Hydroxy Bosentan-d6

Names

[ CAS No. ]:
1246817-57-1

[ Name ]:
Hydroxy Bosentan-d6

[Synonym ]:
Ro 48-8634-d6
4-[2-Hydroxy-1,1-(dimethyl-d6)ethyl]-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)[2,2'-bipyrimidin]-4-yl]-benzenesulfonamide
Ro 48-5033-d6
Hydroxy Bosentan-d6

Biological Activity

[Description]:

Hydroxy Bosentan-d6 is deuterium labeled Hydroxy bosentan. Hydroxy bosentan (Ro 48-5033) is a primary metabolite of Bosentan (BOS) metabolized by the cytochrome P450 system in the liver. Ro 48-5033 assists BOS pharmacologically, retaining 10%-20% activities[1].

[Related Catalog]:

Research Areas >> Cardiovascular 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]. Chen M, et al. Comparison of the inhibitory effect of ketoconazole, voriconazole, fluconazole, and itraconazoleon the pharmacokinetics of bosentan and its corresponding active metabolite hydroxy bosentanin rats. Xenobiotica. 2019 Jul 3:1-8.

Chemical & Physical Properties

[ Molecular Formula ]:
C27H23D6N5O7S

[ Molecular Weight ]:
573.65

[ Exact Mass ]:
573.21600

[ PSA ]:
174.26000

[ LogP ]:
4.33010

Related Compounds