Thiorphan-d7

Names

[ CAS No. ]:
1276297-68-7

[ Name ]:
Thiorphan-d7

[Synonym ]:
N-[3-(2H5)Phenyl-2-(sulfanylmethyl)(3,3-2H2)propanoyl]glycine
Glycine, N-[2-(mercaptomethyl)-1-oxo-3-(phenyl-d5)propyl-3,3-d2]-

Biological Activity

[Description]:

Thiorphan-d7 is the deuterium labeled Thiorphan[1]. Thiorphan is a selective NEP (neprilysin) inhibitor with an IC50 of 6.9 nM[2].

[Related Catalog]:

Research Areas >> Neurological Disease
Signaling Pathways >> Metabolic Enzyme/Protease >> Neprilysin

[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]. Whyteside AR, Turner AJ. Human neprilysin-2 (NEP2) and NEP display distinct subcellular localisations and substrate preferences. FEBS Lett. 2008 Jul 9;582(16):2382-6.  

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
524.0±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C12H8D7NO3S

[ Molecular Weight ]:
260.361

[ Flash Point ]:
270.7±30.1 °C

[ Exact Mass ]:
260.121216

[ LogP ]:
1.37

[ Vapour Pressure ]:
0.0±1.4 mmHg at 25°C

[ Index of Refraction ]:
1.577

Related Compounds