CAS NO: | 869998-49-2 |
包装: | 1mg |
市场价: | 1607元 |
Cas No. | 869998-49-2 |
Canonical SMILES | O=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 tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation 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. |