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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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| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| 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. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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