TAK-861 | OX2R agonist | Probechem Biochemicals

Chemical Structure : TAK-861

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TAK-861 (TAK861)

货号: PC-23032Not For Human Use, Lab Use Only.

TAK-861 is a potent, selective, orally available orexin receptor 2 (OX2R) agonist with EC50 of 2.5 nM, weakly activates OX1R (EC50=7.5 uM).

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生物&药学活性

TAK-861 is a potent, selective, orally available orexin receptor 2 (OX2R) agonist with EC50 of 2.5 nM, weakly activates OX1R (EC50=7.5 uM).
TAK-861 shows no inhibition on various enzymes, receptors, and ion channels (102 targets in total) in in vitro assays.
TAK-861 induces dose-dependent depolarization of the membrane potential in histaminergic neurons in the mouse TMN with EC50 of 31.7 nM.
TAK-861 dose-dependently increases iInositol monophosphate (IP1) contents and increases β-arrestin recruitmentin in OX2R-expressing cells with EC50 of 1.2 nM and 30 nM.
TAK-861 induces phosphorylation of ERK1/2 and phosphorylation of CREB with EC50 of 34 nM and 3.6 nM).
TAK‑861 produces wake‑promoting effects via OX2R activation in both mice and monkeys during the sleep phase, ameliorates narcolepsy‑like phenotypes in orexin/ataxin‑3 mice.

物理化学性质&存储条件

分子量	520.52
分子式	C23H25F5N2O4S
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-((2S,3R)-4,4-difluoro-1-(2-hydroxy-2-methylpropanoyl)-2-((2,3',5'-trifluoro-[1,1'-biphenyl]-3-yl)methyl)pyrrolidin-3-yl)ethanesulfonamide

参考文献

1. Mitsukawa K, et al. Sci Rep. 2024 Sep 6;14(1):20838.

TAK-861 (TAK861)

生物&药学活性

物理化学性质&存储条件

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TAK-861 (TAK861)

生物&药学活性

物理化学性质&存储条件

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