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
C21H28IN3O
98% HPLC
NMR: (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
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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