BRL 50481 - CAS 433695-36-4
Catalog number: 433695-36-4
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
Phosphodiesterase (PDE)
BRL 50481 is a potent, selective substrate-competitive inhibitor of phosphodiesterase (PDE) 7 (Ki = 180 nM).
Off-White Solid
BRL-50481; BRL 50481; BRL50481. 3-(N,N-Dimethylsulfonamido)-4-methylnitrobenzene, 5-Nitro-2-N,N-trimethylbenzenesulfonamide;
Soluble in DMSO
Store at -20 °C
A PDE7 inhibitor that has acceptable selectivity for in vivo studies.
Quality Standard:
Enterprise standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly.
Melting Point:
72-74 °C
Canonical SMILES:
1.Characterization of renal ecto-phosphodiesterase.
Jackson EK;Ren J;Zacharia LC;Mi Z J Pharmacol Exp Ther. 2007 May;321(2):810-5. Epub 2007 Feb 16.
In kidneys, stimulation of adenylyl cyclase causes egress of cAMP, conversion of cAMP to AMP by ecto-phosphodiesterase, and metabolism of AMP to adenosine by ecto-5'-nucleotidase. Although much is known about ecto-5'-nucleotidase, the renal ecto-phosphodiesterase remains uncharacterized. We administered cAMP (10 microM in the perfusate) to 12 different groups of perfused kidneys. AMP was measured in perfusate using ion trap mass spectrometry. In control kidneys (n=19), basal renal secretion rate of AMP was 0.49+/-0.08 and increased to 3.0+/-0.2 nmol AMP/g kidney weight/min during administration of cAMP. A broad-spectrum phosphodiesterase (PDE) inhibitor (1,3-isobutyl-1-methylxanthine, 300 microM, n=6) and an ecto-phosphodiesterase inhibitor (1,3-dipropyl-8-p-sulfophenylxanthine, 1 mM, n=6) significantly attenuated cAMP-induced AMP secretion by 60 and 74%, respectively. Blockade of PDE1 (8-methoxymethyl-3-isobutyl-1-methylxanthine, 100 microM), PDE2 [erythro-9-(2-hydroxy-3-nonyl)adenine, 30 microM], PDE3 (milrinone, 10 microM; cGMP, 10 microM), PDE4 (Ro 20-1724 [4-(3-butoxy-4-methoxybenzyl)imidazolidin-2-one], 100 microM), PDE5 and PDE6 (zaprinast, 30 microM), and PDE7 [BRL-50481 (5-nitro-2,N,N-trimethylbenzenesulfonamide), 10 microM] did not alter renal ecto-phosphodiesterase activity.
2.β-Adrenergic cAMP signals are predominantly regulated by phosphodiesterase type 4 in cultured adult rat aortic smooth muscle cells.
Zhai K;Hubert F;Nicolas V;Ji G;Fischmeister R;Leblais V PLoS One. 2012;7(10):e47826. doi: 10.1371/journal.pone.0047826. Epub 2012 Oct 18.
BACKGROUND: ;We investigated the role of cyclic nucleotide phosphodiesterases (PDEs) in the spatiotemporal control of intracellular cAMP concentrations in rat aortic smooth muscle cells (RASMCs).;METHODOLOGY/PRINCIPAL FINDINGS: ;The rank order of PDE families contributing to global cAMP-PDE activity was PDE4> PDE3  =  PDE1. PDE7 mRNA expression but not activity was confirmed. The Fluorescence Resonance Energy Transfer (FRET)-based cAMP sensor, Epac1-camps, was used to monitor the time course of cytosolic cAMP changes. A pulse application of the β-adrenoceptor (β-AR) agonist isoproterenol (Iso) induced a transient FRET signal. Both β(1)- and β(2)-AR antagonists decreased the signal amplitude without affecting its kinetics. The non-selective PDE inhibitor (IBMX) dramatically increased the amplitude and delayed the recovery phase of Iso response, in agreement with a role of PDEs in degrading cAMP produced by Iso. Whereas PDE1, PDE3 and PDE7 blockades [with MIMX, cilostamide (Cil) and BRL 50481 (BRL), respectively] had no or minor effect on Iso response, PDE4 inhibition [with Ro-20-1724 (Ro)] strongly increased its amplitude and delayed its recovery. When Ro was applied concomitantly with MIMX or Cil (but not with BRL), the Iso response was drastically further prolonged.
3.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.
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