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57192
Rolipram
Activators & Inhibitors
Chemical Modulators

Rolipram #57192

Citations (0)
Chemical structure of Rolipram.

Product Usage Information

Rolipram is supplied as a lyophilized powder. For a 10 mM stock, reconstitute 1 mg of powder in 0.36 mL of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.

Storage

Store lyophilized at room temperature, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Product Description

Molecular Weight 275.3 g/mol
Purity >98%
Molecular Formula C16H21NO3
CAS 61413-54-5
Solubility Soluble in DMSO at 25 mg/mL or ethanol at 25 mg/mL.

Background

The small-molecule Rolipram is an inhibitor of phosphodiesterase 4 (PDE4), which catalyzes the hydrolysis of cyclic-AMP (cAMP) to regulate cellular responses to a number of extracellular signals. Rolipram inhibits multiple isozymes of PDE4, including PDE4A (IC50 = 3 nM), PDE4B (IC50 = 130 nM), and PDE4D (IC50 = 240 nM). Treatment of myeloid cells with Rolipram resulted in phosphorylation of cAMP-response element-binding protein (CREB) and implied the presence of both high (PDE4A4) and low affinity (PDE4B, PDE4D) components (1). Rolipram and other phosphodiesterase inhibitors were seen as having potential therapeutic benefits in preclinical models of psychiatric and neurologic diseases. Unfortunately, severe dose-limiting side effects (e.g., nausea, vomiting) limited the clinical application of PDE inhibitors (2). Still, Rolipram treatment in a mouse model of intracerebral hemorrhage demonstrated some neuroprotective benefits through activation of the cAMP/AMPK/SIRT1 pathway (3). Rolipram treatment of fibroblasts from ligamentum flavum hypertrophy patients inhibited PDE4A and PDE4B activity, blocked TGF-β1 by restoring p-ERK1/2 expression, and inhibited expression of fibrosis-related proteins (4).

Limited Uses

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For Research Use Only. Not for Use in Diagnostic Procedures.
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To Purchase # 57192
Cat. # Size Qty. Price
57192S
10 mg