Roflumilast

• UNSPSC Description:

  Roflumilast (APTA-2217) 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.

• Target Antigen:

  Phosphodiesterase (PDE); RSV

• Type:

  Reference compound

• Related Pathways:

  Anti-infection;Metabolic Enzyme/Protease

• Applications:

  COVID-19-anti-virus

• Field of Research:

  Inflammation/Immunology

• Assay Protocol:

  https://www.medchemexpress.com/Roflumilast.html

• Solubility:

  DMSO : ≥ 50 mg/mL|H2O : < 0.1 mg/mL (ultrasonic)

• Smiles:

  O=C(NC1=C(Cl)C=NC=C1Cl)C2=CC=C(OC(F)F)C(OCC3CC3)=C2

• Molecular Weight:

  403.21

• References & Citations:

  [1]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.|[2]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.|[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]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.|[5]Ding H, et al. Treatment of obesity-associated overactive bladder by the phosphodiesterase type-4 inhibitor roflumilast. Int Urol Nephrol. 2017 Jul 29.

• Shipping Conditions:

  Room Temperature

• Clinical Information:

  Launched

• CAS Number:

  162401-32-3