Apremilast-d8

Apremilast-d8 (CC-10004-d8) is deuterium labeled Apremilast. Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM[1][2].

Product Specifications

CAS Number

[1258597-45-3]

Product Name Alternative

CC-10004-d8

UNSPSC

12352005

Target

Apoptosis; Isotope-Labeled Compounds; Phosphodiesterase (PDE) ; TNF Receptor

Type

Isotope-Labeled Compounds

Related Pathways

Apoptosis; Metabolic Enzyme/Protease; Others

Field of Research

Inflammation/Immunology

Smiles

CS(C[C@H](C1=CC(OC([2H])([2H])C([2H])([2H])[2H])=C(C=C1)OC([2H])([2H])[2H])N2C(C3=C(NC(C)=O)C=CC=C3C2=O)=O)(=O)=O

Molecular Formula

C22H16D8N2O7S

Molecular Weight

468.55

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53 (2) :211-216.|[2]Perez-Aso M, et al. Apremilast, a novel phosphodiesterase 4 (PDE4) inhibitor, regulates inflammation through multiple cAMP downstream effectors. Arthritis Res Ther. 2015 Sep 15;17:249.|[3]Chen LG, et al. Determination of Apremilast in Rat Plasma by UPLC-MS-MS and Its Application to a Pharmacokinetic Study. J Chromatogr Sci. 2016 Sep;54 (8) :1336-40.