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GAT2711 is a full agonist of α9nAChR, with an EC50 of 230 nM. It exhibits 340 times greater selectivity for α9 over α7nAChR. In THP-1 cells, GAT2711 inhibits ATP-induced IL-1β release. Additionally, GAT2711 retains full analgesic activity in α7nAChR knockout mice.
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| Description | GAT2711 is a full agonist of α9nAChR, with an EC50 of 230 nM. It exhibits 340 times greater selectivity for α9 over α7nAChR. In THP-1 cells, GAT2711 inhibits ATP-induced IL-1β release. Additionally, GAT2711 retains full analgesic activity in α7nAChR knockout mice. |
| In vitro | GAT2711 (compound 3; LPS (1 μg/mL) pre-treatment for 5 hours, followed by co-treatment with BzATP (100 μM) for 40 minutes) significantly inhibits ATP-induced IL-1β release in THP-1 cells, with an IC50 value of 0.5 μM, demonstrating potent anti-inflammatory activity similar to acetylcholine. GAT2711 does not induce IL-1β release without ATP, indicating selective inhibition of ATP-mediated inflammatory responses. |
| In vivo | GAT2711 (2-10 mg/kg; intraperitoneal injection; single dose) effectively alleviates inflammatory pain through a mechanism that is independent of α7 nAChR. |
| Formula | C20H27IN4O |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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