Rolipram

Catalog No.S1430 Batch:S143001

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Technical Data

Formula

C16H21NO3
Molecular Weight 275.34 CAS No. 61413-54-5
Solubility (25°C)* In vitro DMSO 55 mg/mL (199.75 mM)
Ethanol 55 mg/mL (199.75 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 2.300mg/ml (8.35mM) Taking the 1 mL working solution as an example, add 50 μL of 46 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 2.300mg/ml (8.35mM) Taking the 1 mL working solution as an example, add 50 μL of 46 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description The PDE4 selective inhibitor, Rolipram, inhibited immunopurified PDE4B and PDE4D activities similarly, with IC50 values of approx. 130 nM and 240 nM respectively; an anti-inflammatory agent.
Targets
PDE4B [1]
(Cell-free assay)		 PDE4D [1]
(Cell-free assay)
130 nM 240 nM

Protocol (from reference)

References

  • https://pubmed.ncbi.nlm.nih.gov/10749688/

Customer Product Validation

D, average percentage difference of cell growth by PDE4D inhibitors between STK11 mutant and wild-type cell lines. The sensitivity on STK11mt cell lines represents the difference of average percentage growth between STK11-mutant (NCI-H1993 and NCI-H1395) and wild-type cell lines (NCI-H82 and NCI-H524). Average percentage growth of each cell line by a PDE4D inhibitor was based on the DMSO control. Cells were treated with a 20 μmol/L of PDE4D inhibitors for 3, 7, and 10 days incubation, respectively. The cell viability was determined using CellTiter-Blue fluorescence. *, P < 0.01 and **, P < 0.05 in the difference between STK11-mutant and wild-type cell lines. All cells used in the experiment were cultured in normal conditioned RPMI medium with 10% FBS and 1% penicillin/streptavidin.

Data from [ , , Mol Cancer Ther, 2014, 13(10):2463-73. ]

Rolipram attenuated neuronal apoptosis in ipsilateral cortex after SAH. (A) Representative transferase-mediated deoxyuridine triphosphate-biotin nick end labeling (TUNEL)/NeuN photomicrographs of the ipsilateral cortex in different groups (scale bar=50 μm). Fluorescence colors: DAPI, blue; TUNEL, green；and NeuN, red. (B) Quantification of the TUNEL/NeuN positive cells in the ipsilateral cortex in different groups. n=4. Data were presented as mean ± SD. *P < .05 versus sham group; #P < .05 versus SAH+vehicle group.

Data from [ , , Biomed Pharmacother, 2018, 99:947-955 ]

Panel C shows the effect of rolipram against H2O2 toxicity and hypoxia in PC12, SH-SY5Y, and NT2 cell lines (*P < .5 vs group without rolipram treatment). shRNA ¼ short hairpin RNA.

Data from [ , , J Sex Med, 2016, 13(12):1834-1843 ]

Representative microphotographs showed the co-localization of NeuN (red) with TUNEL (green)-positive cells in the ipsilateral cortex at 24 h after SAH.

Data from [ , , Neurochem Res, 2018, 43(4):785-795 ]

Selleck's Rolipram Has Been Cited by 18 Publications

P2RY14 cAMP signaling regulates Schwann cell precursor self-renewal, proliferation, and nerve tumor initiation in a mouse model of neurofibromatosis [ Elife, 2022, 11e73511] PubMed: 35311647
Purinergic Signaling in Neurofibromatosis Type 1: Characterizing the Role of P2RY14 in Neurofibroma Development [ ProQuest, 2022, 30509631] PubMed: None
Roflupram protects against rotenone-induced neurotoxicity and facilitates α-synuclein degradation in Parkinson's disease models [ Acta Pharmacol Sin, 2021, 10.1038/s41401-021-00768-4] PubMed: 34531546
Rolipram Prevents the Formation of Abdominal Aortic Aneurysm (AAA) in Mice: PDE4B as a Target in AAA [ Antioxidants (Basel), 2021, 10(3)460] PubMed: 33809405
Release of adenosine-induced immunosuppression: Comprehensive characterization of dual A2A/A2B receptor antagonist [ Int Immunopharmacol, 2021, 96:107645] PubMed: 33894488
The protective effect of the PDE-4 inhibitor rolipram on intracerebral haemorrhage is associated with the cAMP/AMPK/SIRT1 pathway [ Sci Rep, 2021, 11(1):19737] PubMed: 34611179
MicroRNA-30d-5p ameliorates lipopolysaccharide-induced acute lung injury via activating AMPKα [ Immunopharmacol Immunotoxicol, 2021, 43(4):431-442] PubMed: 34157933
Roflupram exerts neuroprotection via activation of CREB/PGC-1α signalling in experimental models of Parkinson's disease. [ Br J Pharmacol, 2020, 177(10):2333-2350] PubMed: 31972868
Roflupram, a novel phosphodiesterase 4 inhibitor, inhibits lipopolysaccharide-induced neuroinflammatory responses through activation of the AMPK/Sirt1 pathway [ Int Immunopharmacol, 2020, S1567-5769(20)33643-2] PubMed: 33243606
The diacylglycerol kinase α (DGKα)/Akt/NF-κB feedforward loop promotes esophageal squamous cell carcinoma (ESCC) progression via FAK-dependent and FAK-independent manner [ Oncogene, 2019, 38(14):2533-2550] PubMed: 30532074

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.