Rolipram, 5 mg

STEMCELL Technologies supplies this cell-permeable small molecule as a selective inhibitor of Type 4 cyclic nucleotide phosphodiesterases (PDE4), the enzymes that mediate cyclic AMP (cAMP) degradation. It is described as a cAMP pathway activator.

The compound preferentially inhibits the PDE4A isoform with an IC₅₀ of 3 nM, compared with IC₅₀ values of 130 nM and 240 nM for isoforms B and D, respectively. It also inhibits interferon (IFN)-γ-stimulated phosphorylation of p38 mitogen-activated protein (MAP) kinase through PDE4B and/or PDE4D isoform inhibition. Its chemical name is 4-[3-(cyclopentyloxy)-4-methoxyphenyl]-2-pyrrolidinone, with alternative names SB 95952 and ZK 62711. The molecular formula is C₁₆H₂₁NO₃, the molecular weight is 275.3 g/mol, the CAS number is 61413-54-5, and the reported purity is ≥98%. It is supplied as a crystalline solid.

Published applications include inducing reprogramming of adult human dermal fibroblasts into induced neuronal stem cells; enhancing osteoblastic differentiation of mouse mesenchymal stem cells induced by BMP-2; inducing neural differentiation of human bone marrow-derived mesenchymal stem cells; suppressing inflammation by inhibiting leukotriene C4 synthesis in human eosinophils and lipopolysaccharide-induced tumor necrosis factor synthesis in human monocytes; promoting survival of newly formed mouse hippocampal neurons in a mouse model of ischemia; and reversing amphetamine-induced reductions in auditory-evoked potentials in a C57BL/6J mouse model of schizophrenia. The safety data sheet classifies the substance as acutely toxic if swallowed and as causing skin and serious eye irritation, with possible respiratory irritation, and recommends appropriate personal protective equipment. The product is stable at -20 °C as supplied and should be protected from prolonged exposure to light.