SPD304

A small-molecule inhibitor of TNFα activity

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库存: 现货

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数量
1mg

￥687.00

550.00

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5mg

￥1525.00

1220.00

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10mg

￥2375.00

1900.00

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25mg

￥4862.00

3890.00

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50mg

￥7800.00

6240.00

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货号: ajce50508
CAS: 869998-49-2
别名:
分子式: C32H32F3N3O2
分子量: 547.61
纯度: >98%
溶解度: DMSO : 25 mg/mL (45.65 mM) Water : 20 mg/mL (36.52 mM)
储存: Store at -20°C
库存: 现货

Background

Tumor necrosis factor α (TNFα) is a primary mediator of many inflammatory conditions including rheumatoid arthritis, toxic shock, and sepsis.^1,2,3 TNFα functions as a trimer and promotes receptor trimerization to activate proinflammatory and/or apoptotic signalling pathways. ^4,5 SPD-304 is an inhibitor of tumor necrosis factor α (TNFα). that prevents binding to the TNF Receptor 1 (TNFR1) with an IC₅₀ of 22 ?M.⁶ It binds to the biologically active TNFα trimer and promotes accelerated displacement of a single subunit to rapidly inactivate the cytokine. In a cell based assay, SPD-304 inhibited TNFα-mediated stimulation of IKB degradation with an IC₅₀ of 4.6 ?M.⁶

1.Beutler, B., Greenwald, D., Hulmes, J.D., et al.Identity of tumor necrosis factor and the macrophage-secreted factor cachectinNature316552-554(1985) 2.Tracey, K.J., Beutler, B., Lowry, S.F., et al.Shock and tissue injury induced by recombinant human cachectinScience234470-474(1986) 3.Bidgood, M.J., Jamal, O.S., Cunningham, A.M., et al.Type IIA secretory phospholipase A2 up-regulates cyclooxygenase-2 and amplifies cytokine-mediated prostaglandin production in human rheumatoid synoviocytesJ. Immunol.1652790-2797(2000) 4.Thornberry, N.A., and Lazebnik, Y.Caspases: Enemies withinScience281(5381)1312-1316(1998) 5.Wallach, D., Varfolomeev, E.E., Malinin, N.L., et al.Tumor necrosis factor receptor and Fas signaling mechanismsAnnu. Rev. Immunol.17133-167(1999) 6.He, M.M., Smith, A.S., Oslob, J.D., et al.Small-molecule inhibition of TNF-αScience3101022-1025(2005)