GSK 189254A - CAS 720690-73-3
Catalog number: B0084-459482
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C21H25N3O2
Molecular Weight:
351.44
COA:
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Targets:
Histamine Receptor
Description:
GSK-189,254 is a H3 histamine receptor inverse agonist. It has subnanomolar affinity for the H3 receptor with Ki of 0.2nM. It possesses stimulant and nootropic effects and analgesic action suggesting a role for H3 receptors in pain processing in the spinal cord. No development was reported about Phase-II clinical trials for Narcolepsy in Europe.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-459482 300 mg $688 In stock
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Purity:
98%
Appearance:
Powder
Synonyms:
6-((3-Cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy)-N-methyl-3-Pyridinecarboxamide,
Solubility:
Soluble in DMSO
Storage:
-20℃ Freezer
MSDS:
Inquire
Application:
Narcolepsy
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
InChIKey:
WROHEWWOCPRMIA-UHFFFAOYSA-N
InChI:
1S/C21H25N3O2/c1-22-21(25)17-6-8-20(23-14-17)26-19-7-5-15-9-11-24(18-3-2-4-18)12-10-16(15)13-19/h5-8,13-14,18H,2-4,9-12H2,1H3,(H,22,25)
Canonical SMILES:
CNC(=O)c1ccc(nc1)Oc2ccc3c(c2)CCN(CC3)C4CCC4
Current Developer:
Originator GlaxoSmithKline
1.Synthesis and preliminary characterization of radioiodinated benzofuran-3-yl-(indol-3-yl)maleimide derivatives as potential SPECT imaging probes for the detection of glycogen synthase kinase-3β (GSK-3β) in the brain.
Ono M1, Kitada A1, Watanabe H1, Miyazaki A1, Kimura H1, Saji H1. J Labelled Comp Radiopharm. 2016 Apr 29. doi: 10.1002/jlcr.3404. [Epub ahead of print]
We report on the synthesis and preliminary characterization of two radioiodinated benzofuran-3-yl-(indol-3-yl)maleimides, 3-(benzofuran-3-yl)-4-(5-[125 I]iodo-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione ([125 I]5), and 3-(5-[125 I]iodo-1-methyl-1H-indol-3-yl)-4-(6-methoxybenzofuran-3-yl)-1H-pyrrole-2,5-dione ([125 I]6), as the first potential SPECT imaging probes targeting glycogen synthase kinase-3β (GSK-3β). In this study, we used 125 I as a surrogate of 123 I because of its ease of use. The radioiodinated ligands were prepared from the corresponding tributyltin precursors through an iododestannylation reaction using hydrogen peroxide as an oxidant with a radiochemical yield of 10-30%. In vitro binding experiments suggested that both compounds show high affinity for GSK-3β at a level similar to a known GSK-3β inhibitor. Biodistribution studies with normal mice revealed that the radioiodinated compounds display sufficient uptake into (1.
2.Neuroprotective effects of honokiol against beta-amyloid-induced neurotoxicity via GSK-3β and β-catenin signaling pathway in PC12 cells.
Xian YF1, Ip SP2, Mao QQ1, Lin ZX3. Neurochem Int. 2016 Apr 27. pii: S0197-0186(16)30064-X. doi: 10.1016/j.neuint.2016.04.014. [Epub ahead of print]
Beta-amyloid (Aβ) accumulation, one of the most important pathogenic traits of Alzheimer's disease (AD), has been reported to induce neurotoxicity in vitro as well as in vivo. Honokiol, isolated from the bark of Magnolia officinalis, has neuroprotective effects in different models of AD in vivo and in vitro. However, the exact mechanism for its neuroprotective effect is not well understood. The present study aimed to investigate the molecular mechanisms underlying the protective action of honokiol against Aβ1-42-induced neurotoxicity in cultured rat pheochromocytoma (PC12) cells. The results revealed that honokiol protected PC12 cells from Aβ1-42 induced cytotoxicity with increases in cell viability, GSH production and Bcl-2 expression, but decreases in the release of lactate dehydrogenase and cytochrome c, the amount of DNA fragmentation and MDA level, as well as Bax expression. Mechanistic study showed that honokiol could inhibit the activation of glycogen synthase kinase (GSK)-3β, attenuate the nuclear accumulation of β-catenin and suppress the phosphorylation of β-catenin (Ser33/Ser37/Thr41 site) in the Aβ1-42-treated PC12 cells.
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CAS 720690-73-3 GSK 189254A

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