ZINC12613047
![mRNA synthesis](/media/diy/images/page/figure1-mrna.png)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
![Tyramine Signal Amplification (TSA)](/media/diy/images/page/figure2-01.png)
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
![screening library](/media/diy/images/page/figure3-01.png)
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
![Cell Counting Kit-8 (CCK-8)](/media/diy/images/page/CCK-8.jpg)
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
![SYBR Safe DNA Gel Stain](/media/diy/images/page/SYBR Safe DNA Gel Stain.png)
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
![Inhibitor Cocktails](/media/diy/images/page/Inhibitor Cocktails.jpg)
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50: 21 nM for human BChE
ZINC12613047 is a BChE inhibitor.
Butyrylcholinesterase (BChE) is considered as a promising drug target as its levels and activity increase significantly in the late stages of Alzheimer’s disease.
In vitro: In previous study, the complex structure between ZINC12613047 and BChE revealed the molecular basis of the high affinity binding. In contrast, the pocket was comparatively smaller in AChE likely explaining why ZINC12613047 displayed low affinity. In addition, ZINC12613047 was tested at 10 μM, where it showed significant Aβ1-42-antiaggregation effects with 61.7% inhibition. The cytotoxicity profile was assessed using the human neuroblastoma SH-SY5Y cell line and the MTS assay. ZINC12613047 at 10 μM was completely noncytotoxic. Moreover, to compare neuronal death induced by Aβ1-42 with or without various concentrations of ZINC12613047, the MTS assay was performed. Results showed that incubation of SH-SY5Y cells with 5 μM Aβ1-42 led to significant toxicity; the cell-death was about 35% higher than in the control. A clear dose-response neuroprotective effect was observed when the cells were incubated with Aβ1-42 in the presence of ZINC12613047. ZINC12613047 at 10 μM could completely protect the human neuronal SH-SY5Y cells from Aβ1-42 peptide toxicity [1].
In vivo: There is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] B. Brus, U. Kosak, S. Turk, et al. Discovery, biological evaluation, and crystal structure of a novel nanomolar selective butyrylcholinesterase inhibitor. Journal of Medicinal Chemistry 57(19), 8167-8179 (2014).
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 442.6 |
Cas No. | 1069521-64-7 |
Formula | C29H34N2O2 |
Solubility | ≤5mg/ml in ethanol;10mg/ml in DMSO |
Chemical Name | N-[[1-(2,3-dihydro-1H-inden-2-yl)-3-piperidinyl]methyl]-N-(2-methoxyethyl)-2-naphthalenecarboxamide |
SDF | Download SDF |
Canonical SMILES | COCCN(C(C1=CC(C=CC=C2)=C2C=C1)=O)CC3CCCN(C4CC(C=CC=C5)=C5C4)C3 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
化学结构
![ZINC12613047](http://www.apexbt.com//media/diy/images/struct/C3580.png)