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首页-小分子抑制剂&激动剂-GPCR-GPR139-TAK-041
TAK-041

Chemical Structure : TAK-041

CAS No.: 1929519-13-0

TAK-041 (Zelatriazin, NBI-1065846, TAK041)

货号: PC-72146Not For Human Use, Lab Use Only.

TAK-041 (Zelatriazin, NBI-1065846) is a potent, selective, brain-penetrant GPR139 agonist with EC50 of 22 nM (CHO-T-REx Ca2+ assays), Ki of 119 nM.

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

生物&药学活性

TAK-041 (Zelatriazin, NBI-1065846) is a potent, selective, brain-penetrant GPR139 agonist with EC50 of 22 nM (CHO-T-REx Ca2+ assays), Ki of 119 nM.
TAK-041 improves the social behavior in BALB/c mice, TAK-041 demonstrated GPR139-agonist-dependent modulation of habenula cell activity and revealed consistent in vivo efficacy to rescue social interaction deficits in the BALB/c mouse strain.
TAK-041 (NBI-1065846) is currently under development for treatment of negative symptoms in SCZ.

物理化学性质&存储条件

分子量 392.338
分子式 C18H15F3N4O3
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

(S)-2-(4-Oxobenzo[d][1,2,3]triazin-3(4H)-yl)-N-(1-(4-(trifluoromethoxy)phenyl)ethyl)acetamide

参考文献

1. Reichard HA, et al. J Med Chem. 2021 Aug 12;64(15):11527-11542.

2. Rabiner EA, et al. Neuropsychopharmacology. 2021 Oct 21.

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