SPD304 dihydrochloride

Modify Date: 2024-01-30 17:45:11

SPD304 dihydrochloride Structure
SPD304 dihydrochloride structure
Common Name SPD304 dihydrochloride
CAS Number 1049741-03-8 Molecular Weight 620.532
Density N/A Boiling Point N/A
Molecular Formula C32H34Cl2F3N3O2 Melting Point N/A
MSDS Chinese USA Flash Point N/A

 Use of 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].

 Names

Name TNF-α Inhibitor
Synonym More Synonyms

 SPD304 dihydrochloride Biological Activity

Description 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].
Related Catalog
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].
In Vivo SPD304 cannot be used in vivo due to its high toxicity[3].
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.

 Chemical & Physical Properties

Molecular Formula C32H34Cl2F3N3O2
Molecular Weight 620.532
Exact Mass 619.197998
Appearance of Characters white Solid
Storage condition Store at -20° C
Water Solubility Soluble in DMSO (10 mg/ml).

 Safety Information

Hazard Codes Xi

 Synonyms

4H-1-Benzopyran-4-one, 6,7-dimethyl-3-[[methyl[2-[methyl[[1-[3-(trifluoromethyl)phenyl]-1H-indol-3-yl]methyl]amino]ethyl]amino]methyl]-, hydrochloride (1:2)
SPD00000304
MFCD09265259
6,7-Dimethyl-3-[(methyl{2-[methyl({1-[3-(trifluoromethyl)phenyl]-1H-indol-3-yl}methyl)amino]ethyl}amino)methyl]-4H-chromen-4-one dihydrochloride
SPD304
6,7-Dimethyl-3-[[methyl[2-[methyl[[1-[3-(trifluoromethyl)phenyl]-1H-indol-3-yl]methyl]amino]ethyl]amino]methyl]-(4H-1-Benzopyran-4-one dihydrochloride