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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-nAChR-4BP-TQS
4BP-TQS

Chemical Structure : 4BP-TQS

CAS No.: 360791-49-7

4BP-TQS (GAT107 racemic)

货号: PC-38475Not For Human Use, Lab Use Only.

4BP-TQS (GAT107 racemic) is a potent, selective, allosteric agonist of α7 nAChRs with EC50 of 17 uM, no activity for α1β1δε-, α3β4-, and α4β2 subunit-containing nAChRs at 100 uM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

4BP-TQS (GAT107 racemic) is a potent, selective, allosteric agonist of α7 nAChRs with EC50 of 17 uM, no activity for α1β1δε-, α3β4-, and α4β2 subunit-containing nAChRs at 100 uM.
Metyllycaconitine is a noncompetitive antagonist of 4BP-TQS.
Mutation of an amino acid (M253L), located in a transmembrane cavity, completely blocks agonist activation by 4BP-TQS.
4BP-TQS acts as potentiator of acetylcholine responses, facilitates recovery of α7 nAChRs from desensitization.

物理化学性质&存储条件

分子量 405.310
分子式 C18H17BrN2O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-(4-bromophenyl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide

参考文献

1. Thakur GA, et al. J Med Chem. 2013 Nov 14;56(21):8943-7.

2. Pałczyńska MM, et al. Mol Pharmacol. 2012 Nov;82(5):910-7.

3. Gill JK, et al. Proc Natl Acad Sci U S A. 2011 Apr 5;108(14):5867-72.

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