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(S)-(+)-Rolipram

SKU: orb1300585

Description

(+)-Rolipram is a selective PDE4 inhibitor with an IC50 of 0.75 μM against the human monocyte enzyme. This compound exhibits anti-inflammatory and CNS antidepressant activities in research models, though it is less potent than its (R)-enantiomer. It is widely used in vitro and in vivo to study PDE4 biology and inflammation-related pathways.

Research Area

Cell Biology, Metabolism Research

Images & Validation

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(S)-(+)-Rolipram

Key Properties

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CAS Number85416-73-5
MW275.34
Purity99.71%
FormulaC16H21NO3
SMILESCOc1ccc(cc1OC1CCCC1)[C@H]1CNC(=O)C1
TargetApoptosis,PDE
SolubilityDMSO:27.5 mg/mL (99.88 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (7.26 mM)

Bioactivity

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Target IC50
PDE4:0.75 μM
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.
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In Vitro
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 [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.
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Storage & Handling

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StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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(S)-Rolipram, (S)(+)Rolipram, (S) (+) Rolipram, (+)-Rolipram, Apoptosis, cAMP, necrosis, PDE4, inhibit, mononuclear, Inhibitor, factor, Phosphodiesterase (PDE), phosphodiesterase, TNFα, Rolipram, S- Rolipram, S- (+)-Rolipram, tumor

Similar Products

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  • S- (+)-Rolipram

    S- (+)-Rolipram [orb1223027]

    >98% (HPLC)

    85416-73-5

    275.34

    C16H21NO3

    1 g, 500 mg, 200 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg
Quality Guarantee

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Compound Identifiers

PubChem CID
158758 ↗

Key Properties

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No computed properties available.

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(S)-(+)-Rolipram (orb1300585)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

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2 mg
$ 70.00
1 ml x 10 mM (in DMSO)
$ 90.00
5 mg
$ 90.00
10 mg
$ 120.00
25 mg
$ 180.00
50 mg
$ 270.00
100 mg
$ 380.00
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