推荐产品
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
CN1C(CN(CC#C)C)=CC2=C1C=CC(OCCCC(CC3)CCN3CC4=CC=CC=C4)=C2
InChI key
ADCBAOTWERXLAP-UHFFFAOYSA-N
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).
Orally active, brain-penetrant, multi-target ligand against MAO-A/B, cholinesterases, H3 & sigma receptors with neuroprotective and pro-cognitive efficacy in vivo.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
法规信息
新产品
历史批次信息供参考:
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
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)
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 -
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
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