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Rolipram

Rolipram

产品编号 T6644   CAS 61413-54-5
别名: SB 95952, ZK 62711, 咯利普兰, (R,S)-Rolipram

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。

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Rolipram Chemical Structure
Rolipram, CAS 61413-54-5
规格 价格/CNY 货期 数量
5 mg ¥ 257 现货
10 mg ¥ 413 现货
50 mg ¥ 578 待询
100 mg ¥ 813 待询
200 mg ¥ 1,180 待询
500 mg ¥ 1,980 待询
1 mL * 10 mM (in DMSO) ¥ 455 现货
其他形式的 Rolipram:
产品目录号及名称: Rolipram (T6644)
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纯度: 99.26%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Rolipram (SB 95952) is a phosphodiesterase 4 inhibitor with antidepressant properties.
靶点活性 PDE4B:130 nM, PDE4D:240 nM
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].
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].
别名 SB 95952, ZK 62711, 咯利普兰, (R,S)-Rolipram
分子量 275.34
分子式 C16H21NO3
CAS No. 61413-54-5

存储

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)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 3.6319 mL 18.1594 mL 36.3187 mL 90.7968 mL
5 mM 0.7264 mL 3.6319 mL 7.2637 mL 18.1594 mL
10 mM 0.3632 mL 1.8159 mL 3.6319 mL 9.0797 mL
20 mM 0.1816 mL 0.908 mL 1.8159 mL 4.5398 mL
50 mM 0.0726 mL 0.3632 mL 0.7264 mL 1.8159 mL

计算器

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稀释计算器
配液计算器
分子量计算器
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参考文献

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
Trapidil Gisadenafil AN3199 Bucladesine sodium CALP2 acetate(261969-04-4 free base) Apremilast-d5 Lotamilast Lirimilast

相关化合物库

该产品包含在如下化合物库中:
神经退行性疾病化合物库 NO PAINS 化合物库 抗菌活性库 抗心血管疾病化合物库 已知活性化合物库 抗阿尔茨海默症化合物库 抑制剂库 经典已知活性库 免疫/炎症分子化合物库 人代谢物化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% ddH2O
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

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

 

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