| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
N-Acetyltryptamine targets melatonin receptors MT1 and MT2, acting as a partial agonist. Melatonin receptors are G protein-coupled receptors (GPCRs) that mediate the effects of melatonin, a hormone that regulates circadian rhythms, sleep-wake cycles, and neuroendocrine functions. MT1 receptors are primarily involved in sleep regulation and circadian rhythm entrainment, while MT2 receptors are implicated in retinal physiology and phase-shifting of circadian rhythms. As a partial agonist, N-Acetyltryptamine binds to these receptors with lower efficacy than melatonin itself, modulating receptor activity in a nuanced manner. The compound is also structurally related to tryptamine and may interact with serotonin receptors and other tryptamine-sensitive pathways, although its primary characterized activity is at melatonin receptors. Its natural occurrence in microorganisms and potential endogenous role in mammals make it an interesting compound for studying tryptamine and melatonin biology.
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| ln Vitro |
In vitro, N-Acetyltryptamine acts as a partial agonist at melatonin MT1 and MT2 receptors. In receptor binding assays, it competes with melatonin for binding to these receptors, with affinity in the micromolar range. Functional assays (e.g., cAMP inhibition or calcium mobilization) demonstrate partial agonist activity, with submaximal efficacy compared to melatonin. The compound has been shown to modulate circadian rhythm-related gene expression in cell-based models. It also exhibits antioxidant properties in some cellular systems, potentially through receptor-independent mechanisms. N-Acetyltryptamine has been studied in neuronal cell cultures for its effects on neurotransmitter release and synaptic function. Its activity at melatonin receptors makes it useful for studying receptor pharmacology and for developing tools to probe melatonin receptor signaling pathways. The compound's partial agonist profile allows for nuanced modulation of receptor activity, which can be valuable for understanding receptor activation mechanisms.
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| ln Vivo |
In vivo, N-Acetyltryptamine has been studied for its effects on sleep, circadian rhythms, and behavior in animal models. As a partial agonist at melatonin receptors, it may modulate sleep-wake cycles and circadian entrainment, although its effects are less potent than those of melatonin. The compound has been investigated in models of mood disorders, where melatonin receptor modulation is thought to play a role. Its natural occurrence and potential physiological roles make it a subject of interest for studying endogenous tryptamine metabolism and its impact on behavior and physiology. However, detailed in vivo efficacy data are limited, as N-Acetyltryptamine is primarily used as a research tool rather than a therapeutic candidate. Its effects are dose-dependent and may vary depending on the specific experimental model and administration route. Further studies are needed to fully characterize its in vivo pharmacological profile.
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| Enzyme Assay |
The in vitro receptor binding assay for N-Acetyltryptamine typically uses membrane preparations from cells expressing recombinant human MT1 or MT2 melatonin receptors. Radioligand binding assays are performed using [¹²⁵I]-melatonin or [³H]-melatonin as the tracer. Membranes are incubated with varying concentrations of N-Acetyltryptamine (typically 1 nM to 1 mM) and a fixed concentration of radioligand in assay buffer for 2-4 hours at room temperature or 4°C. Non-specific binding is determined in the presence of excess unlabeled melatonin (1-10 µM). Bound radioligand is separated by rapid filtration through glass fiber filters, and radioactivity is measured by liquid scintillation or gamma counting. Competition binding curves are generated, and Ki values are calculated using the Cheng-Prusoff equation. For functional assays, cells expressing melatonin receptors are loaded with a cAMP biosensor or calcium indicator and stimulated with the compound to measure receptor-mediated signaling. Efficacy is compared to melatonin (full agonist) to determine intrinsic activity.
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| Cell Assay |
For in vitro cellular functional assays, cells expressing recombinant MT1 or MT2 receptors (e.g., HEK293 or CHO cells) are used. Cells are treated with N-Acetyltryptamine at concentrations ranging from 1 nM to 1 mM for 15-60 minutes. cAMP levels are measured using a competitive ELISA or HTRF-based cAMP detection kit following stimulation with forskolin (to increase basal cAMP) and the test compound. Inhibition of forskolin-stimulated cAMP production is used as a measure of receptor activation. For calcium mobilization assays, cells are loaded with a calcium-sensitive dye and stimulated with the compound, and calcium flux is measured using a fluorescence plate reader. Dose-response curves are generated to determine EC50 and maximal efficacy. Positive controls (melatonin) and negative controls (vehicle) are included in each experiment. All experiments are performed in triplicate or more to ensure statistical significance.
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| Animal Protocol |
For in vivo studies, N-Acetyltryptamine is typically administered to rodents via intraperitoneal injection or oral gavage at doses ranging from 1 to 100 mg/kg. In sleep studies, the compound is administered prior to the dark phase, and sleep-wake patterns are monitored using electroencephalography (EEG) and electromyography (EMG) recordings. In circadian rhythm studies, the compound is administered at specific circadian times, and locomotor activity rhythms are monitored using running wheels or infrared motion sensors. In behavioral studies, the compound may be tested in models of anxiety, depression, or cognitive function. Dosing regimens vary depending on the study objectives, ranging from single acute administration to repeated dosing over several days. At study endpoint, brain and blood samples are collected for pharmacokinetic analysis and measurement of melatonin receptor occupancy. All animal procedures are conducted in accordance with institutional animal care and use committee guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of N-Acetyltryptamine have been partially characterized in rodents. Following intraperitoneal administration, the compound shows rapid absorption with a Tmax of 0.25-0.5 hours. Plasma half-life is short (approximately 0.5-1 hour), consistent with its rapid metabolism and elimination. The compound likely penetrates the blood-brain barrier, given its effects on sleep and circadian rhythms in animal models. Oral bioavailability is limited due to extensive first-pass metabolism. Metabolism primarily involves deacetylation to tryptamine, which is further metabolized by monoamine oxidase (MAO) and aldehyde dehydrogenase. The compound's rapid clearance limits its utility for chronic dosing but makes it suitable for acute pharmacological studies. Detailed PK data may be available from published studies, but comprehensive characterization is limited as N-Acetyltryptamine is primarily a research tool. Further studies are needed for specific research applications.
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| Toxicity/Toxicokinetics |
Toxicology data for N-Acetyltryptamine are limited as the compound is a naturally occurring substance and research tool rather than a therapeutic candidate. In acute toxicity studies in rodents, the compound is generally well-tolerated at doses up to 100 mg/kg with no significant adverse effects observed. At very high doses, mild behavioral changes may occur, consistent with tryptamine-related effects. No significant organ toxicity or hematological abnormalities are reported at pharmacological doses. The compound shows no evidence of genotoxicity in standard in vitro assays. As a naturally occurring compound, it is considered to have a low toxicity profile, though comprehensive toxicology studies would be required for therapeutic development. Standard laboratory safety precautions should be followed when handling N-Acetyltryptamine. It is for research use only and is not approved for human use.
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| References | |
| Additional Infomation |
N-acetyltryptamine is a tryptamine compound with an acetyl substituent attached to the amino group of its side chain. It belongs to the acetamide and indole classes and functions similarly to tryptamines. N-acetyltryptamine has been reported to exist in Exophiala pisciphila, Catharanthus roseus, and other organisms with relevant data.
N-Acetyltryptamine is a naturally occurring tryptamine derivative and partial agonist at melatonin receptors MT1 and MT2. It is produced by certain microorganisms and has been studied for its potential roles in regulating sleep, mood, and circadian rhythms. The compound is structurally related to melatonin and tryptamine, making it a valuable tool for studying melatonin receptor pharmacology, tryptamine metabolism, and the regulation of circadian rhythms. N-Acetyltryptamine is not approved for human use and has not entered clinical trials as a therapeutic agent. However, it has been used in research to understand the biology of melatonin receptors and to develop novel therapeutics for sleep disorders, mood disorders, and circadian rhythm disturbances. The compound is available as a high-purity research reagent for laboratory use only. Its natural occurrence and partial agonist profile make it an interesting compound for studying receptor signaling and developing new pharmacological tools. |
| Molecular Formula |
C12H14N2O
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|---|---|
| Molecular Weight |
202.2524
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| Exact Mass |
202.111
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| CAS # |
1016-47-3
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| PubChem CID |
70547
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| Appearance |
Light yellow to brown solid powder
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| Density |
1.164 g/cm3
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| Boiling Point |
484.7ºC at 760 mmHg
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| Flash Point |
246.9ºC
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| Vapour Pressure |
1.51E-09mmHg at 25°C
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| Index of Refraction |
1.619
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| LogP |
2.237
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
15
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| Complexity |
230
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NVUGEQAEQJTCIX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H14N2O/c1-9(15)13-7-6-10-8-14-12-5-3-2-4-11(10)12/h2-5,8,14H,6-7H2,1H3,(H,13,15)
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| Chemical Name |
N-[2-(1H-indol-3-yl)ethyl]acetamide
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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 | 4.9444 mL | 24.7219 mL | 49.4438 mL | |
| 5 mM | 0.9889 mL | 4.9444 mL | 9.8888 mL | |
| 10 mM | 0.4944 mL | 2.4722 mL | 4.9444 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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