For research use only. Not for therapeutic Use.
GSK1370319A is a potent P2X7 antagonist (IC50 = 3.2 nM). GSK1370319A inhibits ATP-induced increase in IL-1β release and caspase 1 activation in lipopolysaccharide (LPS)-primed mixed glia by blocking assembly of the inflammasome in a pannexin 1-dependent manner. GSK1370319A also inhibits ATP-induced subregion-specific neuronal loss in hippocampal organotypic slice cultures, which is dependent on its ability to prevent inflammasome assembly in glia. Significantly, GSK1370319A attenuates age-related deficits in long-term potentiation (LTP) and inhibits the accompanying age-related caspase 1 activity. We conclude that inhibiting P2X(7) receptor-activated NLRP3 inflammasome formation and the consequent IL-1β release from glia preserve neuronal viability and synaptic activity.
| Catalog Number | I028316 |
| CAS Number | 1001389-31-6 |
| Synonyms | GSK1370319A; GSK-1370319A; GSK 1370319A; GSK1370319; GSK-1370319; GSK 1370319; |
| Molecular Formula | C13H14Cl2N2O2 |
| Purity | 98% |
| Solubility | Soluble in DMSO |
| Appearance | Solid powder |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| IUPAC Name | (2S)-N-[(2,4-Dichlorophenyl)methyl]-1-methyl-5-oxo-2-pyrrolidinecarboxamide |
| InChI | InChI=1S/C13H14Cl2N2O2/c1-17-11(4-5-12(17)18)13(19)16-7-8-2-3-9(14)6-10(8)15/h2-3,6,11H,4-5,7H2,1H3,(H,16,19)/t11-/m0/s1 |
| InChIKey | YMNOJCVLDDTECB-NSHDSACASA-N |
| SMILES | ClC1=CC=C(C(Cl)=C1)CNC([C@H]2N(C(CC2)=O)C)=O |
| Reference | 1: Homerin G, Jawhara S, Dezitter X, Baudelet D, Dufrénoy P, Rigo B, Millet R, |
