Comparison

S-(+)-Rolipram European Partner

Item no. S2127-10
Manufacturer Selleckchem
CASRN 85416-73-5
Amount 10 mg
Quantity options 10 mg 1 g 10 g 10 mM/1 ml 25 mg 5 mg 50 mg 5 g
Category
Type Inhibitors
Specific against other
ECLASS 10.1 32160490
ECLASS 11.0 32160490
UNSPSC 12000000
Alias PDE4,PDE
Similar products S-
Available
Storage Conditions
2 years -20°C Powder, 2 weeks 4°C in DMSO, 2 months -80°C in DMSO
Molecular Weight
275, 34
Administration
Administered via i.v.
Animal Models
Male Hartley guinea pigs
Clinical Trials
Rolipram (including both R- and S-enantiomers of Rolipram) is under the Phase I clinical trial for its antidepressant effects on cAMP specific phosphodiesterase (PDE4) in depressed patients.
Dosages
1 mL/kg
Formulation
S-(+)-Rolipram is dissolved in 100% PEG at an appropriate concentration.
IC50
750 nM [1], 750 nM [1], 750 nM [1], 750 nM [1], 750 nM [1], 750 nM [1]
In vitro
S-(+)-Rolipram suppresses LPS-induced TNFalpha expression from human monocyte through inhibiting PDE4 with IC50 about 2 uM. [1] 1 uM 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]
Kinase Assay
PDE Assay, PDE activity is determined by the two-step radioisotope method of Thompson et al (1979). The reaction mixture contains: Tris-HCl 20 mM (pH 8.0), MgCl2 10 mM, 2-mercaptoethanol 4 mM, ethyleneglycol-bis-(f-aminoethyl ether) N, N, N', N'-tetraacetic acid (EGTA) 0.2 mM, bovine serum albumin, 0.05 mg/mL. Unless otherwise stated, the substrate concentration is 1 uM. The IC50 values (concentration which produced 50% inhibition of substrate hydrolysis) for the compounds are determined from concentration (0.1 nM to 40 uM)-response curves. At least three concentration-response curves are generated for each agent.
Solubility (25C)
DMSO 55 mg/mL, Water <1 mg/mL, Ethanol 55 mg/mL
Information
S-(+)-Rolipram inhibits human monocyte cyclic AMP-specific PDE4 with IC50 of 0.75 uM.

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.

Amount: 10 mg
Available: In stock
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