Tolvaptan-d7

• CAT Number: S000539
• CAS Number: 1246818-18-7
• Molecular Formula: C26H18D7ClN2O3
• Molecular Weight: 455.98
• Purity: ≥95%

Tolvaptan-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].
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].

Reference

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

[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.
 [Content Brief]

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

[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.
 [Content Brief]

[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.