Biological Activity
Roflupram is a selective, orally active and brain-penetrant PDE4 inhibitor, with an IC50 of 26.2 nM for core catalytic domains of human PDE4. Roflupram can reverse cognitive deficits and reduce the production of pro-inflammatory factors[1][2].
References
[1]. Li D, et, al. Roflupram, a novel phosphodiesterase 4 inhibitor, inhibits lipopolysaccharide-induced neuroinflammatory responses through activation of the AMPK/Sirt1 pathway. Int Immunopharmacol. 2021 Jan;90:107176.
[2]. You T, et, al. Roflupram, a Phosphodiesterase 4 Inhibitior, Suppresses Inflammasome Activation through Autophagy in Microglial Cells. ACS Chem Neurosci. 2017 Nov 15;8(11):2381-2392.