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    Rolipram (ME 3167; ZK 62711; SB 95952)
    Rolipram (ME 3167; ZK 62711; SB 95952)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0788
    CAS #: 61413-54-5 Purity ≥98%

    Description: 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.  

    References: Trends Pharmacol Sci. 1997 May;18(5):164-71; Br J Pharmacol. 1996 Jun;118(3):649-58; J Pharmacol Exp Ther. 1993 Jul;266(1):306-13.

    Related CAS: 85416-75-7 (R-enantiomer of Rolipram); 85416-73-5 (S-enantiomer of Rolipram)

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    Molecular Weight (MW)275.34
    FormulaC16H21NO3
    CAS No.61413-54-5 (racemic); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 55 mg/mL (199.8 mM)
    Water:<1 mg/mL
    Ethanol:  55 mg/mL (199.8 mM)
    Solubility (In vivo)30% PEG400+0.5% Tween80+5% propylene glycol: 10 mg/L 
    SynonymsZK-62711; SB 95952; SB95952; SB-95952; ME-3167; ZK-62711; ME3167; ZK62711; ME 3167; ZK 62711 

    Chemical Name: 4-(3-(cyclopentyloxy)-4-methoxyphenyl)pyrrolidin-2-one

    InChi Key: HJORMJIFDVBMOB-UHFFFAOYSA-N

    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)

    SMILES Code: O=C1NCC(C2=CC=C(OC)C(OC3CCCC3)=C2)C1


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    In Vitro

    In vitro activity: S-(+)-Rolipram suppresses LPS-induced TNFα expression from human monocyte through inhibiting PDE4 with IC50 about 2 μM. 1 μM S-(+)-Rolipram significantly antagonizes ovalbumin (OA) induced concentration-related contractions of tracheal rings which are isolated from OA-sensitized guinea pigs. S-(+)-Rolipram inhibits PDE4 activity in a CHO-K1 cell line which stably expresses a recombinant full length human PDE-4a with IC50 at 450 nM. Treatment of the human glioma cell line A-172 with Rolipram (including both R- and S-enantiomers of Rolipram) results in increased expression of the cell cycle inhibitors p21 and p27, and decreased activity of cdk2, a cyclindependent kinase essential for cell cycle progression. As a result, the proliferation of A-172 cells is inhibited, with induction of a G1 block. Eventually, Rolipram-treated A-172 cells undergo differentiation, which is followed by apoptotic cell death.


    Kinase Assay: The PDE4 selective inhibitor, Rolipram, inhibits immunopurified PDE4B and PDE4D activities similarly, with IC50s of approx. 130 nM and 240 nM respectively. In contrast, Rolipram inhibits immunopurified PDE4A activity with a dramatically lower IC50 of around 3 nM. Rolipram increases phosphorylation of cAMP-response-element-binding protein (CREB) in U937 cells in a dose-dependent fashion, which implies the presence of both high affinity (IC50 approx. 1 nM) and low affinity (IC50 approx. 120 nM) components. Rolipram dose-dependently inhibits the IFN-gamma-stimulated phosphorylation of p38 MAPK in a simple monotonic fashion with an IC50 of approx. 290 nM.


    Cell Assay: J774 murine macrophages (ATCC) are cultured at 37°C in 5% CO2 atmosphere in DMEM supplemented with glutamax-1 containing 10% heat-inactivated FBS, 100 U/mL penicillin, 100 μg/mL streptomycin and 250 ng/mL amphotericin B. For experiments, cells are seeded on 24-well plates at a density of 2×105 cells per well. Cell monolayers are grown for 72 h before the experiments are started. Rolipram, IBMX and BIRB 796 are dissolved in DMSO, and 8-Br-cAMP in HBSS. LPS (10 ng/mL) or the compounds of interest at concentrations indicated or the solvent (DMSO, 0.1% v/v) are added to the cells in fresh culture medium containing 10% FBS and the supplements. Cells are further incubated for the time indicated. The effect of LPS and the tested chemicals on cell viability is evaluated by Cell Proliferation Kit II (XTT).

    In VivoIn anesthetized, ventilated OA-sensitive guinea pigs, S-(+)-Rolipram reduces OA-induced bronchoconstriction with ID50 values of approximately 0.25 mg/kg i.v. Histamine- and leukotriene D4-induced bronchoconstriction are not affected by doses of S-(+)-Rolipram which abolishes the response to OA. Higher doses (3-10 mg/kg) reduce histamine-, but not the leukotriene D4-induced bronchoconstriction. In conscious OA-sensitive guinea pigs, intragastric pretreatment with S-(+)-Rolipram dose-dependently reduces both the OA-induced decreases in specific conductance as well as the corresponding pulmonary eosinophil influx as assessed by both bronchoalveolar lavage and histological evaluation.
    Animal modelMale Hartley guinea pigs
    Formulation & DosageDissolved in 100% PEG at an appropriate concentration; 1 mL/kg; i.v. injection
    ReferencesTrends Pharmacol Sci. 1997 May;18(5):164-71; Br J Pharmacol. 1996 Jun;118(3):649-58; J Pharmacol Exp Ther. 1993 Jul;266(1):306-13.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Rolipram

    Br J Pharmacol. 1996 Jun; 118(3): 649–658.


    Rolipram

    Br J Pharmacol. 1996 Jun; 118(3): 649–658.



    Rolipram

    Br J Pharmacol. 1996 Jun; 118(3): 649–658.


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