Bay 60-7550 - CAS 439083-90-6
Catalog number: 439083-90-6
Category: Inhibitor
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Molecular Formula:
C27H32N4O4
Molecular Weight:
476.57
COA:
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Targets:
Phosphodiesterase (PDE)
Description:
Bay 60-7550 is a potent PDE2 inhibitor. It is 50-fold more selective for PDE2 compared to PDE1 and greater than 100-fold selective compared to PDE5 PDE3B, PDE4B, PDE7B, PDE8A, PDE9A, PDE10A, and PDE11A.
Purity:
>98%
Synonyms:
BAY60-7550; BAY 60-7550; BAY-60-7550; BAY-607550; BAY 607550; BAY607550.
MSDS:
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InChIKey:
MYTWFJKBZGMYCS-NQIIRXRSSA-N
InChI:
InChI=1S/C27H32N4O4/c1-17-25-27(33)29-24(16-20-13-14-22(34-3)23(15-20)35-4)30-31(25)26(28-17)21(18(2)32)12-8-11-19-9-6-5-7-10-19/h5-7,9-10,13-15,18,21,32H,8,11-12,16H2,1-4H3,(H,29,30,33)/t18-,21+/m1/s1
Canonical SMILES:
CC1=C2C(=O)N=C(NN2C(=N1)C(CCCC3=CC=CC=C3)C(C)O)CC4=CC(=C(C=C4)OC)OC
1.A novel PDE2A reporter cell line: characterization of the cellular activity of PDE inhibitors.
Wunder F;Gnoth MJ;Geerts A;Barufe D Mol Pharm. 2009 Jan-Feb;6(1):326-36. doi: 10.1021/mp800127n.
We report here the generation and pharmacological characterization of a phosphodiesterase 2A (PDE2A) reporter cell line. Human PDE2A was stably transfected in a parental cell line expressing the atrial natriuretic peptide (ANP) receptor and the cyclic nucleotide-gated (CNG) cation channel CNGA2, acting as the biosensor for intracellular cGMP. In this reporter cell line, cGMP levels can be monitored in real-time via aequorin luminescence stimulated by calcium influx through the CNG channel. By using different PDE inhibitors, we could show that our PDE2A reporter assay specifically monitors PDE2A inhibition with high sensitivity. In the absence of ANP stimulation, the PDE2A selective inhibitors EHNA, BAY 60-7550 and PDP did not increase basal luminescence levels in this experimental setting. However, in combination with ANP, these inhibitors stimulated luminescence signals and induced leftward shifts of ANP concentration-response curves. Similar results were obtained when using IBMX, trequinsin and dipyridamole, which inhibit PDE2A nonselectively with lower potency. PDP, the most potent PDE2A inhibitor known to date, was found to exhibit much lower cellular activity as anticipated from its biochemical PDE2A inhibitory activity.
2.In vivo selective binding of (R)-[11C]rolipram to phosphodiesterase-4 provides the basis for studying intracellular cAMP signaling in the myocardium and other peripheral tissues.
Kenk M;Greene M;Thackeray J;deKemp RA;Lortie M;Thorn S;Beanlands RS;DaSilva JN Nucl Med Biol. 2007 Jan;34(1):71-7. Epub 2006 Nov 16.
INTRODUCTION: ;Phosphodiesterase-4 (PDE4) enzymes specifically break down the second messenger cAMP, thereby terminating the intracellular signaling cascade that plays an essential role in neurohormonal modulation of many physiological systems. PDE4 activity and expression are regulated by cAMP levels, suggesting that measurement of PDE4 provides an index of intracellular cAMP signaling.;METHODS: ;Male Sprague-Dawley rats were administered (R)- or the less active enantiomer (S)-[11C]rolipram and sacrificed 30 min later with tracer retention measured in various tissues. Co-injections with saturating doses of unlabeled (R)-rolipram, (S)-rolipram and Ro 20-1724, as well as subtype-selective PDE inhibitors vinpocetine, Bay 60-7550, cilostazol and zaprinast were used to establish binding selectivity for PDE4 over PDE1, PDE2, PDE3 and PDE5 subtypes, respectively. Autoradiography was performed to substantiate results of biodistribution studies in the myocardium.;RESULTS: ;In vivo (R)-[11C]rolipram retention was dose-dependently reduced by co-injections of (R)-rolipram and (S)-rolipram (ED50 values of 0.03 mg/kg and 0.2 mg/kg, respectively). Vinpocetine, Bay 60-7550, cilostazol and zaprinast had no effect on (R)-[11C]rolipram binding, while (R)-rolipram and Ro 20-1724 reduced the tracer uptake to nonspecific levels in PDE4-rich tissues.
3.Selective blockade of phosphodiesterase types 2, 5 and 9 results in cyclic 3'5' guanosine monophosphate accumulation in retinal pigment epithelium cells.
Diederen RM;La Heij EC;Markerink-van Ittersum M;Kijlstra A;Hendrikse F;de Vente J Br J Ophthalmol. 2007 Mar;91(3):379-84. Epub 2006 Aug 30.
AIM: ;To investigate which phosphodiesterase (PDE) is involved in regulating cyclic 3'5' guanosine monophosphate breakdown in retinal pigment epithelium (RPE) cells.;METHODS: ;cGMP content in the cultured RPE cells (D407 cell line) was evaluated by immunocytochemistry in the presence of non-selective or isoform-selective PDE inhibitors in combination with the particulate guanylyl cyclase stimulator atrial natriuretic peptide (ANP) or the soluble guanylyl cyclase stimulator sodium nitroprusside (SNP). mRNA expression of PDE2, PDE5 and PDE9 was studied in cultured human RPE cells and rat RPE cell layers using non-radioactive in situ hybridisation.;RESULTS: ;In the absence of PDE inhibitors, cGMP levels in cultured RPE cells are very low. cGMP accumulation was readily detected in cultured human RPE cells after incubation with Bay60-7550 as a selective PDE2 inhibitor, sildenafil as a selective PDE5 inhibitor or Sch51866 as a selective PDE9 inhibitor. In the presence of PDE inhibition, cGMP content increased markedly after stimulation of the particulate guanylyl cyclase. mRNA of PDE2,PDE5 and PDE9 was detected in all cultured human RPE cells and also in rat RPE cell layers.;CONCLUSIONS: ;PDE2, PDE5 and PDE9 have a role in cGMP metabolism in RPE cells.
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CAS 439083-90-6 Bay 60-7550

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