Home Metabolism PDE inhibitor Rolipram For research use only.

Rolipram

Synonyms: ZK-62711, SB 95952

The PDE4 selective inhibitor, Rolipram, inhibited immunopurified PDE4B and PDE4D activities similarly, with IC50 values of approx. 130 nM and 240 nM respectively; an anti-inflammatory agent.

Rolipram Chemical Structure

Rolipram Chemical Structure

CAS No. 61413-54-5

Purity & Quality Control

Rolipram Related Products

Signaling Pathway

PDE Signaling Pathways

PDE Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 cells Function assay Inhibition of recombinant human PDE4A expressed in Sf9 cells, IC50=4 nM 11052785
human PBMC Function assay Inhibition of LPS-induced TNFalpha production in human PBMC, IC50=0.06 μM 19049349
COS7 cells Function assay Inhibition of PDE4B2 expressed in COS7 cells assessed as cAMP hydrolysis, IC50=0.105 μM 18222088
HEK293 cells Function assay Inhibition of PDE4 expressed in HEK293 cells coexpressing G-protein coupled receptor and cyclic nucleotide gated ion channel by fluorescence assay, EC50=0.1315 μM 19464886
rat UMR106 cells Function assay Inhibition of PDE in rat UMR106 cells co-expressing CRE-luc assessed as PTH-induced cAMP accumulation by luciferase reporter gene assay, IC50=0.6 μM 22030030
human U937 cells Function assay Inhibition of PDE4 in human U937 cells assessed as accumulation of [3H]adenosine by scintillation counting, IC50=0.86 μM 19303290
Click to View More Cell Line Experimental Data

Biological Activity

Description The PDE4 selective inhibitor, Rolipram, inhibited immunopurified PDE4B and PDE4D activities similarly, with IC50 values of approx. 130 nM and 240 nM respectively; an anti-inflammatory agent.
Targets
PDE4B [1]
(Cell-free assay)		 PDE4D [1]
(Cell-free assay)
130 nM 240 nM
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01215552 Terminated
Healthy Elderly Volunteers
Dart NeuroScience LLC
 September 2010 Phase 1

Chemical Information & Solubility

Molecular Weight 275.34 Formula

C16H21NO3
CAS No. 61413-54-5 SDF Download Rolipram SDF
Smiles COC1=C(C=C(C=C1)C2CC(=O)NC2)OC3CCCC3
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 55 mg/mL ( (199.75 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 55 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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