Roflumilast

• Description :

  Roflumilast (APTA-2217) is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDE4A4, PDE4B1, and PDE4B2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells.

• Product Name Alternative :

  APTA-2217; BYK 20869; B9302-107

• UNSPSC :

  12352005

• Hazard Statement :

  H302, H315, H319, H335

• Target :

  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

• Purity :

  99.98

• 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 Formula :

  C17H14Cl2F2N2O3

• Molecular Weight :

  403.21

• Precautions :

  H302, H315, H319, H335

• References & Citations :

  [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.|[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.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Launched

• Isoform :

  PDE4

• CAS Number :

  [162401-32-3]