| Name | (S)-(+)-Rolipram |
| Description | (S)-(+)-Rolipram ((+)-Rolipram) inhibits human monocyte cyclic AMP-specific PDE4 with an IC50 of 0.75 μM and exhibits anti-inflammatory and anti-depressant activity in the central nervous system, though it is less potent than its R enantiomer. |
| In vitro | S-(+)-Rolipram suppresses LPS-induced TNFα expression from human monocyte through inhibiting PDE4 with IC50 about 2 μM. [1] 1 μM S-(+)-Rolipram significantly antagonizes ovalbumin (OA) induced concentration-related contractions of tracheal rings which are isolated from OA-sensitized guinea pigs. [2] 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. [3] 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 [Cip1] and p27 [Kip1], 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. [4] |
| In vivo | In 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. [2] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (7.26 mM), Sonication is recommended.
DMSO : 27.5 mg/mL (99.88 mM), Sonication is recommended.
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| Keywords | tumor | TNFα | S- Rolipram | Rolipram | Phosphodiesterase (PDE) | phosphodiesterase | PDE4 | necrosis | mononuclear | Inhibitor | inhibit | factor | cAMP | Apoptosis | (S)(+)Rolipram | (S) (+) Rolipram |
| Inhibitors Related | Stavudine | Aceglutamide | Urea | Tamoxifen | Cysteamine hydrochloride | D(+)-Raffinose pentahydrate | Metronidazole | Citric Acid Triammonium | Formamide | Dimethyl phthalate | Alginic acid | Sildenafil citrate |
| Related Compound Libraries | Apoptosis Compound Library | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Inhibitor Library | Anti-Cardiovascular Disease Compound Library | Metabolism Compound Library | Immunology/Inflammation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Preclinical Compound Library | Anti-Metabolism Disease Compound Library | Nucleotide Compound Library |
United States
