|N-(苯并[d][1,3]二氧戊环-5-基)-2-(N-(5-氯-2-甲氧基苯基)苯基磺酰胺基)乙酰胺|CsnPharm

CAS No.: 333745-53-2

LX2343 Catalog No. CSN21265

Synonyms: Lx2343

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.

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实验方案

技术信息

生物活性

描述The β secretase, widely known as β-site amyloid precursor protein cleaving enzyme 1 (BACE1), initiates the production of the toxic amyloid β (Aβ) that plays a crucial early part in Alzheimer's disease pathogenesis ^[1]. Amyloid fibrils are protein homopolymers that adopt diverse cross-β conformations. Some amyloid fibrils are associated with the pathogenesis of devastating neurodegenerative disorders, including Alzheimer's disease and Parkinson's disease ^[2]. The anti-amyloid effects of LX2343 were attributed inhibiting BACE1 enzymatic activity with an IC₅₀ value of 11.43±0.36 μM. LX2343 (5–20 μM) dose-dependently decreased Aβ accumulation in HEK293-APP_sw and CHO-APP cells, and promoted Aβ clearance in SH-SY5Y cells and primary astrocytes. Furthermore, LX2343 acted as a non-ATP competitive PI3K inhibitor to negatively regulate AKT/mTOR signaling, thus promoting autophagy, and increasing Aβ clearance ^[3]. Administration of LX2343 in APP/PS1 transgenic mice significantly ameliorated cognitive deficits and markedly ameliorated the Aβ pathology in their brains ^[3].
作用机制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.
参考文献

[1] Yan R, Vassar R. Targeting the β secretase BACE1 for Alzheimer's disease therapy. Lancet Neurol. 2014 Mar;13(3):319-29. doi: 10.1016/S1474-4422(13)70276-X. Epub 2014 Feb 17. PMID: 24556009; PMCID: PMC4086426.
[2] Chuang E, Hori AM, Hesketh CD, Shorter J. Amyloid assembly and disassembly. J Cell Sci. 2018 Apr 13;131(8):jcs189928. doi: 10.1242/jcs.189928. PMID: 29654159; PMCID: PMC5963839.
[3] Guo XD, Sun GL, Zhou TT, Xu X, Zhu ZY, Rukachaisirikul V, Hu LH, Shen X. 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. doi: 10.1038/aps.2016.80. Epub 2016 Aug 29. PMID: 27569389; PMCID: PMC5057240.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1056 mL
- 10.5282 mL
- 21.0564 mL
- 5 mM
- 0.4211 mL
- 2.1056 mL
- 4.2113 mL
- 10 mM
- 0.2106 mL
- 1.0528 mL
- 2.1056 mL

技术信息

CAS号

333745-53-2

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H19ClN2O6S

运输

蓝冰

分子量

474.91

别名

Lx2343

溶解度

DMSO	165.0 mg/mL (347.4 mM)
Water	insoluble

动物实验配方

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