首页 工具
登录
购物车
LX2343

LX2343

产品编号 T4398   CAS 333745-53-2

LX2343 是一种非 ATP 竞争性 PI3K 抑制剂,IC50 为 15.99±3.23 μM。它是一种 BACE1 酶抑制剂,IC50 值为 11.43±0.36 μM。它在促进 Aβ 清除中刺激自噬

TargetMol的所有产品和服务仅用于科学研究,不能被用于人体,我们也不向个人提供产品和服务。
LX2343 Chemical Structure
LX2343, CAS 333745-53-2
规格 价格/CNY 货期 数量
1 mg ¥ 329 现货
2 mg ¥ 478 现货
5 mg ¥ 778 现货
10 mg ¥ 1,170 现货
25 mg ¥ 1,980 现货
50 mg ¥ 2,950 现货
100 mg ¥ 4,260 现货
1 mL * 10 mM (in DMSO) ¥ 822 现货
产品目录号及名称: LX2343 (T4398)
点击图片重新获取验证码
选择批次  
纯度: 99.92%
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 LX2343 is a BACE1 enzyme inhibitor with an IC50 value of 11.43±0.36 μM. LX2343 acts as a non-ATP competitive PI3K inhibitor with an IC50 of 15.99±3.23 μM. LX2343 stimulates autophagy in its promotion of Aβ clearance.
靶点活性 BACE1:11.43 μM, PI3K:15.99 μM, Autophagy:, Aβ:
体外活性 LX2343 (5-20 μM) dose-dependently decreased Aβ accumulation in HEK293-APPsw and CHO-APP cells. It also promotes Aβ clearance in SH-SY5Y cells and primary astrocytes. LX2343 ameliorates cognitive dysfunction in APP/PS1 transgenic mice through both Aβ production inhibition and clearance promotion, which highlights the potential of LX2343 in the treatment of AD. Western blot results in both HEK293-APPsw cells and CHO-APP cells demonstrate that LX2343 fails to regulate BACE1 protein levels, while in vitro BACE1 enzymatic activity assays indicated that LX2343 dose-dependently decreases BACE1 activity (TDC as a positive control) with an IC50 of 11.43±0.36 μM. To test whether competition exists between LX2343 and ATP, we investigated the effects of ATP at different concentrations on the inhibitory activity of LX2343. The result demonstrated that the inhibition of LX2343 against PI3K is virtually unaffected by ATP. Thus, this result suggested that LX2343 is a non-ATP competitive inhibitor of PI3K. In the presence of 10 μM of ATP, the IC50 of LX2343 is 13.11±1.47 μM, in the presence of 50 μM ATP, the IC50 of LX2343 is 13.86±1.12 μM, in the presence of 100 μM ATP, the IC50 of LX2343 is 15.99±3.23 μM.
体内活性 APP/PS1 mice express chimeric human Swedish mutant APP and a mutant human presenilin 1 protein and are widely used as an effective animal model for AD dementia. The amelioration of memory impairment by LX2343 is evaluated t in this model using the MWM test. The path lengths and escape latencies used to find the platform for APP/PS1 transgenic mice are remarkably longer than those for non-transgenic mice in 8-d training trials. However, 10 mg/kg LX2343 administration obviously antagonizes the prolonged path lengths and escape latencies at d 7 and 8. In the probe trial assay, the LX2343-administered transgenic mice cross over the hidden location of the platform more frequently compared with the vehicle-administered transgenic mice.
激酶实验 Inhibition of BACE1 enzyme by LX2343 is assayed using BACE1 activity kits in vitro. Briefly, BACE1 substrate (250 nM), BACE1 enzyme (0.35 U/mL), and varied concentrations of LX2343 (5, 10, and 20 μM) are sequentially incubated for 1 h at 37°C in the dark. Fluorescence intensity is measured with excitation and emission wavelengths at 545 and 585 nm, respectively
细胞实验 SH-SY5Y cells are transfected with mRFP-GFP-LC3 plasmids via an adenovirus. The cells are treated without or with Streptozotocin (0.8 mM) in combination with 5 or 20 μM LX2343 for 4 h and then fixed with 4% paraformaldehyde and observed using an Olympus Fluoview FV1000 confocal microscope
动物实验 LX2343 is dissolved in 3% DMSO and 5% tween-80.MiceAPP/PS1 [B6C3-Tg(APPswe, PS1dE9)] transgenic mice are used. Genotyping to confirm APP/PS1 DNA sequences in their offspring is performed by assaying the DNA from tail biopsies, with Tg-negative mice as a negative control. Twenty male APP/PS1 mice are divided into two groups with ten non-transgenic mice in one group to serve as a negative control. The two 6-month transgenic groups are administered 10 mg/kg per day of LX2343 or vehicle, and the 6-month non-transgenic group is administered the vehicle for 100 d via intraperitoneal injection. After 100 d of administration, MWM assays are applied to evaluate the cognitive abilities of the mice for 8 d under continuous LX2343 treatment. Upon completion of the MWM test, the mice are euthanized, and the brains are removed and bisected at the mid-sagittal plane. The right hemispheres are frozen and stored at -80°C, and the left hemispheres are fixed in 4% paraformaldehyde
分子量 474.91
分子式 C22H19ClN2O6S
CAS No. 333745-53-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 155 mg/mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
=
X
X
X
=
X
=
/
g/mol

输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Guo XD,etal.Small molecule LX2343 ameliorates cognitive deficits in AD model mice by targeting both amyloid β production and clearance.Acta Pharmacol Sin. 2016 Sep;37(10):1281-1297.
RAGE antagonist peptide acetate BSBM7 CGP52411 β-Amyloid 15-21 acetate 2-O-Acetyl-20-hydroxyecdysone Deferoxamine Mesylate Cedrin Astrophloxine

相关化合物库

该产品包含在如下化合物库中:
神经退行性疾病化合物库 激酶抑制剂库 神经信号分子库 抗肝癌化合物库 NO PAINS 化合物库 氧化还原化合物库 神经元分化化合物库 抗结直肠癌化合物库 抗阿尔茨海默症化合物库 糖代谢化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

LX2343 333745-53-2 Autophagy Neuroscience PI3K/Akt/mTOR signaling Beta Amyloid Beta-Secretase BACE PI3K LX-2343 Amyloid-β Inhibitor LX 2343 β-Secretase Beta-secretase inhibit Phosphoinositide 3-kinase β-amyloid peptide Abeta inhibitor

 

陶术
生物
TargetMol®中国区唯一合作伙伴
点击进入陶术生物官网陶术生物
联系我们
400-820-0310

上海市静安区江场三路238号8楼