Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK-1482160 is a CNS-penetrant negative allosteric modulator of P2X7 receptor with oral activity. The P2X7 receptor is involved in the production of pro-inflammatory cytokines by central and peripheral immune cells, so GSK-1482160 has the potential to study inflammatory diseases. GSK-1482160 shows excellent in vitro potency (in functional and electrophysiological assays at recombinant and naive P2X7 receptors across multiple species including humans) and cross-target selectivity.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 34.00 | |
5 mg | In stock | $ 80.00 | |
10 mg | In stock | $ 128.00 | |
25 mg | In stock | $ 263.00 | |
50 mg | In stock | $ 463.00 | |
100 mg | In stock | $ 683.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 89.00 |
Description | GSK-1482160 is a CNS-penetrant negative allosteric modulator of P2X7 receptor with oral activity. The P2X7 receptor is involved in the production of pro-inflammatory cytokines by central and peripheral immune cells, so GSK-1482160 has the potential to study inflammatory diseases. GSK-1482160 shows excellent in vitro potency (in functional and electrophysiological assays at recombinant and naive P2X7 receptors across multiple species including humans) and cross-target selectivity. |
In vitro | ATP-induced secretion of tau-containing exosome was significantly suppressed by GSK-1482160 treatment from primary murine microglia, but not from neurons or astrocytes [2]. |
In vivo | Oral administration of GSK-1482160 significantly reduced accumulation of MC1+ and Alz50+ misfolded tau in hippocampal regions, which was accompanied with reduced accumulation of Tsg101, an exosome marker, in hippocampal neurons. GSK-1482160 also significantly increased accumulation of Tsg101 and CD81 in microglia in vivo, suggesting its suppression of P2RX7-induced exosome secretion from microglia [2]. |
Molecular Weight | 334.72 |
Formula | C14H14ClF3N2O2 |
CAS No. | 1001389-72-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 90.0 mg/mL (268.9 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. More
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GSK-1482160 1001389-72-5 Membrane transporter/Ion channel Neuroscience P2X Receptor inhibitor inhibit