Roflumilast-d4 N-Oxide

• UNSPSC Description:

  Roflumilast-d4 N-Oxide 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].

• Target Antigen:

  Phosphodiesterase (PDE); RSV

• Type:

  Isotope-Labeled Compounds

• Related Pathways:

  Anti-infection;Metabolic Enzyme/Protease

• Field of Research:

  Inflammation/Immunology

• Solubility:

  10 mM in DMSO

• Smiles:

  [2H]C1([2H])C([2H])([2H])C1COC2=C(C=CC(C(NC3=C(Cl)C=[N+]([O-])C=C3Cl)=O)=C2)OC(F)F

• Molecular Weight:

  423.23

• References & Citations:

  [1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. |[2]Ding H, et al. Treatment of obesity-associated overactive bladder by the phosphodiesterase type-4 inhibitor roflumilast. Int Urol Nephrol. 2017 Jul 29.|[3]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.|[4]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.|[5]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.|[6]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.

• Shipping Conditions:

  Room Temperature

• Clinical Information:

  No Development Reported

• CAS Number:

  1794760-31-8