Axon 2694
CAS [360791-49-7]
MF C18H17BrN2O2SMW 405.31
4BP-TQS is an allosteric agonist of α7 nicotinic acetylcholine receptors (nAChR). The agonism was shown to act through a site topographically distinct from the ACh site. 4BP-TQS was a more potent and efficacious agonist of α7 nAChR than ACh (8-fold lower EC50 and 45-fold larger maximal response).
The bioactive enantiomer of 4BP-TQS, GAT107 (Axon 2621), is also available.
KEYWORDS: 4BP-TQS | supplier | α7 nAChR allosteric agonist | 4BPTQS | 4-BPTQS | 4-BP-TQS | CAS [360791-49-7] | Acetylcholine | nAChR | Allosteric agonist | Ion Channels | CAS [1476053-27-6]
JK Gill et al. Agonist activation of alpha7 nicotinic acetylcholine receptors via an allosteric transmembrane site. Proc Natl Acad Sci USA. 2011 Apr 5;108(14):5867-72. |
RL Papke. The activity of GAT107, an allosteric activator and positive modulator of α7 nicotinic acetylcholine receptors (nAChR), is regulated by aromatic amino acids that span the subunit interface. J Biol Chem. 2014 Feb 14;289(7):4515-31. |
4-(4-Bromophenyl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide
[360791-49-7]
Axon Medchem的业务之一,是独有的Axon Ligands配体库,在世界范围内,被认为是药物研发的标准。这其中,针对850余种生物靶标(包括细胞信号、基因转录、凋亡、细胞周期调控、CNS等),Axon Medchem拥有多达2000余种小分子抑制剂或调节剂。除了配体库,Axon Medchem还是欧洲著名的CRO公司,主要针对生物活性分子和药物类似分子展开合成及协议开发工作,在过去的10年中,Axon Medchem已经发现了多种潜在药物分子,并在生物医药界享有一定的声誉。