LX2343|cas:333745-53-2|西域试剂

LX2343,99.74%

产品编号：Bellancom-111383| CAS NO：333745-53-2| 分子式：C₂₂H₁₉ClN₂O₆S| 分子量：474.91

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货号	价格	库存与货期
Bellancom-111383	￥950.00	杭州北京（现货）
Bellancom-111383	￥1500.00	杭州北京（现货）
Bellancom-111383	￥4900.00	杭州北京（现货）
Bellancom-111383	￥7500.00	杭州北京（现货）

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LX2343

产品介绍

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

生物活性

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.

体外研究

LX2343 (5-20 μM) 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-APP_sw 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 .

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (210.57 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1057 mL	10.5283 mL	21.0566 mL
5 mM	0.4211 mL	2.1057 mL	4.2113 mL
10 mM	0.2106 mL	1.0528 mL	2.1057 mL

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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.26 mM); 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 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.26 mM); 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。