GW 4869

Name: GW 4869
Brand: Tocris Bioscience
SKU: 6741

Tocris Bioscience, part of Bio-Techne | Catalog # 6741

Citations (6)

COA / SDS

Selective neutral sphingomyelin phosphodiesterase (N-SMase) inhibitor

Key Product Details

Description:	Selective neutral sphingomyelin phosphodiesterase (N-SMase) inhibitor
Chemical Name:	3,3'-(1,4-Phenylene)bis[N-[4-(4,5-dihydro-1H-imidazol-2-yl)phenyl]-2-propenamide] ditrifluoroacetate
Purity:	≥90% (HPLC)
Molecular Weight:	732.64

View Full Technical Details for GW 4869

Technical Data
Citations

Biological Activity for GW 4869

GW 4869 is a 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.

Technical Data for GW 4869

M. Wt	732.64
Formula	C₃₀H₂₈N₆O₂.2CF₃COOH
Storage	Store at -20°C
Purity	≥90% (HPLC)
InChi Key	OVUGNZQTDFNYTB-CLEIDKRQSA-N
Smiles	O=C(/C=C/C1=CC=C(C=C1)/C=C/C(NC2=CC=C(C3=NCCN3)C=C2)=O)NC4=CC=C(C5=NCCN5)C=C4.OC(C(F)(F)F)=O.OC(C(F)(F)F)=O

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.

Solubility for GW 4869

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	1.47	2

Preparing Stock Solutions for GW 4869

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

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References for GW 4869

References are publications that support the biological activity of the product.

Lallemand NSMase2 (type 2-neutral sphingomyelinase) deficiency or inhibition by GW4869 reduces inflammation and atherosclerosis in apoe -/- mice. Arterioscler.Thromb.Vasc.Biol. 2018 PMID: 29794115
Tabatadze Inhibition of neutral sphingomyelinase-2 perturbs brain sphingolipid balance and spatial memory in mice. J.Neurosci.Res. 2010 PMID: 20629193
Figuera-Losada Cambinol, a novel inhibitor of neutral sphingomyelinase 2 shows neuroprotective properties. PLoS One 2015 PMID: 26010541
Essandoh Blockade of exosome generation with GW4869 dampens the sepsis-induced inflammation and cardiac dysfunction. Biochim.Biophys.Acta 2015 PMID: 26300484