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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-nAChR-PHA-543613
PHA-543613

Chemical Structure : PHA-543613

CAS No.: 478149-53-0

PHA-543613 (PHA-543,613, PHA543613)

货号: PC-22783Not For Human Use, Lab Use Only.

PHA-543613 is a potent, selective agonist of alpha7 neuronal nicotinic acetylcholine receptor (α7 nAChR) with Ki of 8.8 nM, EC50 of 65 nM in cell-based FLIPR assay.

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

生物&药学活性

PHA-543613 is a potent, selective agonist of alpha7 neuronal nicotinic acetylcholine receptor (α7 nAChR) with Ki of 8.8 nM, EC50 of 65 nM in cell-based FLIPR assay.
PHA-543613 shows no detectible agonist activity (>100 μM) and negligible antagonist activity at both muscle-like nAChRs (TE671 cells) and ganglion-like nAChRs (SH-SY5Y cells), as well as α4β2 nAChR subtype.
PHA-543613 is characterized by rapid brain penetration and high oral bioavailability in rat and demonstrates in vivo efficacy in auditory sensory gating and, in an in vivo model to assess cognitive performance, novel object recognition.

物理化学性质&存储条件

分子量 271.32
分子式 C15H17N3O2
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

N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide

参考文献

1. Wishka DG, et al. J Med Chem. 2006 Jul 13;49(14):4425-36.

2. Freitas K, et al. Neuropharmacology. 2013 Feb;65:156-64.

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