Tezosentan-d4

Names

[ CAS No. ]:
1794707-10-0

[ Name ]:
Tezosentan-d4

Biological Activity

[Description]:

Tezosentan-d4 (RO 610612-d4) is the deuterium labeled Tezosentan. Tezosentan (RO 610612) is an endothelin (ET) receptor antagonist, with pA2s of 9.5, 7.7 for ETA and ETB receptors, respectively[1][2].

[Related Catalog]:

Research Areas >> Cancer
Research Areas >> Cardiovascular Disease
Research Areas >> Endocrinology
Signaling Pathways >> GPCR/G Protein >> Endothelin Receptor
Research Areas >> Neurological Disease

[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]. Clozel M, et al. Pharmacology of tezosentan, new endothelin receptor antagonist designed for parenteral use. J Pharmacol Exp Ther. 1999 Aug;290(2):840-6.

Chemical & Physical Properties

[ Molecular Formula ]:
C27H23D4N9O6S

[ Molecular Weight ]:
609.65

Related Compounds