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Postion:Product Catalog >Biochemical Engineering>Inhibitors>Metabolism>PDE inhibitors>Rolipram
Rolipram
  • Rolipram

Rolipram NEW

Price $43 $61 $87
Package 10mg 50mg 100mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-19

Product Details

Product Name: Rolipram CAS No.: 61413-54-5
Purity: 99.26% Supply Ability: 10g
Release date: 2024/11/19

Product Introduction

Bioactivity

NameRolipram
DescriptionRolipram (SB 95952) is a phosphodiesterase 4 inhibitor with antidepressant properties.
Cell ResearchRolipram 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].
In vitroThe 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 vivoIn 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.
Storagestore at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationEthanol : 20.7 mg/mL (75 mM)
DMSO : 20.7 mg/mL (75 mM)
KeywordsZK-62711 | ZK62711 | SB-95952 | SB95952 | Rolipram | Phosphodiesterase (PDE) | Inhibitor | inhibit | Human immunodeficiency virus | HIV | Bacterial
Inhibitors RelatedNeomycin sulfate | Stavudine | Dehydroacetic acid sodium | Emtricitabine | Ampicillin sodium | Methyl anthranilate | Dextran sulfate sodium salt (MW 4500-5500) | Kanamycin sulfate | Sulfamethoxazole sodium | Lamivudine | Doxycycline | Dimethyl sulfoxide
Related Compound LibrariesBioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Anti-Alzheimer's Disease Compound Library | Drug Repurposing Compound Library | Anti-Viral Compound Library | Inhibitor Library | Anti-Cardiovascular Disease Compound Library | Anti-Bacterial Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Preclinical Compound Library | Anti-COVID-19 Compound Library

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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