Size | Price | Stock | Qty |
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10mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
Rolipram (formerly called ME-3167; ZK-62711; SB95952; the racemic mixture of R- and S-rolipram) is a novel, potent and selective phosphodiesterase PDE4 inhibitor with potential anti-inflammatory and anti-depressant activity. It inhibits PDE4A/4B/4D with IC50s of 3 nM, 130 nM and 240 nM, respectively.
ln Vitro |
The activity of immunopurified PDE4B and PDE4D was also inhibited by the PDE4-selective inhibitor Rolipram, with IC50 values of 130 nM and 240 nM, respectively. Conversely, immunopurified PDE4A's activity was inhibited by Rolipram, albeit at a much lower IC50 of about 3 nM. Rolipram increases cAMP response element binding protein (CREB) phosphorylation in U937 cells in a dose-dependent manner, suggesting the presence of components with high and low affinity (IC50 ~1 nM and IC50 ~120 nM, respectively). With a 290 nM IC50, rolipram dose-dependently and simply and monotonically inhibits the phosphorylation of p38 MAPK when stimulated by IFN-γ [1]. All four PDE4 isoforms are inhibited by the selective PDE4 inhibitor rolipram. Rolipram inhibits the production of TNF induced by LPS in a maximal/submaximal manner and in a dose-dependent manner (IC50 of 25.9 nM). At a dosage of 2 μM, inhibitory effects were noted in J774 cells [2].
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ln Vivo |
Rolipram appears to have decreased the TNF mRNA and protein expression that LPS produced in WT mice's peritoneal macrophages (PM) (74% and 63% suppression of TNF mRNA and TNF protein, respectively). In line with previous findings, LPS-induced TNF production was higher in MKP-1 (-/-) mice's PM than in WT mice's PM. It's interesting to note that Rolipram's suppression of TNF mRNA and protein expression was much reduced and did not reach statistical significance in the PM of MKP-1 (-/-) mice [2]. In trained helpless rats, repeated intraperitoneal injections of Rolipram (1.25 mg/kg) can decrease the number of unsuccessful escape attempts [3].
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Animal Protocol |
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References |
[1]. MacKenzie SJ, et al. 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 monocyticcells. Biochem J. 2000 Apr
[2]. Korhonen R, et al. Attenuation of TNF production and experimentally induced inflammation by PDE4 inhibitor rolipram is mediated by MAPK phosphatase-1. Br J Pharmacol. 2013 Aug;169(7):1525-36. [3]. Shalaby AM, et al. Effect of rolipram, a phosphodiesterase enzyme type-4 inhibitor, on γ-amino butyric acid content of the frontal cortex in mice exposed to chronic mild stress. J Pharmacol Pharmacother. 2012 Apr;3(2):132-7 |
Molecular Formula |
C16H21NO3
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Molecular Weight |
275.34
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CAS # |
61413-54-5
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Related CAS # |
(R)-(-)-Rolipram;85416-75-7;(S)-(+)-Rolipram;85416-73-5
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C1NCC(C2=CC=C(OC)C(OC3CCCC3)=C2)C1
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InChi Key |
HJORMJIFDVBMOB-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C16H21NO3/c1-19-14-7-6-11(12-9-16(18)17-10-12)8-15(14)20-13-4-2-3-5-13/h6-8,12-13H,2-5,9-10H2,1H3,(H,17,18)
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Chemical Name |
4-(3-(cyclopentyloxy)-4-methoxyphenyl)pyrrolidin-2-one
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Synonyms |
ZK-62711; SB 95952; SB95952; SB-95952; ME-3167; ZK-62711; ME3167; ZK62711; ME 3167; ZK 62711
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.08 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.08 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.08 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 30% PEG400+0.5% Tween80+5% propylene glycol:10 mg/L |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.6319 mL | 18.1594 mL | 36.3187 mL | |
5 mM | 0.7264 mL | 3.6319 mL | 7.2637 mL | |
10 mM | 0.3632 mL | 1.8159 mL | 3.6319 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT05522673 | Terminated Has Results | Drug: 11(R)-rolipram | Depression | National Institute of Mental Health (NIMH) |
February 8, 2023 | Phase 1 |
NCT00011375 | Completed | Drug: Rolipram | Multiple Sclerosis | National Institute of Neurological Disorders and Stroke (NINDS) |
February 2001 | Phase 2 |
NCT01215552 | Terminated | Drug: HT-0712 | Healthy Elderly Volunteers | Dart NeuroScience, LLC | September 2010 | Phase 1 |
NCT00250172 | Completed | Drug: [C-11](R)-rolipram | Dosimetry Healthy |
National Institute of Mental Health (NIMH) |
October 31, 2005 | Phase 1 |