GAT2711 | α9 nAChR agonist
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $70.00 | ||
| 25 mg | $265.00 |
GAT2711 is a novel full agonist of the α9 nicotinic acetylcholine receptor (EC50 = 230 nM; EC50 for α9α10 = 990 nM). It was 340-fold selective over the α7 receptor. GAT2711 significantly and dose-dependently inhibited the BzATP-induced release of the pro-inflammatory cytokine IL-1ß in THP-1 cells (IC50 = 0.5 µM). It fully attenuated inflammatory pain in mice in an α7 nAChR-independent manner. α9 nAChR agonists represent a novel approach to treating inflammatory and/or neuropathic pain.
References/Citations:
- Andleeb et al. (2024), Explorations of Agonist Selectivity for the α9* nAChR with Novel Substituted Carbamoyl/Amido/Heteroaryl Dialkylpiperazinium Salts and Their Therapeutic Implications in Pain and Inflammation; J. Med. Chem. 67 8642
Safety Data Sheet:
Product Data Sheet:
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GAT2711 is a novel full agonist of the α9 nicotinic acetylcholine receptor (EC50 = 230 nM; EC50 for α9α10 = 990 nM). It was 340-fold selective over the α7 receptor. GAT2711 significantly and dose-dependently inhibited the BzATP-induced release of the pro-inflammatory cytokine IL-1ß in THP-1 cells (IC50 = 0.5 µM). It fully attenuated inflammatory pain in mice in an α7 nAChR-independent manner. α9 nAChR agonists represent a novel approach to treating inflammatory and/or neuropathic pain.
References/Citations:
- Andleeb et al. (2024), Explorations of Agonist Selectivity for the α9* nAChR with Novel Substituted Carbamoyl/Amido/Heteroaryl Dialkylpiperazinium Salts and Their Therapeutic Implications in Pain and Inflammation; J. Med. Chem. 67 8642
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