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品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear
儲存溫度
2-8°C
SMILES 字串
CN1C(CN(CC#C)C)=CC2=C1C=CC(OCCCC(CC3)CCN3CC4=CC=CC=C4)=C2
生化／生理作用
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).
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
Upregulation of Antioxidant Enzymes by ASS234, a Multitarget Directed Propargylamine for Alzheimer's Disease Therapy.
Eva Ramos et al.
CNS neuroscience & therapeutics, 22(9), 799-802 (2016-07-07)
Óscar M Bautista-Aguilera et al.
Journal of medicinal chemistry, 61(15), 6937-6943 (2018-07-04)
Contilisant, a permeable, antioxidant, and neuroprotectant agent, showing high nM affinity at H3R and excellent inhibition of the monoamine oxidases and cholinesterases, is an affine and selective S1R agonist in the nanomolar range, based on the binding affinity and functional
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
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
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
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