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Rolipram

In stock
Catalog No.
A4328
PDE4-inhibitor and an anti-inflammatory agent
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$55.00
In stock
10mg
$50.00
In stock
50mg
$65.00
In stock

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Email: [email protected]

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Background

Rolipram is a PDE4-inhibitor and an anti-inflammatory agent.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt275.34
Cas No.61413-54-5
FormulaC16H21NO3
Solubility≥13 mg/mL in DMSO, ≥24.65 mg/mL in EtOH with ultrasonic, <2.19 mg/mL in H2O
Chemical Name4-(3-cyclopentyloxy-4-methoxyphenyl)pyrrolidin-2-one
SDFDownload SDF
Canonical SMILESCOC1=C(C=C(C=C1)C2CC(=O)NC2)OC3CCCC3
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Protocol

Kinase experiment [1]:

Phosphodiesterase (PDE) assays

Determination of the total PDE3 and PDE4 activities was done using 1 μM cAMP as substrate and 10 μM of either the PDE3 selective inhibitor, Cilostimide, or the PDE4 selective inhibitor, Rolipram.

Cell experiment [1]:

Cell lines

U937 cells

Preparation method

The solubility of this compound in DMSO is > 13 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

0 ~ 10000 nM; 20 mins

Applications

In U937 cells, Rolipram increased protein kinase A (PKA)-mediated cAMP-response-element-binding protein (CREB) phosphorylation in a dose-dependent manner. In contrast, Rolipram dose-dependently inhibited p38 MAP kinase phosphorylation induced by interferon-γ, with an IC50 value of 294 ± 99 nM.

Animal experiment [2]:

Animal models

SD rats

Dosage form

300 μg/100 g; i.v.

Applications

In SD rats, Rolipram significantly reduced mean arterial pressure. In SD rats treated with lipopolysaccharide and Rolipram, cardiac index significantly increased only at 3 hrs. In addition, Rolipram significantly decreased sinusoidal volumetric flow and increased sinusoidal diameter, which indicated protective effects of Rolipram on sinusoidal microhemodynamics in endotoxemia.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. MacKenzie SJ, Houslay MD. Action of rolipram on specific PDE4 cAMP phosphodiesterase isoforms and on the phosphorylation of cAMP-response-element-binding protein (CREB) and p38 mitogen-activated protein (MAP) kinase in U937 monocytic cells. Biochem J. 2000 Apr 15;347(Pt 2):571-8.

[2]. Wollborn J, Wunder C, Stix J, Neuhaus W, Bruno RR, Baar W, Flemming S, Roewer N, Schlegel N, Schick MA. Phosphodiesterase-4 inhibition with rolipram attenuates hepatocellular injury in hyperinflammation in vivo and in vitro without influencing inflammation and HO-1 expression. J Pharmacol Pharmacother. 2015 Jan-Mar;6(1):13-23.

Quality Control

Chemical structure

Rolipram