Nisoldipine-d₃  (Synonyms: BAY-k 5552-d₃)

Nisoldipine-d₃ is deuterated labeled Nisoldipine (HY-17402). Nisoldipine (BAY-k 5552; Sular) is a highly efficient and specific L-type Cav1.2 channel blocker with an IC50 of 10 nM.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

391.43

C₂₀H₂₁D₃N₂O₆

63675-72-9

O=C(C1=C(C)NC(C)=C(C(OCC(C)C)=O)C1C2=CC=CC=C2[N+]([O-])=O)OC([2H])([2H])[2H]

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

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

  [2]. Hamilton SF, Houle LM, Thadani U. Rapid-release and coat-core formulations of nisoldipine in treatment of hypertension, angina, and heart failure. Heart Dis. 1999 Nov-Dec;1(5):279-88.  [Content Brief]

  [3]. Fodor JG. Nisoldipine CC: efficacy and tolerability in hypertension and ischemic heart disease. Cardiovasc Drugs Ther. 1997 Jan;10 Suppl 3:873-9.  [Content Brief]

  [4]. D.J. Duncker, J.M. Hartog, P.G. Hugenholtz, et al. The effects of nisoldipine (Bay K 5552) on cardiovascular performance and regional blood flow in pentobarbital - anaesthetized pigs with or without β-adrenoceptor blockade. British Journal of Pharmacology. 1986,88(1): 9-18

  [5]. Jan W. De Jong, Tom Huizer, Jan G.P. Tijssen. Energy conservation by nisoldipine in ischaemic heart. British Journal of Pharmacology. 1984, 83(4): 943-949