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GW 4869 New
Selective neutral sphingomyelin phosphodiesterase (N-SMase) inhibitor (IC50 = 1 μM). Exhibits selectivity for neutral sphingomyelinase over acid sphingomyelinase (a-SMase) at concentrations up to 150 μM as well as B. cereus PC-PLC, human lyso-PAF PLC, and bovine PP2A at 10 μM. Blocks exosome biogenesis. Inhibits TNF-α-induced sphingomyelin hydrolysis and TNF-α-induced cell death in MCF-7 cells. Reverses hypoxia-induced pulmonary vasoconstriction in rats. Neuroprotective.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 732.64. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.02 mM||68.25 mL||341.23 mL||682.46 mL|
|0.1 mM||13.65 mL||68.25 mL||136.49 mL|
|0.2 mM||6.82 mL||34.12 mL||68.25 mL|
|1 mM||1.36 mL||6.82 mL||13.65 mL|
References are publications that support the biological activity of the product.
Essandoh et al (2015) Blockade of exosome generation with GW4869 dampens the sepsis-induced inflammation and cardiac dysfunction. Biochim.Biophys.Acta 1852 2362 PMID: 26300484
Tabatadze et al (2010) Inhibition of neutral sphingomyelinase-2 perturbs brain sphingolipid balance and spatial memory in mice. J.Neurosci.Res. 88 2940 PMID: 20629193
Figuera-Losada et al (2015) Cambinol, a novel inhibitor of neutral sphingomyelinase 2 shows neuroprotective properties. PLoS One 10 e0124481 PMID: 26010541
Lallemand et al (2018) NSMase2 (type 2-neutral sphingomyelinase) deficiency or inhibition by GW4869 reduces inflammation and atherosclerosis in apoe -/- mice. Arterioscler.Thromb.Vasc.Biol. 38 1479 PMID: 29794115
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Keywords: GW 4869, GW 4869 supplier, 6823-69-4, GW4869, N-SMase, neutral, sphingomyelinase, inhibitors, inhibits, potent, cell, permeable, sphyngomyelin, phosphodiesterase, 2, selective, Other, Hydrolases, 6741, Tocris Bioscience
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