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ent-Tadalafil-d3

Names

[ CAS No. ]:
1329568-92-4

[ Name ]:
ent-Tadalafil-d3

Biological Activity

[Description]:

ent-Tadalafil-d3 (ent-IC-351-d3) is the deuterium labeled ent-Tadalafil. ent-Tadalafil (ent-IC-351), compound (6S,12aS), is a inactive cis-enantiomer of compound (6R,12aS). compound (6R,12aS) is a potent PDE5 inhibitor with an IC50 of 0.090 μM, while ent-Tadalafil is inactive at concentrations up to 10 µM[1][2].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE)

[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]. Daugan A, et al. The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione analogues.J Med Chem. 2003 Oct 9;46(21):4533-42.

Chemical & Physical Properties

[ Melting Point ]:
271-273 °C

[ Molecular Formula ]:
C22H16D3N3O4

[ Molecular Weight ]:
392.42

Safety Information

[ Hazard Codes ]:
Xi

Related Compounds