SPD304 dihydrochloride 

SPD304 dihydrochloride is a selective TNF-α inhibitor, which promotes dissociation of TNF trimers and therefore blocks the interaction of TNF and its receptor. SPD304 has an IC₅₀ of 22 µM for inhibiting in vitro TNF receptor 1 (TNFR1) binding to TNF-α^[1][2].

IC50: 22 µM (TNFα)^[1].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SPD304 cannot be used in vivo due to its high toxicity^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

620.53

C₃₂H₃₄Cl₂F₃N₃O₂

1049741-03-8

Solid

White to off-white

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.[H]Cl.[H]Cl

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]