Home Metabolism PDE inhibitor S-(+)-Rolipram For research use only.

S-(+)-Rolipram

S-(+)-Rolipram inhibits human monocyte cyclic AMP-specific PDE4 with IC50 of 0.75 μM, has anti-inflammatory and anti-depressant activity in the central nervous system, less potent than its R enantiomer.

S-(+)-Rolipram Chemical Structure

S-(+)-Rolipram Chemical Structure

CAS: 85416-73-5

Selleck's S-(+)-Rolipram has been cited by 1 publication

Purity & Quality Control

Batch: S212701 DMSO] 55 mg/mL] false] Ethanol] 55 mg/mL] false] Water] Insoluble] false Purity: 100%
100

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Signaling Pathway

PDE Signaling Pathways

PDE Signaling Pathway

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Biological Activity

Description S-(+)-Rolipram inhibits human monocyte cyclic AMP-specific PDE4 with IC50 of 0.75 μM, has anti-inflammatory and anti-depressant activity in the central nervous system, less potent than its R enantiomer.
Targets
PDE4 [1]
0.75 μM
In vitro
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 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]
Animal Research Animal Models Male Hartley guinea pigs
Dosages 1 mL/kg
Administration Administered via i.v.

Chemical Information & Solubility

Molecular Weight 275.34 Formula

C16H21NO3
CAS No. 85416-73-5 SDF Download S-(+)-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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