| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
The primary target of nebracetam is the muscarinic acetylcholine receptor M1, where it acts as an agonist. It also modulates other neurotransmitter systems, including glutamate and GABA. By activating M1 receptors, it enhances cholinergic neurotransmission, which is important for learning and memory. Nebracetam has an EC50 of 1.59 mM for M1 receptor activation. It may also have antioxidant and anti-apoptotic properties.
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|---|---|
| ln Vitro |
In vitro, nebracetam acts as an M1 receptor agonist with an EC50 of 1.59 mM. It exhibits neuroprotective and cognitive-enhancing activities. It may protect neurons from oxidative stress and apoptosis. The compound is used in cell-based assays to study cholinergic signaling and neuroprotection. However, specific IC50 values for other targets are not publicly available.
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| ln Vivo |
In vivo, nebracetam exhibits neuroprotective and cognitive-enhancing activities. It has been studied in animal models of Alzheimer's disease and other neurological disorders. It improves cognitive function and memory in behavioral tests. However, detailed in vivo efficacy, pharmacokinetic, and toxicity data are not extensively documented in publicly available literature.
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| Enzyme Assay |
For in vitro M1 receptor binding assays, membranes from cells expressing the human M1 receptor are incubated with radiolabeled antagonists (e.g., [3H]N-methylscopolamine) and increasing concentrations of nebracetam. Bound ligand is separated by filtration, and radioactivity is quantified. EC50 values are calculated from dose-response curves. Positive controls include carbachol or oxotremorine.
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| Cell Assay |
For in vitro cell-based assays, cells expressing M1 receptors (e.g., CHO cells) are treated with nebracetam at various concentrations. M1 receptor activation is measured by calcium mobilization or cAMP accumulation. Neuroprotection against amyloid-beta or oxidative stress is evaluated by pretreating primary neuronal cultures with nebracetam before exposure to the insult.
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| Animal Protocol |
For in vivo animal experiments, models of Alzheimer's disease (e.g., amyloid-beta-injected mice or transgenic mice) are used. Nebracetam is administered orally or intraperitoneally at doses determined from pharmacokinetic studies. Behavioral tests (e.g., Morris water maze, novel object recognition) assess cognitive function. Brain tissues are collected for histological analysis of amyloid burden and neuronal loss. All procedures require ethical approval.
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| References |
| Molecular Formula |
C12H16N2O
|
|---|---|
| Molecular Weight |
204.273
|
| Exact Mass |
204.126
|
| CAS # |
97205-34-0
|
| Related CAS # |
:97205-35-1 (fumarate);116041-13-5;1177279-49-0 (HCl)
|
| PubChem CID |
65926
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
1.632
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
15
|
| Complexity |
224
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1C(CN(C1=O)CC2=CC=CC=C2)CN
|
| InChi Key |
LCAFGJGYCUMTGS-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C12H16N2O/c13-7-11-6-12(15)14(9-11)8-10-4-2-1-3-5-10/h1-5,11H,6-9,13H2
|
| Chemical Name |
4-(aminomethyl)-1-benzylpyrrolidin-2-one
|
| Synonyms |
WEB 1881 WEB1881, WEB-1881 Nebracetam
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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 | 4.8955 mL | 24.4774 mL | 48.9548 mL | |
| 5 mM | 0.9791 mL | 4.8955 mL | 9.7910 mL | |
| 10 mM | 0.4895 mL | 2.4477 mL | 4.8955 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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