Sparsentan-d5

Names

[ CAS No. ]:
1801597-09-0

[ Name ]:
Sparsentan-d5

Biological Activity

[Description]:

Sparsentan-d5 is deuterium labeled Sparsentan. Sparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively[1].

[Related Catalog]:

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

[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]. Murugesan N, et al. Dual angiotensin II and endothelin A receptor antagonists: synthesis of 2'-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and pharmacokinetics. J Med Chem. 2005 Jan 13;48(1):171-9.

Chemical & Physical Properties

[ Molecular Formula ]:
C32H35D5N4O5S

[ Molecular Weight ]:
597.78

Related Compounds