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GSK-1482160
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GSK-1482160
Catalog No. T61025Cas No. 1001389-72-5
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.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose. | Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 5 mg | $48 | In Stock | |
| 10 mg | $76 | In Stock | |
| 25 mg | $157 | In Stock | |
| 50 mg | $277 | In Stock | |
| 100 mg | $397 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $53 | In Stock |
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| 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 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 90.0 mg/mL (268.9 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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