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SPD304
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SPD304图片
CAS NO:869998-49-2
包装:1mg
市场价:1607元

产品介绍
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。
Cas No.869998-49-2
Canonical SMILESO=C1C(CN(C)CCN(C)CC2=CN(C3=CC=CC(C(F)(F)F)=C3)C4=C2C=CC=C4)=COC5=CC(C)=C(C)C=C15
分子式C32H32F3N3O2
分子量547.61
溶解度DMSO : 25 mg/mL (45.65 mM) Water : 20 mg/mL (36.52 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

SPD304 is a selective inhibitor of tumor necrosis factor α (TNFα) and promotes dissociation of TNF trimers and therefore blocks the interaction of TNF and its receptor, with an IC50 of 22 µM for inhibiting in vitro TNF receptor 1 (TNFR1) binding to TNF-α[1][2]. SPD304 cannot be used in vivo due to its high toxicity[3].

SPD304 (2 μM) significantly rescues the survivability of aHSCs, reduces the production of lipid hydroxides, and increased intracellular GSH. The co-treatment of GA (75 μM) and SPD304 (2 μM), down-regulate TRADD almost 2-fold (w/o inhibitor vs. w/ inhibitor) and p-RIP3 1.4-fold compared to GA alone, and promotes caspase 8 activation[4].

[1]. Molly M. He, et al. Small-Molecule Inhibition of TNF-α. Science 11 Nov 2005. [2]. Alexiou P, et al. Rationally designed less toxic SPD-304 analogs and preliminary 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 active dual-binding protein-protein interaction inhibitor targeting TNFα through combined in silico/in vitro/in vivo screening. Sci Rep. 2017 Jun 13;7(1):3424. [4]. Gallic acid induces necroptosis via TNF-α signaling pathway in activated hepatic stellate cells. Chang YJ, et al. PLoS One. 2015 Mar 27;10(3):e0120713.