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GAT107
- Optical Purity: >99%
- Soluble in DMSO
- MF: C18H17BrN2O2S
- MW: 405.31
Description
GAT107, the bioactive enantiomer of 4BP-TQS (Axon 2694), is an allosteric agonist (EC50 value 28 μM) and positive allosteric modulator (PAM) of α7 nicotinic acetylcholine receptors. GAT107 reverses nociception in mouse models of inflammatory and neuropathic pain.
More Information
| Parent CAS No. | 1476807-74-5 |
|---|---|
| Chemical Name | (3aR,4S,9bS)-4-(4-bromophenyl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide |
| SMILES | N1C2=C(C=C(S(N)(=O)=O)C=C2)[C@H]2C=CC[C@H]2[C@H]1C1=CC=C(Br)C=C1 |&1:11,15,16,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C18H17BrN2O2S/c19-12-6-4-11(5-7-12)18-15-3-1-2-14(15)16-10-13(24(20,22)23)8-9-17(16)21-18/h1-2,4-10,14-15,18,21H,3H2,(H2,20,22,23)/t14-,15+,18+/m0/s1 |
| InChiKey | YNCXHXYZTLIZTO-HDMKZQKVSA-N |
| CID | 6554040 |
| Short Description | α7 nAChR agonist and PAM |
References
- GA Thakur et al. Expeditious synthesis, enantiomeric resolution, and enantiomer functional characterization of (4-(4-bromophenyl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide (4BP-TQS).... J Med Chem. 2013 Nov 14;56(21):8943-7.
- D Bagdas. The α7 nicotinic receptor dual allosteric agonist and positive allosteric modulator GAT107 reverses nociception inmouse models of inflammatory and neuropathic pain. Br J Pharmacol. 2016 Aug;173(16):2506-20.
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