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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-iGluR-TAK-653
TAK-653

Chemical Structure : TAK-653

CAS No.: 1358751-06-0

TAK-653 (Osavampator, NBI-1065845, TAK653)

货号: PC-22292Not For Human Use, Lab Use Only.

TAK-653 (NBI-1065845, Osavampator) is a potent, selective AMPA receptor positive allosteric modulator/potentiator, induces Ca2+ influx in hGluA1i CHO cells with EC50 of 2.2 uM.

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

生物&药学活性

TAK-653 (NBI-1065845, Osavampator) is a potent, selective AMPA receptor positive allosteric modulator/potentiator, induces Ca2+ influx in hGluA1i CHO cells with EC50 of 2.2 uM.
TAK-653 exhibits minimal agonistic properties, binds to the ligand binding domain of recombinant AMPA-R in a glutamate-dependent manner.
TAK-653 strictly potentiated a glutamate-induced Ca2+ influx in hGluA1i-expressing CHO cells through structural interference at Ser743 in GluA1.
TAK-653 augmented AMPA-induced Ca2+ influx and AMPA-elicited currents via physiological AMPA-R with little agonistic effects in primary neurons.
TAK-653 enhanced electrically evoked AMPA-R-mediated EPSPs more potently than AMPA (agonist) or LY451646 (AMPA-R potentiator with a prominent agonistic effect) in brain slices.
TAK-653 improved cognition for both working memory and recognition memory.

物理化学性质&存储条件

分子量 373.47
分子式 C19H23N3O3S
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

9-(4-(Cyclohexyloxy)phenyl)-7-methyl-3,4-dihydropyrazino[2,1-c][1,2,4]thiadiazine 2,2-dioxide

参考文献

1. O'Donnell P, et al. Transl Psychiatry. 2021 May 27;11(1):325.

2. Suzuki A, et al. Sci Rep. 2021 Jul 21;11(1):15255.

3. Suzuki A, et al. Sci Rep. 2021 Jul 15;11(1):14532.

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