LX-2343 | CAS#333745-53-2 | neuroprotective agent

MedKoo Cat#: 555226 | Name: LX-2343

Description:

WARNING: This product is for research use only, not for human or veterinary use.

LX-2343 is a neuroprotective agent for the treatment of Alzheimer's disease. 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. LX2343 ameliorates the cognitive dysfunction in the AD model rats by suppressing OS-induced neuronal apoptosis and tauopathy, thus highlighting the potential of LX2343 for the treatment of AD.

Chemical Structure

LX-2343

CAS#333745-53-2

Theoretical Analysis

MedKoo Cat#: 555226

Name: LX-2343

CAS#: 333745-53-2

Chemical Formula: C22H19ClN2O6S

Exact Mass: 474.0652

Molecular Weight: 474.91

Elemental Analysis: C, 55.64; H, 4.03; Cl, 7.46; N, 5.90; O, 20.21; S, 6.75

Price and Availability

Size	Price	Availability
10mg	USD 150.00	Ready to ship
25mg	USD 250.00	Ready to ship
50mg	USD 450.00	Ready to ship
100mg	USD 850.00	Ready to ship
200mg	USD 1,450.00	Ready to ship
500mg	USD 1,950.00	Ready to ship
1g	USD 2,650.00	Ready to ship
2g	USD 3,950.00	Ready to ship
5g	USD 6,450.00	2 weeks

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Related CAS #

No Data

Synonym

LX-2343; LX 2343; LX2343;

IUPAC/Chemical Name

N-(benzo[d][1,3]dioxol-5-yl)-2-(N-(5-chloro-2-methoxyphenyl)phenylsulfonamido)acetamide

InChi Key

ZGYSGIYKAVUVOR-UHFFFAOYSA-N

InChi Code

InChI=1S/C22H19ClN2O6S/c1-29-19-9-7-15(23)11-18(19)25(32(27,28)17-5-3-2-4-6-17)13-22(26)24-16-8-10-20-21(12-16)31-14-30-20/h2-12H,13-14H2,1H3,(H,24,26)

SMILES Code

C1=C(NC(CN(C2=CC(Cl)=CC=C2OC)S(C2=CC=CC=C2)(=O)=O)=O)C=C2OCOC2=C1

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#A9T03K25

QC Data

View QC data: current batch, Lot#A9T03K25

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

LX2343 is a BACE1 enzyme inhibitor with an IC50 value of 11.43±0.36 μM.

In vitro activity:

As demonstrated in Figure 1D and 1E, STZ (Streptozotocin) treatment induced an 18.11%±1.15% and 27.82%±0.82% decrease in cell viability for SH-SY5Y and primary neuronal cells, respectively, while co-incubation with LX2343 effectively antagonized the effects of STZ. In addition, quantitative evaluation of apoptosis in SH-SY5Y cells using Annexin V-FITC staining further demonstrated the capability of LX2343 to prevent STZ-induced apoptosis (Figure 1F). Compared with the controls, the apoptosis rate of the SH-SY5Y cells was increased to 21.88%±0.91% when the cells were stimulated with STZ, and the apoptosis rate was decreased to 14.57%±0.66% after the cells were co-incubated with 20 μmol/L LX2343. These data indicated that treating SH-SY5Y and primary neuronal cells with LX2343 could reduce cell death and increase cell viability. Reference: Acta Pharmacol Sin. 2017 Aug; 38(8): 1104–1119. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5547549/

In vivo activity:

Next, the promotion of LX2343 on Aβ clearance by activating PI3K/AKT/mTOR-mediated autophagy was investigated in the cortex of APP/PS1 transgenic mice via Western blot analysis. The results indicated that the phosphorylation levels of PI3K, AKT, mTOR, P70S6, and ULK1 and the protein level of p62 were higher, while the cleavage of LC3 was more restrained in transgenic mice compared to non-transgenic mice, indicating the suppression of autophagy. LX2343 administration alleviated these effects, thus activating autophagy. These results demonstrated the efficacy of LX2343 in promoting PI3K/AKT/mTOR-mediated autophagy in APP/PS1 transgenic mice (Figure 8E–8G). Reference: Acta Pharmacol Sin. 2016 Oct; 37(10): 1281–1297. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5057240/

	Solvent	mg/mL	mM
Solubility
	DMSO	73.3	154.41
	DMF	33.0	69.49

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 474.91 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Guo XD, Sun GL, Zhou TT, Wang YY, Xu X, Shi XF, Zhu ZY, Rukachaisirikul V, Hu LH, Shen X. LX2343 alleviates cognitive impairments in AD model rats by inhibiting oxidative stress-induced neuronal apoptosis and tauopathy. Acta Pharmacol Sin. 2017 Aug;38(8):1104-1119. doi: 10.1038/aps.2016.128. Epub 2017 Jun 26. PMID: 28649128; PMCID: PMC5547549. 2. 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.

In vitro protocol:

In vivo protocol:

1: Sun G, Wang J, Guo X, Lei M, Zhang Y, Wang X, Shen X, Hu L. Design, synthesis and biological evaluation of LX2343 derivatives as neuroprotective agents for the treatment of Alzheimer's disease. Eur J Med Chem. 2018 Feb 10;145:622-633. doi: 10.1016/j.ejmech.2017.12.080. Epub 2018 Jan 2. PubMed PMID: 29339255. 2: Guo XD, Sun GL, Zhou TT, Wang YY, Xu X, Shi XF, Zhu ZY, Rukachaisirikul V, Hu LH, Shen X. LX2343 alleviates cognitive impairments in AD model rats by inhibiting oxidative stress-induced neuronal apoptosis and tauopathy. Acta Pharmacol Sin. 2017 Aug;38(8):1104-1119. doi: 10.1038/aps.2016.128. Epub 2017 Jun 26. PubMed PMID: 28649128; PubMed Central PMCID: PMC5547549. 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. PubMed PMID: 27569389; PubMed Central PMCID: PMC5057240.