Sildenafil citrate-d8

Names

[ CAS No. ]:
1215071-03-6

[ Name ]:
Sildenafil citrate-d8

Biological Activity

[Description]:

Sildenafil (citrate)-d8 is the deuterium labeled Sildenafil citrate[1]. Sildenafil citrate is a potent phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 5.22 nM.

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis
Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE)
Signaling Pathways >> Autophagy >> Autophagy
Signaling Pathways >> Anti-infection >> Bacterial

[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 Feb;53(2):211-216.  

[2]. Wang Z, et al. The Selectivity and Potency of the New PDE5 Inhibitor TPN729MA. J Sex Med. 2013 Nov;10(11):2790-7.  

[3]. Li BB, et al. Sildenafil potentiates the proliferative effect of porcine pulmonary artery smooth muscle cells induced by serotonin in vitro. Chin Med J (Engl). 2011 Sep124(17):2733-40.  

[4]. Moretti R, et al. Sildenafil, a cyclic GMP phosphodiesterase inhibitor, induces microglial modulation after focal ischemia in the neonatal mouse brain. J Neuroinflammation. 2016 Apr 2813(1):95.  

[5]. Korkmaz MF, et al. The Effect of Sildenafil on Recuperation from Sciatic Nerve Injury in Rats. Balkan Med J. 2016 Mar33(2):204-11.  

Chemical & Physical Properties

[ Molecular Formula ]:
C28H30D8N6O11S

[ Molecular Weight ]:
674.75

Related Compounds