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Rolipram

Catalog No. T6644 CAS 61413-54-5

Synonyms: SB 95952, ZK 62711, (R,S)-Rolipram

Rolipram (SB 95952) is a phosphodiesterase 4 inhibitor with antidepressant properties.

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Rolipram, CAS 61413-54-5

Pack Size	Availability	Price/USD
10 mg	In stock	$ 43.00
50 mg	In stock	$ 61.00
100 mg	In stock	$ 87.00
200 mg	In stock	$ 128.00
500 mg	In stock	$ 212.00
1 mL * 10 mM (in DMSO)	In stock	$ 48.00

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Purity: 99.26%

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Description	Rolipram (SB 95952) is a phosphodiesterase 4 inhibitor with antidepressant properties.
Targets&IC50	PDE4B:130 nM, PDE4D:240 nM
In vitro	The PDE4 selective inhibitor, Rolipram, inhibits immunopurified PDE4B and PDE4D activities similarly, with IC50s of approx. 130 nM and 240 nM respectively. In contrast, Rolipram inhibits immunopurified PDE4A activity with a dramatically lower IC50 of around 3 nM. Rolipram increases phosphorylation of cAMP-response-element-binding protein (CREB) in U937 cells in a dose-dependent fashion, which means that both high affinity (IC50 approx. 1 nM) and low affinity (IC50 approx. 120 nM) components are presented. Rolipram dose-dependently inhibits the IFN-gamma-stimulated phosphorylation of p38 MAPK in a simple monotonic fashion with an IC50 of approx. 290 nM[1]. Rolipram is a selective PDE4 inhibitor that inhibits all PDE4 isoforms A, B, C and D. Rolipram inhibits LPS-induced TNF production in a dose-dependent manner (IC50 25.9 nM), and maximal/submaximal inhibition is observed with 2 μM drug concentration in J774 cells[2].
In vivo	In peritoneal macrophages (PM) from wild-type (WT) mice, lipopolysaccharide (LPS) induces TNF mRNA and protein expression, which is significantly reduced by Rolipram (by 74% and 63% for TNF mRNA and protein, respectively). However, LPS-induced TNF production is elevated in PM from MKP-1(-/-) mice compared to WT mice, aligning with existing research. Notably, Rolipram's ability to suppress TNF mRNA and protein levels in PM from MKP-1(-/-) mice is considerably weakened and lacks statistical significance. Furthermore, repeated Rolipram administration (1.25 mg/kg, i.p.) diminishes the incidence of escape failures in rats with learned helplessness, suggesting its potential therapeutic effect.
Cell Research	Rolipram is dissolved in DMSO and stored, and then diluted with appropriate medium before use[2]. J774 murine macrophages (ATCC) are cultured at 37°C in 5% CO2 atmosphere in DMEM supplemented with glutamax-1 containing 10% heat-inactivated FBS, 100 U/mL penicillin, 100 μg/mL streptomycin and 250 ng/mL amphotericin B. For experiments, cells are seeded on 24-well plates at a density of 2×105 cells per well. Cell monolayers are grown for 72 h before the experiments are started. Rolipram, IBMX and BIRB 796 are dissolved in DMSO, and 8-Br-cAMP in HBSS. LPS (10 ng/mL) or the compounds of interest at concentrations indicated or the solvent (DMSO, 0.1% v/v) are added to the cells in fresh culture medium containing 10% FBS and the supplements. Cells are further incubated for the time indicated. The effect of LPS and the tested chemicals on cell viability is evaluated by Cell Proliferation Kit II (XTT)[2].

Synonyms	SB 95952, ZK 62711, (R,S)-Rolipram
Molecular Weight	275.34
Formula	C16H21NO3
CAS No.	61413-54-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 20.7 mg/mL (75 mM)

DMSO: 20.7 mg/mL (75 mM)

References and Literature

1. MacKenzie SJ, et al. Action of rolipram on specific PDE4 cAMP phosphodiesterase isoforms and on the phosphorylation of cAMP-response-element-binding protein (CREB) and p38 mitogen-activated protein (MAP) kinase in U937 monocyticcells. Biochem J. 2000 Apr 2. Korhonen R, et al. Attenuation of TNF production and experimentally induced inflammation by PDE4 inhibitor rolipram is mediated by MAPK phosphatase-1. Br J Pharmacol. 2013 Aug;169(7):1525-36. 3. Shalaby, A., & Kamal, S. (2012). Effect of rolipram, a phosphodiesterase enzyme type-4 inhibitor, on γ-amino butyric acid content of the frontal cortex in mice exposed to chronic mild stress. J Pharmacol Pharmacother, 3(2), 132-7. doi: 10.4103/0976-500X.95509

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Neurodegenerative Disease Compound Library Drug Repurposing Compound Library Clinical Compound Library NO PAINS Compound Library CNS-Penetrant Compound Library Bioactive Compounds Library Max Stem Cell Differentiation Compound Library Human Metabolite Library Metabolism Compound Library

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Keywords

Rolipram 61413-54-5 Metabolism Microbiology/Virology Proteases/Proteasome Antibacterial PDE HIV Protease SB-95952 Human immunodeficiency virus SB 95952 Inhibitor Bacterial ZK 62711 Phosphodiesterase (PDE) (R,S)-Rolipram ZK-62711 HIV inhibit ZK62711 SB95952 inhibitor

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