生物活性：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].
IC50 & Target：V2 Receptor
体外研究(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].
QY千亿国际 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量：455.98
Formula：C26H18D7ClN2O3
CAS 号：1246818-18-7
非标记 CAS：150683-30-0
中文名称：托伐普坦 d7
运输条件：Room temperature in continental US; may vary elsewhere.
储存方式：Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
Data Sheet (536 KB)
产品使用指南 (1538 KB)
参考文献
[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.