| 中文名称: | LX2343 | ||||
|---|---|---|---|---|---|
| 英文名称: | LX2343 | ||||
| 别名: | N-(benzo[d][1,3]dioxol-5-yl)-2-(N-(5-chloro-2-methoxyphenyl)phenylsulfonamido)acetamide | ||||
| CAS No: | 333745-53-2 | 分子式: | C22H19ClN2O6S | 分子量: | 474.91 |
| CAS No: | 333745-53-2 | ||||
| 分子式: | C22H19ClN2O6S | ||||
| 分子量: | 474.91 | ||||
基本信息
|
产品编号： |
L10367 |
||||
|
产品名称： |
LX2343 |
||||
|
CAS: |
333745-53-2 |
储存条件 |
粉末 |
-20℃ |
四年 |
|
|
|
||||
|
分子式： |
溶于液体 |
-80℃ |
6个月 |
||
|
分子量： |
474.91 |
-20℃ |
1个月 |
||
|
化学名： |
N-(benzo[d][1,3]dioxol-5-yl)-2-(N-(5-chloro-2-methoxyphenyl)phenylsulfonamido)acetamide |
||||
|
Solubility (25°C)： |
|||||
|
体外:
|
DMSO |
95mg/mL (200.03mM) |
|||
|
Ethanol |
Insoluble |
||||
|
Water |
Insoluble |
||||
|
体内(现配现用): |
1.请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility:≥2.5mg/mL(5.26mM);Clear solution |
||||
|
此⽅案可获得 ≥ 2.5 mg/mL (5.26 mM，饱和度未知) 的澄清溶液。 以 1 mL ⼯作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加⼊ 50 μ L Tween-80，混合均匀；然后继续加⼊ 450 μL ⽣理盐⽔定容⾄ 1 mL。 |
|||||
|
2.请依序添加每种溶剂：10% DMSO→90% corn oil Solubility:≥2.5mg/mL(5.26mM);Clear solution |
|||||
|
此⽅案可获得 ≥ 2.5 mg/mL (5.26 mM，饱和度未知) 的澄清溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。 以 1 mL ⼯作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL ⽟⽶油中，混合均匀。 |
|||||
|
＜1mg/ml表示微溶或不溶。 |
|||||
|
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
|||||
|
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
|||||
制备储备液
|
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
|
1mM |
2.1057mL |
10.5283mL |
21.0566mL |
|
5mM |
0.4211mL |
2.1057mL |
4.2113mL |
|
10mM |
0.2106mL |
1.0528mL |
2.1057mL |
生物活性
|
产品描述 |
一种BACE1酶抑制剂，IC50值为11.43±0.36μM。LX2343是一种非ATP竞争性的PI3K抑制剂，IC50为15.99±3.23μM。LX2343刺激自噬促进Aβ清除。 |
|
靶点 |
Beta-secretase;PI3K;Amyloid-β;Autophagy |
|
体外研究 |
LX2343 (5-20μM) dose-dependently decreased Aβ accumulation in HEK293-APPsw and CHO-APP cells,and promotes Aβ clearance in SH-SY5Y cells and primary astrocytes.LX2343 ameliorates cognitive dysfunction in APP/PS1 transgenic mice via 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±0.36μM.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 10μM of ATP,the IC50 of LX2343 is 13.11±1.47μM,in the presence of 50μM ATP,the IC50 of LX2343 is 13.86±1.12μM,in the presence of 100μM ATP,the IC50 of LX2343 is 15.99±3.23μM. |
|
体内研究 |
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.In 8-d training trials,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,while 10mg/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. |
推荐实验方法(仅供参考)
|
激酶实验： |
|
Inhibition of BACE1 enzyme by LX2343 is assayed using BACE1 activity kits in vitro.Briefly,BACE1 substrate (250nM),BACE1 enzyme (0.35 U/mL),and varied concentrations of LX2343 (5,10,and 20μM) are sequentially incubated for 1h at 37℃ in the dark.Fluorescence intensity is measured with excitation and emission wavelengths at 545 and 585nm,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 (0.8mM) in combination with 5 or 20μM LX2343 for 4h and then fixed with 4% paraformaldehyde and observed using an Olympus Fluoview FV1000 confocal microscope. |
|
|
动物实验: |
|
|
Mice APP/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 10mg/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℃,and the left hemispheres are fixed in 4% paraformaldehyde. |
|
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
