Rolipram

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Chemical Structure| 61413-54-5 同义名 : (R,S)-Rolipram;ZK 62711;ME-3167;SB 95952;(±)-Rolipram
CAS号 : 61413-54-5
货号 : A110225
分子式 : C16H21NO3
纯度 : 99%+
分子量 : 275.343
MDL号 : MFCD00270906
存储条件：

Pure form Sealed in dry,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 40 mg/mL(145.27 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • PDE4

    PDE4B, IC50:130 nM
描述 cAMP is a fundamental second-messenger molecule produced in essentially all mammalian cells. 3′5′-Cyclic nucleotide phosphodiesterases (PDEs) are the enzymatic machinery that is responsible for the degradation of cAMP in cells by catalysing the hydrolysis of cAMP to 5′AMP. PDE4 family members specifically degrade cAMP, and they are expressed essentially in all immune cells including macrophages, neutrophils, eosinophils and lymphocytes, and in many other cell types, including epithelial cells, endothelium and fibroblasts. Rolipram is a selective inhibitor of phosphodiesterase PDE4, especially the PDE4B with IC50 of 130 nM and IC50 of 240 nM for PDE4D, with anti-inflammatory activity. Transient global cerebral ischemia in rats was induced by BCCAO. Rolipram at 0.3 mg/kg, but not 0.1 mg/kg, increased the time spent in the open arms and Discrimination index in the object location task, and the number of DCX-immunoreactive (DCX is a microtubule protein transiently expressed in both cytoplasm and dendrites of newborn neurons) neurons in BCCAO mice as compared to the BCCAO + veh group[3]. Bevacizumab (6.5 μg/ml) and rolipram (103 μM) individually led to the significant increase in the relative values of p53 and cleaved-caspase3 expressions in glioblastoma cancer stem-like cells (GCSCs) and the effect was strongly amplified when bevacizumab and rolipram were added to culture medium simultaneously[4]. Rolipram inhibited LPS-induced TNF production and TNF mRNA levelsin a dose-dependent manner (IC50 25.9 nM) in J774 mouse macrophages, which was mediated by MAPK phosphatase-1 (MKP-1)[5].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
COS7 cells Function assay Inhibition of PDE4B2 expressed in COS7 cells assessed as cAMP hydrolysis, IC50=0.105 μM 18222088
HEK293 cells Function assay Inhibition of PDE4 expressed in HEK293 cells coexpressing G-protein coupled receptor and cyclic nucleotide gated ion channel by fluorescence assay, EC50=0.1315 μM 19464886
human PBMC Function assay Inhibition of LPS-induced TNFalpha production in human PBMC, IC50=0.06 μM 19049349
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01805518 Adverse Mental/Physical Effect... 展开 >>s of Low Dose S. Tortuosum. 收起 << Phase 1 Completed - Puerto Rico ... 展开 >> Michel A. Woodbury, MD San Juan, Puerto Rico, 00918 收起 <<
NCT02743377 Nervous System Disease Phase 1 Phase 2 Recruiting March 25, 2020 United States, Maryland ... 展开 >> National Institutes of Health Clinical Center Recruiting Bethesda, Maryland, United States, 20892 Contact: For more information at the NIH Clinical Center contact Office of Patient Recruitment (OPR)    800-411-1222 ext TTY8664111010    prpl@cc.nih.gov 收起 <<
NCT01602900 Huntington Disease Phase 1 Completed - United Kingdom ... 展开 >> GSK Investigational Site London, United Kingdom, NW10 7EW GSK Investigational Site London, United Kingdom, W12 ONN 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.63mL

0.73mL

0.36mL

18.16mL

3.63mL

1.82mL

36.32mL

7.26mL

3.63mL
参考文献

[1]Korhonen R, Hommo T, 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.

[2]MacKenzie SJ, Houslay MD. 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 monocytic cells. Biochem J. 2000 Apr 15;347(Pt 2):571-8.

[3]Soares LM, De Vry J, Steinbusch HWM, Milani H, Prickaerts J, Weffort de Oliveira RM. Rolipram improves cognition, reduces anxiety- and despair-like behaviors and impacts hippocampal neuroplasticity after transient global cerebral ischemia. Neuroscience. 2016 Jun 21;326:69-83. doi: 10.1016/j.neuroscience.2016.03.062. Epub 2016 Apr 4. PMID: 27058148.

[4]Ramezani S, Vousooghi N, Kapourchali FR, Hadjighasem M, Hayat P, Amini N, Joghataei MT. Rolipram potentiates bevacizumab-induced cell death in human glioblastoma stem-like cells. Life Sci. 2017 Mar 15;173:11-19. doi: 10.1016/j.lfs.2017.02.005. Epub 2017 Feb 12. PMID: 28202289.

[5]Korhonen R, Hömmö T, Keränen T, Laavola M, Hämäläinen M, Vuolteenaho K, Lehtimäki L, Kankaanranta H, Moilanen E. 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. doi: 10.1111/bph.12189. PMID: 23849041; PMCID: PMC3724109.