Chemical Structure : TAK-861
CAS No.:
2460722-04-5
TAK-861
(TAK861)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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520.52
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Formula
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C23H25F5N2O4S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Mitsukawa K, et al. Sci Rep. 2024 Sep 6;14(1):20838.
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