| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
ASS234 targets multiple enzymes relevant to Alzheimer's disease: monoamine oxidase A (MAO-A), monoamine oxidase B (MAO-B), acetylcholinesterase (AChE), and butyrylcholinesterase (BuChE). By inhibiting MAO-A and MAO-B, it increases the levels of monoamine neurotransmitters such as serotonin, dopamine, and norepinephrine. By inhibiting AChE and BuChE, it increases acetylcholine levels. This multitarget approach is designed to address the complex pathophysiology of Alzheimer's disease.
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| ln Vitro |
In vitro, ASS234 is a potent MAO inhibitor with IC50 values of 5.2 nM for MAO-A and 43 nM for MAO-B. It also inhibits AChE and BuChE with IC50 values of 350 nM and 460 nM, respectively. Its multi-target activity has been characterized in various biochemical and cell-based assays.
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| ln Vivo |
In vivo, ASS234 has been studied in preclinical models of Alzheimer's disease. Its ability to inhibit MAO, AChE, and BuChE contributes to its potential cognitive-enhancing and neuroprotective effects. The compound is designed to cross the blood-brain barrier.
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| Enzyme Assay |
The activity of ASS234 can be assessed using cell-free enzyme assays. MAO-A and MAO-B activities are measured by incubating the enzymes with a substrate (e.g., kynuramine) and varying concentrations of ASS234. The production of metabolites is measured spectrophotometrically. AChE and BuChE activities are measured using the Ellman's assay. The IC50 values for each enzyme are determined from dose-response curves.
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| Cell Assay |
To evaluate the cellular effects of ASS234, neuronal cells are treated with the compound. The inhibition of MAO and cholinesterase activities is measured in cell lysates. The effects on neurotransmitter levels, cell viability, and neuroprotection are assessed. The compound's effects on amyloid-beta toxicity and tau phosphorylation can also be evaluated in relevant cell models.
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| Animal Protocol |
In vivo studies with ASS234 typically involve administration to animal models via oral or intraperitoneal routes. In models of Alzheimer's disease, the compound's effects on cognitive function, neuroinflammation, amyloid pathology, and neurodegeneration are assessed. Its effects on neurotransmitter levels in the brain are measured.
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| ADME/Pharmacokinetics |
ASS234 has a molecular formula of C29H37N3O and a molecular weight of 443.62 g/mol. Its CAS number is 1334106-34-1. It appears as a white to off-white solid powder. It is soluble in DMSO. The purity is ≥98%. It should be stored at -20°C.
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| Toxicity/Toxicokinetics |
Specific toxicology data for ASS234 are not extensively detailed in the available literature. As with all research compounds, standard safety precautions should be taken when handling ASS234. It is intended for research use only and is not for human consumption.
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| Additional Infomation |
ASS234 is a multitarget directed propargylamine for Alzheimer's disease therapy. It is a potent MAO-A/B inhibitor and also inhibits AChE and BuChE. Its multi-target activity makes it a promising candidate for the treatment of Alzheimer's disease. It is a research tool for studying multitarget approaches to neurodegenerative diseases.
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| Molecular Formula |
C29H37N3O
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|---|---|
| Molecular Weight |
443.623587369919
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| Exact Mass |
443.293
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| CAS # |
1334106-34-1
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| PubChem CID |
53378764
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
582.5±45.0 °C at 760 mmHg
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| Flash Point |
306.1±28.7 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.573
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| LogP |
5.74
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
33
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| Complexity |
616
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(C1C=CC2=C(C=C(CN(C)CC#C)N2C)C=1)CCCC1CCN(CC2C=CC=CC=2)CC1
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| InChi Key |
ADCBAOTWERXLAP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C29H37N3O/c1-4-16-30(2)23-27-20-26-21-28(12-13-29(26)31(27)3)33-19-8-11-24-14-17-32(18-15-24)22-25-9-6-5-7-10-25/h1,5-7,9-10,12-13,20-21,24H,8,11,14-19,22-23H2,2-3H3
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| Chemical Name |
N-[[5-[3-(1-benzylpiperidin-4-yl)propoxy]-1-methylindol-2-yl]methyl]-N-methylprop-2-yn-1-amine
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2542 mL | 11.2709 mL | 22.5418 mL | |
| 5 mM | 0.4508 mL | 2.2542 mL | 4.5084 mL | |
| 10 mM | 0.2254 mL | 1.1271 mL | 2.2542 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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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