5-BDBD - CAS 768404-03-1
Category: Inhibitor
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Molecular Weight:
5-BDBD is a potent P2X4 receptor antagonist. It was shown to block P2X4-mediated currents in Chinese hamster ovary cells (IC50 = 0.50 μM).
Brife Description:
P2X4 receptor antagonist
≥99% by HPLC
Canonical SMILES:
1.A high concentration of fatty acids induces TNF-α as well as NO release mediated by the P2X4 receptor, and the protective effects of puerarin in RAW264.7 cells.
Tu YM;Gong CX;Ding L;Liu XZ;Li T;Hu FF;Wang S;Xiong CP;Liang SD;Xu H Food Funct. 2017 Dec 13;8(12):4336-4346. doi: 10.1039/c7fo00544j.
Circulating levels of free fatty acids (FFAs) are often found to be increased in patients with type 2 diabetes mellitus (T2DM) and metabolic syndrome (MS). High plasma FFA levels may give rise to maladaptive macrophage activation and promote inflammatory responses, which has been proposed as a potential mechanism for the development of DM and MS. P2X4 receptor (P2X4R), a ligand-gated cation channel activated by extracellular adenosine triphosphate (ATP), plays a primary role in the regulation of inflammatory responses. Puerarin has been reported to possess potential anti-inflammatory activity. However, the anti-inflammatory activity of puerarin and the underlying molecular mechanisms in a setting of a high concentration of FFAs remain unknown. In this study, we found that a high concentration of FFAs increased the expression of P2X4R, cytosolic Ca;2+; concentration and the phosphorylation of extracellular signal-regulated kinase (ERK) and induced the expression of tumor necrosis factor (TNF)-α and inducible nitric oxide synthase (iNOS) mRNA and the release of TNF-α and nitric oxide (NO) in RAW264.7 macrophages. Such a high concentration FFA-induced inflammation may be reversed by the P2X4R selective antagonist 5-BDBD, which manifests the important role of P2X4R in the TNF-α and NO release caused by the high concentration of FFAs in RAW264.
2.Pharmacological characterization of the P2 receptors profile in the podocytes of the freshly isolated rat glomeruli.
Ilatovskaya DV;Palygin O;Levchenko V;Staruschenko A Am J Physiol Cell Physiol. 2013 Nov 15;305(10):C1050-9. doi: 10.1152/ajpcell.00138.2013. Epub 2013 Sep 18.
Calcium flux in the podocytes is critical for normal and pathophysiological regulation of these types of cells, and excessive calcium signaling results in podocytes damage and improper glomeruli function. Purinergic activation of P2 receptors is a powerful and rapid signaling process; however, the exact physiological identity of P2 receptors subtypes in podocytes remains essentially unknown. The goal of this study was to determine the P2 receptor profile in podocytes of the intact Sprague-Dawley rat glomeruli using available pharmacological tools. Glomeruli were isolated by differential sieving and loaded with Fluo-4/Fura Red cell permeable calcium indicators, and the purinergic response in the podocytes was analyzed with ratiometric confocal fluorescence measurements. Various P2 receptors activators were tested and compared with the effect of ATP, specifically, UDP, MRS 2365, bzATP, αβ-methylene, 2-meSADP, MRS 4062, and MRS 2768, were analyzed. Antagonists (MRS 2500, 5-BDBD, A438079, and NF 449) were tested when 10 μM ATP was applied as the EC50 for ATP activation of the calcium influx in the podocytes was determined to be 10.7 ± 1.5 μM. Several agonists including MRS 2365 and 2-meSADP caused calcium flux.
3.Podocyte Purinergic P2X4 Channels Are Mechanotransducers That Mediate Cytoskeletal Disorganization.
Forst AL;Olteanu VS;Mollet G;Wlodkowski T;Schaefer F;Dietrich A;Reiser J;Gudermann T;Mederos y Schnitzler M;Storch U J Am Soc Nephrol. 2016 Mar;27(3):848-62. doi: 10.1681/ASN.2014111144. Epub 2015 Jul 9.
Podocytes are specialized, highly differentiated epithelial cells in the kidney glomerulus that are exposed to glomerular capillary pressure and possible increases in mechanical load. The proteins sensing mechanical forces in podocytes are unconfirmed, but the classic transient receptor potential channel 6 (TRPC6) interacting with the MEC-2 homolog podocin may form a mechanosensitive ion channel complex in podocytes. Here, we observed that podocytes respond to mechanical stimulation with increased intracellular calcium concentrations and increased inward cation currents. However, TRPC6-deficient podocytes responded in a manner similar to that of control podocytes, and mechanically induced currents were unaffected by genetic inactivation of TRPC1/3/6 or administration of the broad-range TRPC blocker SKF-96365. Instead, mechanically induced currents were significantly decreased by the specific P2X purinoceptor 4 (P2X4) blocker 5-BDBD. Moreover, mechanical P2X4 channel activation depended on cholesterol and podocin and was inhibited by stabilization of the actin cytoskeleton. Because P2X4 channels are not intrinsically mechanosensitive, we investigated whether podocytes release ATP upon mechanical stimulation using a fluorometric approach.
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CAS 768404-03-1 5-BDBD

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