咯利普兰 T6644

Product Introduction
Bioactivity


英文名: Rolipram

描述: Rolipram (SB 95952) 是一种磷酸二酯酶 PDE4的选择性抑制剂，抑制 PDE4A，PDE4B 和 PDE4D 的 IC50分别为 3 nM，130 nM 和 240 nM。

细胞实验: 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].

体外活性: 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].

体内活性: TNF mRNA and protein expression is induced by LPS in peritoneal macrophages (PM) from WT mice, and that is clearly (by 74 and 63% for TNF mRNA and TNF protein, respectively) inhibited by Rolipram. LPS-induced TNF production is enhanced in PM from MKP-1(-/-) mice as compared to that in PM from WT mice, which is consistent with the published results. Interestingly, the inhibition of TNF mRNA and protein expression by Rolipram is markedly attenuated in PM from MKP-1(-/-) mice and does not reach statistical significance[2]. Repeated administration of Rolipram (1.25 mg/kg, i.p.) reduces the number of escape failures in learned helplessness rats[3].

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

溶解度: Ethanol : 20.7 mg/mL (75 mM)
DMSO : 20.7 mg/mL (75 mM)
5% DMSO+95% Saline : 1.04 mg/mL (3.76 mM, suspension)


关键字: SB-95952 | Human immunodeficiency virus | Inhibitor | Rolipram | Bacterial | Phosphodiesterase (PDE) | ZK-62711 | HIV | inhibit | ZK62711 | SB95952

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相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Anti-COVID-19 Compound Library | Bioactive Compounds Library Max | Anti-Metabolism Disease Compound Library | Inhibitor Library | Anti-Bacterial Compound Library | Preclinical Compound Library | Anti-Viral Compound Library | Anti-Alzheimer's Disease Compound Library

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