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Submit ReviewGW 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.
分子量 | 732.64 |
公式 | C30H28N6O2.2CF3COOH |
储存 | Store at -20°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 1.47 | 2 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for GW 4869, please let us know.
关键词: 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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