货号:A110225
同义名:
(R,S)-Rolipram;ZK 62711
Rolipram is a selective inhibitor of phosphodiesterases PDE 4, especially the PDE 4B with IC50 of 130 nM while IC50 for PDE4D is 240 nM, it's an anti-inflammatory agent.
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产品名称 | PDE ↓ ↑ | PDE1 ↓ ↑ | PDE10A ↓ ↑ | PDE2 ↓ ↑ | PDE3 ↓ ↑ | PDE4 ↓ ↑ | PDE5 ↓ ↑ | PDE6 ↓ ↑ | 其他靶点 | 纯度 | |||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Doxofylline | ✔ | 99+% | |||||||||||||||||
Deltarasin |
+++
PDEδ , Kd: 38 nM |
99+% | |||||||||||||||||
7-(2,3-Dihydroxypropyl)theophylline | ✔ | 99%+ | |||||||||||||||||
Aminophylline |
+
PDE, IC50: 0.12 mM |
99%+ | |||||||||||||||||
Anagrelide HCl | ✔ | 99%+ | |||||||||||||||||
Irsogladine | ✔ | mAChR,AChR | 99%+ | ||||||||||||||||
PF-8380 |
+++
Autotaxin, IC50: 2.8 nM |
99%+ | |||||||||||||||||
Dipyridamole | ✔ | 99%+ | |||||||||||||||||
Balipodect |
++++
PDE10A, IC50: 0.3 nM |
99%+ | |||||||||||||||||
PF-2545920 |
++++
PDE10A, IC50: 0.37 nM |
97% | |||||||||||||||||
Luteolin |
+
PDE1, Ki: 15.0 μM |
++
PDE2, Ki: 6.4 μM |
+
PDE3, Ki: 13.9 μM |
+
PDE4, Ki: 11.1 μM |
+
PDE5, Ki: 9.5 μM |
98% | |||||||||||||
Milrinone |
++
PDE2, IC50: 5.2 μM |
++
PDE3, IC50: 2.1 μM |
ATPase | 99%+ | |||||||||||||||
Pimobendan |
++
PDE3, IC50: 0.32 μM |
99%+ | |||||||||||||||||
Cilostazol |
++
PDE3, IC50: 0.2 μM |
99%+ | |||||||||||||||||
Fenspiride HCl |
+
PDE3, pIC50: 3.44 |
+
PDE4, pIC50: 4.16 |
99%+ | ||||||||||||||||
(S)-(+)-Rolipram |
++
PDE4, IC50: 0.75 μM |
98% | |||||||||||||||||
Apremilast |
+++
PDE4, IC50: 74 nM |
98% | |||||||||||||||||
GSK256066 |
++++
PDE4B, IC50: 3.2 pM |
98+% | |||||||||||||||||
Roflumilast |
++++
PDE4A4, IC50: 4.3 nM PDE4A1, IC50: 0.7 nM |
99% | |||||||||||||||||
Rolipram |
+++
PDE4B, IC50: 130 nM |
99%+ | |||||||||||||||||
Cilomilast |
+++
LPDE4, IC50: 100 nM HPDE4, IC50: 120 nM |
98+% | |||||||||||||||||
Avanafil |
++++
PDE5, IC50: 1 nM |
99%+ | |||||||||||||||||
Vardenafil HCl Trihydrate |
++++
PDE5, IC50: 0.7 nM |
99%+ | |||||||||||||||||
Tadalafil |
++++
PDE5, IC50: 1.8 nM |
98% | |||||||||||||||||
Icariin |
++
PDE5, IC50: 0.432 μM |
98% | |||||||||||||||||
Sildenafil | ✔ |
+++
PDE6, IC50: 33 nM |
99%+ | ||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
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 | ||
human U937 cells | Function assay | Inhibition of PDE4 in human U937 cells assessed as accumulation of [3H]adenosine by scintillation counting, IC50=0.86 μM | 19303290 | ||
Dose | Mice: 1.25 mg/kg - 5 mg/kg[3] (i.p.); 0.015 mg/kg - 0.06 mg/kg[4] (s.c.) Rat: 0.03 mg/kg - 0.3 mg/kg[5] (i.p.), 0.5 mg/kg - 4 mg/kg[6] (i.p.) Guinea pig: 0.1 mg/kg - 10 mg/kg[7] (i.v.) |
Administration | i.p., s.c., i.v. |
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 << |
计算器 | ||||
存储液制备 | ![]() |
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 |
CAS号 | 61413-54-5 |
分子式 | C16H21NO3 |
分子量 | 275.343 |
别名 | (R,S)-Rolipram;ZK 62711;ME-3167;SB 95952;(±)-Rolipram |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,Store in freezer, under -20°C 液体 -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 |