SML2769
ASS234
≥98% (HPLC)
别名:
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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关于此项目
Quality Level
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
InChI key
ADCBAOTWERXLAP-UHFFFAOYSA-N
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).
Orally active, brain-penetrant, multi-target ligand against MAO-A/B, cholinesterases, H3 & sigma receptors with neuroprotective and pro-cognitive efficacy in vivo.
存储类别
11 - Combustible Solids
wgk
WGK 3
法规信息
新产品
此项目有
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
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| SML2769-5MG | 04061841693123 |
| SML2769-25MG | 04061841693116 |