Rolipram
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 275.34 |
| Cas No. | 61413-54-5 |
| Formula | C16H21NO3 |
| Solubility | insoluble in H2O; ≥13 mg/mL in DMSO; ≥24.65 mg/mL in EtOH with ultrasonic |
| Chemical Name | 4-(3-cyclopentyloxy-4-methoxyphenyl)pyrrolidin-2-one |
| SDF | Download SDF |
| Canonical SMILES | COC1=C(C=C(C=C1)C2CC(=O)NC2)OC3CCCC3 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Kinase experiment [1]: | |
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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]: | |
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Cell lines |
U937 cells |
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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. |
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Reacting condition |
0 ~ 10000 nM; 20 mins |
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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]: | |
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Animal models |
SD rats |
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Dosage form |
300 μg/100 g; i.v. |
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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. |
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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. |
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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. |
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Quality Control & MSDS
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Chemical structure
