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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-nAChR-A-867744
A-867744

Chemical Structure : A-867744

CAS No.: 1000279-69-5

A-867744 (A 867744;A867744)

货号: PC-42900Not For Human Use, Lab Use Only.

A-867744 is a potent, selective α7 nAChR positive allosteric modulator (PAM) with Ki of 23 nM, potentiates acetylcholine (ACh)-evoked currents with EC50 of 1 uM.

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

生物&药学活性

A-867744 is a potent, selective α7 nAChR positive allosteric modulator (PAM) with Ki of 23 nM, potentiates acetylcholine (ACh)-evoked currents with EC50 of 1 uM; A-867744 failed to potentiate responses mediated by 5-HT3A or α3β4 and α4β2 nAChRs; increases choline-evoked α7 currents and recovery from inhibition/desensitization, and enhances spontaneous inhibitory postsynaptic current activity at 10 uM in rat hippocampus; normalizes gating deficits in rodent model of sensory gating.

物理化学性质&存储条件

分子量 402.8945
分子式 C20H19ClN2O3S
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

Benzenesulfonamide, 4-[5-(4-chlorophenyl)-2-methyl-3-(1-oxopropyl)-1H-pyrrol-1-yl]-

参考文献

1. Malysz J, et al. J Pharmacol Exp Ther. 2009 Jul;330(1):257-67.

2. Faghih R, et al. J Med Chem. 2009 May 28;52(10):3377-84.

3. Hu M, et al. Br J Pharmacol. 2009 Dec;158(8):1857-64.

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