SPD304是肿瘤坏死因子α (TNFα)的选择性抑制剂,能够促进肿瘤坏死因子三聚体的分离,从而阻断其与受体间的相互作用,其体外抑制肿瘤坏死因子α和受体1间结合的IC50值为22µM。SPD304毒性高,不能用于体内。
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CAS No. : 869998-49-2
分子量:547.61
分子式:C₃₂H₃₂F₃N₃O₂
CAS No.:869998-49-2
纯度: >99.0%
描述:SPD304是肿瘤坏死因子α(TNFα)的选择性抑制剂,可促进TNF三聚体的解离,从而阻断TNF及其受体的相互作用,IC50为22μM,可抑制体外TNF受体1(TNFR1)的结合。TNF-α[1][2]。SPD304由于其高毒性而不能在体内使用[3]。
IC50 & Target:IC50: 22 µM (TNFα)[1].
体外:SPD304(2μM)显着挽救了aHSCs的存活率,减少了脂质氢氧化物的产生,并增加了细胞内GSH。与单独的GA相比,GA(75μM)和SPD304(2μM)的共同处理使TRADD下调几乎2倍(w / o抑制剂对w /抑制剂)和p-RIP3 1.4倍,并促进caspase 8激活[4]。
相关文献:
[1]. Molly M. He, et al. Small-Molecule Inhibition of TNF-α. Science 11 Nov2005.
[2]. Alexiou P, et al. Rationally designed less toxic SPD-304 analogs andpreliminary evaluation of their TNF inhibitory effects. Arch Pharm (Weinheim).2014 Nov;347(11):798-805.
[3]. Mouhsine H, et al. Identification of an in vivo orally activedual-binding protein-protein interaction inhibitor targeting TNFα throughcombined in silico/in vitro/in vivo screening. Sci Rep. 2017 Jun13;7(1):3424.
[4]. Gallic acid induces necroptosis via TNF-α signaling pathway inactivated hepatic stellate cells. Chang YJ, et al. PLoS One. 2015 Mar27;10(3):e0120713.
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