[CAS NO. 869998-49-2] SPD304
PRODUCTS SPECIFICATIONS [869998-49-2]
DESCRIPTION [869998-49-2]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 547.61 |
| Molecular Formula | C32H32F3N3O2 |
| 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 |
4 Publications Citing Use of MCE
Summary
SPD304 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 IC 50 of 22 µM for inhibiting in vitro TNF receptor 1 (TNFR1) binding to TNF-α [1] [2] .
IC50 & Target
IC50: 22 µM (TNFα) [1] .
In Vitro
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
SPD304 cannot be used in vivo due to its high toxicity [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 25 mg/mL ( 45.65 mM ; Need ultrasonic)
H 2 O : 20 mg/mL ( 36.52 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.8261 mL | 9.1306 mL | 18.2612 mL |
| 5 mM | 0.3652 mL | 1.8261 mL | 3.6522 mL |
| 10 mM | 0.1826 mL | 0.9131 mL | 1.8261 mL |
References
- [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.