labeled Tolvaptan. Tolvaptan is a selective, competitive arginine vasopressin receptor 2 antagonist with an IC50 of 1.28μM for the inhibition of AVP-induced platelet aggregation[1][2].

 Names

Name Tolvaptan-d7
Synonym More Synonyms

 Tolvaptan-d7 Biological Activity

Description Tolvaptan-D7 (OPC-41061-D7) is the deuterium labeled Tolvaptan. Tolvaptan is a selective, competitive arginine vasopressin receptor 2 antagonist with an IC50 of 1.28μM for the inhibition of AVP-induced platelet aggregation[1][2].
Related Catalog
In Vitro Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
References

[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

[2]. Friedman B, Cirulli J.Hyponatremia in critical care patients: Frequency, outcome, characteristics, and treatment with the vasopressin V(2)-receptor antagonist tolvaptan.J Crit Care. 2012 Aug 8.

[3]. Inomata T.Tolvaptan (vasopressin receptor antagonist).Nihon Rinsho. 2011 Nov;69 Suppl 9:408-11.

[4]. Vaduganathan M, Gheorghiade M, Pang PS, Konstam MA, Zannad F, Swedberg K, Grinfeld L, Burnett JC Jr, Krasa HB, Zimmer C, Blair J, Ouyang J, Maggioni AP; EVEREST investigators.Efficacy of oral tolvaptan in acute heart failure patients with hypotension and renal impairment.J Cardiovasc Med (Hagerstown). 2012 Jul;13(7):415-22.

[5]. Y Yamamura et al. OPC-41061, a Highly Potent Human Vasopressin V2-Receptor Antagonist: Pharmacological Profile and Aquaretic Effect by Single and Multiple Oral Dosing in Rats. J. Pharmacol. Exp. Ther. 1998, 287(3), 860-867.

[6]. RW Schrier et al. Tolvaptan, a Selective Oral Vasopressin V2-Receptor Antagonist, for Hyponatremia. N Engl J Med 2006, 355, 2099-2112.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 594.4±50.0 °C at 760 mmHg
Molecular Formula C26H18D7ClN2O3
Molecular Weight 455.984
Flash Point 313.3±30.1 °C
Exact Mass 455.199310
LogP 4.09
Vapour Pressure 0.0±1.8 mmHg at 25°C
Index of Refraction 1.664

 Synonyms

Tolvaptan-d7
N-{4-[(7-Chloro-5-hydroxy-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl)carbonyl]-3-methylphenyl}-2-(2H3)methyl(2H4)benzamide
Benzamide-2,3,4,5-d4, N-[4-[(7-chloro-2,3,4,5-tetrahydro-5-hydroxy-1H-1-benzazepin-1-yl)carbonyl]-3-methylphenyl]-6-(methyl-d3)-