| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 500mg | |||
| 1g | |||
| Other Sizes |
| Targets |
Not defined; it reduces reactive oxygen species (ROS) and oxidative stress. The exact molecular target of LZWL02003 is not specified. It acts as an anti-neuroinflammatory and neuroprotective agent. It has been shown to reduce LPS-induced nitric oxide production in microglial cells (IC50s of 7.48 and 4.94 uM in C6 and BV-2 cells, respectively), indicating an effect on inflammatory pathways like iNOS. It also protects against MPP+-induced damage, suggesting an effect on mitochondrial function or oxidative stress pathways.
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| ln Vitro |
LZWL02003 has a protective effect on MPP+-induced neuronal damage and reduces the expression of ROS. It significantly reduces LPS-induced nitric oxide (NO) production in C6 rat glioma cells (IC50 = 7.48 uM) and BV-2 mouse microglia (IC50 = 4.94 uM). It is a derivative of N-salicyloyl tryptamine with improved neuroprotective properties.
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| ln Vivo |
LZWL02003 improves cognition, memory, learning, and athletic ability in a Rotenone-induced Parkinson's disease (PD) rat model. This suggests in vivo efficacy and indicates its potential for neurodegenerative disease research. It effectively crosses the blood-brain barrier to exert its neuroprotective effects.
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| Enzyme Assay |
LZWL02003 is an anti-neuroinflammatory agent. For binding or target engagement studies, the exact target is unknown. A typical protocol to study its anti-inflammatory activity involves using a cell-free iNOS (inducible nitric oxide synthase) activity assay. The enzyme is incubated with LZWL02003 (1-100 uM) in an assay buffer. The reaction is initiated with L-arginine and NADPH. After 60 minutes, the concentration of nitrite (a stable product of NO) is measured using the Griess reaction. A decrease in nitrite concentration indicates iNOS inhibition. However, more targeted studies would be required to identify a specific binding site.
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| Cell Assay |
For in vitro cellular studies, murine BV-2 microglial cells or rat C6 glioma cells are seeded in 96-well plates (1×10⁴ cells/well). To induce inflammation, cells are treated with lipopolysaccharide (LPS, 1 ug/mL) for 24 hours. LZWL02003 (1-100 uM) is co-administered with LPS. After 24 hours, the culture supernatant is collected. Nitric oxide (NO) levels are measured by the Griess reaction, and pro-inflammatory cytokines (TNF-alpha, IL-6) are measured by ELISA. To assess neuroprotection, SH-SY5Y cells are treated with MPP+ (1-methyl-4-phenylpyridinium, 500 uM) to induce a Parkinson's-like state. LZWL02003 (1-100 uM) is added, and cell viability is measured by MTT after 48 hours. ROS levels are measured using the DCFH-DA fluorescent probe.
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| Animal Protocol |
A typical in vivo protocol uses the rotenone-induced Parkinson's disease (PD) rat model. Male Sprague-Dawley rats (200-250 g) are administered rotenone (1 mg/kg/day, s.c.) for 4 weeks. LZWL02003 is administered daily via intraperitoneal (i.p.) injection at a dose of 5-20 mg/kg, either prophylactically (starting before rotenone) or therapeutically. Behavioral testing (open field test for locomotion, rotarod for motor coordination, and Morris water maze for learning and memory) is performed during weeks 3 and 4 of treatment. At the study's conclusion, rats are sacrificed, and brain regions (striatum, substantia nigra) are analyzed for tyrosine hydroxylase (TH) expression (a marker of dopaminergic neurons) by immunohistochemistry, and for levels of inflammatory cytokines (IL-6, TNF-alpha) by qPCR. Blood and brain levels of the compound can be measured by LC-MS.
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| ADME/Pharmacokinetics |
No pharmacokinetic data has been reported. As a small molecule with a molecular weight of 294.35 g/mol (C18H18N2O2), and given its neuroprotective activity, it is speculated to have the ability to cross the blood-brain barrier (BBB) to exert its effects. However, its oral bioavailability, plasma half-life, and volume of distribution are unknown and should be determined experimentally.
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| Toxicity/Toxicokinetics |
No specific toxicity data has been reported. In the in vitro studies, LZWL02003 appears to be well-tolerated at the active concentrations (1-100 uM). In the rat rotenone model, repeated doses of 5-20 mg/kg i.p. for several weeks did not appear to cause significant adverse effects (no body weight loss or mortality was reported). However, full toxicological profiling has not been conducted. It is for research use only.
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| References |
1: Su JH, Wu GP, Peng X, Zhao GQ, Peng Y, Zhang HH, Zhao YT, Sun R, Chen ST, Tian Y, Wang Z. Neuroprotective Effects of an N-Salicyloyl Tryptamine Derivative against Cerebral Ischemia/Reperfusion Injury. ACS Chem Neurosci. 2023 Jun 7;14(11):2146-2158. doi: 10.1021/acschemneuro.3c00149. Epub 2023 May 11. PMID: 37170554. 2: Li X, Wang S, Duan S, Long L, Zhuo L, Peng Y, Xiong Y, Li S, Peng X, Yan Y, Wang Z, Jiang W. Exploring the Therapeutic Effects of Multifunctional N-Salicylic Acid Tryptamine Derivative against Parkinson's Disease. ACS Omega. 2023 Jul 28;8(31):28910-28923. doi: 10.1021/acsomega.3c04277. PMID: 37576637; PMCID: PMC10413456.
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| Additional Infomation |
LZWL02003, also known as p-methyl-N-salicyloyl Tryptamine, is a research compound for neuroinflammation and Parkinson's disease. It is a derivative of N-salicyloyl tryptamine, which is known to have neuroprotective and anti-inflammatory properties. This compound is a small molecule with the chemical name N-((1H-indol-3-yl)methyl)-2-hydroxy-4-methylbenzamide. It is not approved for clinical use. Its IUPAC name is 2-hydroxy-4-methyl-N-(2-(1H-indol-3-yl)ethyl)benzamide.
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| Exact Mass |
294.14
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|---|---|
| Elemental Analysis |
C, 73.45; H, 6.16; N, 9.52; O, 10.87
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| CAS # |
1371564-45-2
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| Appearance |
White to off-white solid powder
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| SMILES |
O=C(C1=C(O)C=C(C)C=C1)NCCC2=CNC3=CC=CC=C32
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| InChi Key |
IIXQVHOWQHXBKW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H18N2O2/c1-12-6-7-15(17(21)10-12)18(22)19-9-8-13-11-20-16-5-3-2-4-14(13)16/h2-7,10-11,20-21H,8-9H2,1H3,(H,19,22)
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| Chemical Name |
N-(2-(1H-indol-3-yl)ethyl)-2-hydroxy-4-methylbenzamide
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| Synonyms |
LZWL02003; LZWL-02003; LZWL 02003; p-methyl-N-salicyloyl Tryptamine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~339.7 mM; with ultrasonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.49 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.49 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (8.49 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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