Rolipram-R-S-Rolipram-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemERolipramCat. No.: HY-16900CAS No.: 61413-54-5Synonyms: (R,S)-Rolipram; SB 95952; ZK 62711分式: CHNO分量: 275.34作靶点: Phosphodiesterase (PDE)作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C

2、1 month溶解性数据体外实验 DMSO : 41 mg/mL (148.91 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.6319 mL 18.1594 mL 36.3187 mL5 mM 0.7264 mL 3.6319 mL 7.2637 mL10 mM 0.3632 mL 1.8159 mL 3.6319 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当

3、的溶解案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (9.08 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (9.08 mM); Clear solut

4、ion1/3 Master of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (9.08 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Rolipram种选择性的磷酸酯酶 PDE4 抑制剂，抑制 PDE4A，PDE4B 和 PDE4D，的 IC50 分别为 3nM，130 nM 和 240 nM。IC50 & Target IC50: 3 nM (PDE4A), 130 nM (PDE4B), 240 nM (PDE4

5、D) 1体外研究 The PDE4 selective inhibitor, Rolipram, inhibits immunopurified PDE4B and PDE4D activities similarly, withIC50s of approx. 130 nM and 240 nM respectively. In contrast, Rolipram inhibits immunopurified PDE4Aactivity with a dramatically lower IC50 of around 3 nM. Rolipram increases phosphoryl

6、ation of cAMP-response-element-binding protein (CREB) in U937 cells in a dose-dependent fashion, which implies thepresence of both high affinity (IC50 approx. 1 nM) and low affinity (IC50 approx. 120 nM) components.Rolipram dose-dependently inhibits the IFN-gamma-stimulated phosphorylation of p38 MA

7、PK in a simplemonotonic fashion with an IC50 of approx. 290 nM 1. Rolipram is a selective PDE4 inhibitor that inhibits allPDE4 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 M drug co

8、ncentration in J774 cells2.体内研究 TNF mRNA and protein expression is induced by LPS in peritoneal macrophages (PM) from WT mice, andthat 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 com

9、pared to that in PM from WT mice,which is in line with the published results. Interestingly, the inhibition of TNF mRNA and protein expressionby Rolipram is markedly attenuated in PM from MKP-1(-/-) mice and does not reach statistical significance2. Repeated administration of Rolipram (1.25 mg/kg, i

10、.p.) reduces the number of escape failures in learnedhelplessness rats 3.PROTOCOLCell Assay 2 J774 murine macrophages (ATCC) are cultured at 37C in 5% CO2 atmosphere in DMEM supplementedwith glutamax-1 containing 10% heat-inactivated FBS, 100 U/mL penicillin, 100 g/mL streptomycin and 250ng/mL ampho

11、tericin B. For experiments, cells are seeded on 24-well plates at a density of 2105 cells perwell. Cell monolayers are grown for 72 h before the experiments are started. Rolipram, IBMX and BIRB 796are dissolved in DMSO, and 8-Br-cAMP in HBSS. LPS (10 ng/mL) or the compounds of interest atconcentrati

12、ons indicated or the solvent (DMSO, 0.1% v/v) are added to the cells in fresh culture mediumcontaining 10% FBS and the supplements. Cells are further incubated for the time indicated. The effect ofLPS and the tested chemicals on cell viability is evaluated by Cell Proliferation Kit II (XTT) 2.MCE ha

13、s not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 22/3 Master of Small Molecules 您边的抑制剂师www.MedChemEAdministration 2 Inbred C57BL/6 MKP-1(-/-) mice are used. C57BL/6 mice (20-25 g) are divided into groups of six mice andtreated with 200 L of PBS or

14、Rolipram (100 mg/kg in PBS) by an i.p. injection 2 h before applyingcarrageenan. Before the administration of carrageenan, the mice are anaesthetized by i.p. injection of 0.5mg/kg of medetomidine and 75 mg/kg of ketamine. The mice receive a 30 L i.d. injection of carrageenan(1.5%, dissolved in norma

15、l saline) in one hind paw. The contralateral paw receive 30 L of saline and it isused as a control. Paw volume is measured before and 3 h after the carrageenan injection with aplethysmometer. Oedema is expressed as a change in paw volume over time.MCE has not independently confirmed the accuracy of

16、these methods. They are for reference only.户使本产品发表的科研献 Front Pharmacol. 2018 Mar 9;9:200. Psychopharmacology (Berl). 2018 Aug;235(8):2377-2385.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. MacKenzie SJ, et al. Action of rolipram on specific PDE4 cAMP phosphodiesterase isoform

17、s and on the phosphorylation of cAMP-response-element-binding protein (CREB) and p38 mitogen-activated protein (MAP) kinase in U937 monocyticcells. Biochem J. 2000 Apr2. Korhonen R, et al. Attenuation of TNF production and experimentally induced inflammation by PDE4 inhibitor rolipram is mediated byMAPK phosphatase-1. Br J Pharmacol. 2013 Aug;169(7):1525-36.3. Shalaby AM, et al. Effect of rolipram, a phosphodiesterase enzyme type-4 inhibitor, on -amino butyric acid content of the frontal cortexin mice exposed to