Apremilast-d8 (CC-10004-d8) is a deuterated apremilast. Apremilast (CC-10004) is an orally available phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 74 nM. Apremilast inhibits TNF-α release from lipopolysaccharide (LPS) with an IC50 of 104 nM.

Physicochemical Properties

Molecular Formula	C22H16D8N2O7S
Molecular Weight	468.55
CAS #	1258597-45-3
SMILES	[C@@H](C1C=CC(OC([H])([H])[H])=C(OC([H])([H])C([H])([H])[H])C=1)(N1C(C2=CC=CC(NC(=O)C)=C2C1=O)=O)CS(=O)(=O)C
Synonyms	Apremilast-d8; CC-10004-d8
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

References

[1]. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [2]. Apremilast, a novel phosphodiesterase 4 (PDE4) inhibitor, regulates inflammation through multiple cAMP downstream effectors. Arthritis Res Ther. 2015 Sep 15;17:249. [3]. 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.

Solubility Data

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.1342 mL	10.6712 mL	21.3424 mL
	5 mM	0.4268 mL	2.1342 mL	4.2685 mL
	10 mM	0.2134 mL	1.0671 mL	2.1342 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.