Roflumilast-d4

Roflumilast-d4 is the deuterium labeled Roflumilast. Roflumilast is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells[1][2].

Product Specifications

CAS Number

[1398065-69-4]

Product Name Alternative

APTA-2217-d4; BYK 20869-d4; B9302-107-d4

UNSPSC

12352005

Hazard Statement

H315, H319, H335

Target

Isotope-Labeled Compounds; Phosphodiesterase (PDE) ; RSV

Type

Isotope-Labeled Compounds

Related Pathways

Anti-infection; Metabolic Enzyme/Protease; Others

Applications

COVID-19-anti-virus

Field of Research

Inflammation/Immunology

Purity

97.26

Solubility

10 mM in DMSO

Smiles

FC(OC1=C(C=C(C=C1)C(NC2=C(C=NC=C2Cl)Cl)=O)OCC3C([2H])(C3([2H])[2H])[2H])F

Molecular Formula

C17H10D4Cl2F2N2O3

Molecular Weight

407.23

Precautions

H315, H319, H335

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]Hatzelmann A, et al. The preclinical pharmacology of roflumilast--a selective, oral phosphodiesterase 4 inhibitor in development for chronic obstructive pulmonary disease. Pulm Pharmacol Ther. 2010 Aug;23 (4) :235-56.|[3]Rabe KF. Update on roflumilast, a phosphodiesterase 4 inhibitor for the treatment of chronic obstructive pulmonary disease. Br J Pharmacol. 2011 May;163 (1) :53-67.|[4]Hatzelmann A, et al. Anti-inflammatory and immunomodulatory potential of the novel PDE4 inhibitor roflumilast in vitro. J Pharmacol Exp Ther. 2001 Apr;297 (1) :267-79.|[5]Richmond BW, et al. Airway bacteria drive a progressive COPD-like phenotype in mice with polymeric immunoglobulin receptor deficiency. Nat Commun. 2016 Apr 5;7:11240.|[6]Ding H, et al. Treatment of obesity-associated overactive bladder by the phosphodiesterase type-4 inhibitor roflumilast. Int Urol Nephrol. 2017 Jul 29.