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SML2769

Sigma-Aldrich

ASS234

≥98% (HPLC)

Sinónimos:

N,1-Dimethyl-5-[3-[1-(phenylmethyl)-4-piperidinyl]propoxy]-N-2-propyn-1-yl-1H-indole-2-methanamine, N-[[5-[3-(1-Benzylpiperidin-4-yl)propoxy]-1-methyl-1H-indol-2-yl]methyl]-N-methyl-2-propyn-1-amine

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About This Item

Fórmula empírica (notación de Hill):
C29H37N3O
Número de CAS:
1334106-34-1
Peso molecular:
443.62
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

CN1C(CN(CC#C)C)=CC2=C1C=CC(OCCCC(CC3)CCN3CC4=CC=CC=C4)=C2

Biochem/physiol Actions

ASS234 is a brain-penetrant and orally active multi-target small molecule (MTSM) against (acetyl & butyryl) cholinesterases (hAChE/hBuChE IC50 = 0.81/1.82 μM), monoamine oxidases (hMAO-A/B IC50 = 0.27/120 nM), histamine H3 receptor (hH3R Ki = 84.2 nM; hH4R Ki >10 μM) and sigma-1/2 receptors (hS1R/rS2R = 2.82/50.3 nM). ASS234 exhibits antioxidative and neuroprotective effects in SH-SY5Y cultures (5 μM) and demonstrates therapeutic efficacy in neurodegerative disease models in vivo via sc. (0.62 mg/kg/d mice; 5 mg/kg rats), ip. (1 mg/kg mice) or po. (1 & 10 mg/kg mice).

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

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Óscar M Bautista-Aguilera et al.
Angewandte Chemie (International ed. in English), 56(41), 12765-12769 (2017-09-02)
The therapy of complex neurodegenerative diseases requires the development of multitarget-directed drugs (MTDs). Novel indole derivatives with inhibitory activity towards acetyl/butyrylcholinesterases and monoamine oxidases A/B as well as the histamine H3 receptor (H3R) were obtained by optimization of the neuroprotectant
Javier Del Pino et al.
ACS chemical neuroscience, 9(12), 2880-2885 (2018-07-27)
There is clear evidence that neuroinflammation plays a crucial role in the pathogenesis of Alzheimer's disease. Consequently, modulating the inflammatory environment in brain has become a powerful and attractive strategy to deal with Alzheimer's disease physiopathology. In spite of the
José Marco-Contelles et al.
Frontiers in neuroscience, 10, 294-294 (2016-07-23)
ASS2324 is a hybrid compound resulting from the juxtaposition of donepezil and the propargylamine PF9601N ASS2324 is a multi-target directed propargylamine able to bind to all the AChE/BuChE and MAO A/B enzymesASS2324 shows antioxidant, neuroprotective and suitable permeability propertiesASS2324 restores
Wnt signaling pathway, a potential target for Alzheimer's disease treatment, is activated by a novel multitarget compound ASS234.
Javier del Pino et al.
CNS neuroscience & therapeutics, 20(6), 568-570 (2014-04-10)
Anna Stasiak et al.
Current pharmaceutical design, 20(2), 161-171 (2013-05-25)
Neurodegenerative disorders are associated with different neurochemical and morphological alterations in the brain leading to cognitive and behavioural impairments. New therapeutic strategies comprise multifunctional drugs. The aim of the presented studies is to evaluate in vivo the novel compounds -
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