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首页-小分子抑制剂&激动剂-GPCR-mAChR-TAK-071
TAK-071

Chemical Structure : TAK-071

CAS No.: 1820812-16-5

TAK-071 (TAK071;TAK 071)

货号: PC-35576Not For Human Use, Lab Use Only.

TAK-071 (TAK071) is a potent, selective, low cooperativity (α-value) positive allosteric modulator of muscarinic M1 receptor with inflection point of 2.7 nM in Ca2+ flux assays in CHO-K1 cells.

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

生物&药学活性

TAK-071 (TAK071) is a potent, selective, low cooperativity (α-value) positive allosteric modulator of muscarinic M1 receptor with inflection point of 2.7 nM in Ca2+ flux assays in CHO-K1 cells.
TAK-071 displays >370-fold M1R selectivity over other muscarinic receptors.
TAK-071 selectively induces afterdepolarization in prefrontal cortical pyramidal neurons significantly ameliorates scopolamine-induced cognitive deficits in rats combined with acetylcholinesterase inhibitor donepezil, with minimizing peripheral cholinergic side effects.

物理化学性质&存储条件

分子量 421.472
分子式 C24H24FN3O3
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-fluoro-2-[(3S,4S)-4-hydroxytetrahydro-2H-pyran-3-yl]-5-methyl-6-[4-(1H-pyrazol-1-yl)benzyl]-2,3-dihydro-1H-isoindol-1-one

参考文献

1. Sako Y, et al. Neuropsychopharmacology. 2018 Aug 1. doi: 10.1038/s41386-018-0168-8.

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