Roflumilast
PDE4 inhibitor / Potent and selective phosphodiesterase (PDE4) inhibitor, IC50=0.7, 0.9, 0.7, 0.2 nM for PDE4A1, PDE4A4, PDE4B1 and PDE4B2 respectively1. Clinically useful agent for treatment of COPD2. Improves sensory gating in humans3 and improves memory in rodent models4. Mimics calorie restriction effects via activation of AMPK/SIRT1 and protects against diabetic nephropathy5. Reduces weight gain by increasing energy expenditure and improves glucose metabolism in mice6.
Biochemicals & reagents
162401-32-3
BYK-20869
1) Hatzelmann et al. (2010), The preclinical pharmacology of roflumilast—a selective, oral phosphodiesterase 4 inhibitor in development for chronic obstructive pulmonary disease; Pulm, Pharmacol. Ther., 23 235 2) Rabe et al. (2011), Update on roflumilast, a phosphodiesterase 4 inhibitor for the treatment of chronic obstructive pulmonary disease; Br. J. Pharmacol, 163 53 3) Heckman et al. (2018), Acute administration of roflumilast enhances sensory gating in healthy young humans in a randomized trial; Psychopharmacology (Berl.), 235 301 4) Vanmierlo et al. (2016), The PDE4 inhibitor roflumilast improves memory in rodents at non-emetic doses; Behav. Brain Res., 303 26 5) Tikoo et al. (2014), Calorie restriction mimicking effects of roflumilast prevents diabetic nephropathy; Biochem. Biophy. Res. Commun., 450 1581 6) Mollmann et al. (2017), The PDE4 inhibitor roflumilast reduced weight gain by increasing energy expenditure and leads to improved glucose metabolism; Diabetes Obes. Metab., 19 496
-20°C
TARGET: PDE (Phosphodiesterase) -- PATHWAY: Carbohydrate metabolism; AMPK pathway; Glycation; cAMP / cGMP signaling -- DISEASE AREA: Inflammation; DiabetesKidney disease