| Size | Price | |
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| 1mg | ||
| Other Sizes |
| Targets |
Sweet taste receptors, specifically the T1R2/T1R3 heterodimeric G protein-coupled receptor (GPCR) expressed in taste buds on the tongue. Upon binding to the sweet taste receptor, neotame activates downstream G protein signaling pathways, leading to taste perception of sweetness. The (R)-enantiomer is one of the two stereoisomers of neotame, with the racemic mixture or specific isomer being used in food applications.
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| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as tracers for quantification throughout the drug development process. Due to its potential to alter the pharmacokinetic and metabolic characteristics of medications, deuteration has drawn attention[1].
As a deuterated internal standard, (R)-Neotame-d3 is not assessed for biological activity in the same way as a drug candidate. The non-deuterated neotame is a potent sweetener, activating the T1R2/T1R3 sweet taste receptor with high efficacy. Neotame is a methyl ester derivative of the dipeptide N-(3,3-dimethylbutyl)-L-alpha-aspartyl-L-phenylalanine. It is metabolized differently from aspartame, reducing the phenylalanine burden for individuals with phenylketonuria (PKU). |
| ln Vivo |
As a deuterated internal standard, (R)-Neotame-d3 is not intended for in vivo administration as a therapeutic. The non-deuterated neotame is used as a food additive (sweetener) and is not administered as a drug. Following oral consumption, neotame is rapidly absorbed from the gastrointestinal tract and metabolized primarily via ester hydrolysis to de-esterified neotame, which is excreted in the urine and feces. No therapeutic in vivo activity is relevant for this compound.
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| Enzyme Assay |
For analytical method development, neotame and its deuterated internal standard (R)-Neotame-d3 are analyzed by LC-MS/MS. A fixed concentration of the internal standard is added to all samples (standards, quality controls, and test samples) at the beginning of sample preparation. After protein precipitation or solid-phase extraction (SPE), the supernatant is injected onto a C18 reversed-phase column. The analyte and internal standard are detected in multiple reaction monitoring (MRM) mode, and peak area ratios are used for quantification.
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| Cell Assay |
A typical sample preparation protocol involves adding a known amount of (R)-Neotame-d3 internal standard to food or beverage samples. Samples are extracted with a mixture of water and organic solvent (e.g., acetonitrile or methanol), vortex-mixed, sonicated, and centrifuged. The supernatant may be diluted and filtered before injection into LC-MS/MS. Calibration curves are prepared by spiking known concentrations of non-deuterated neotame into blank matrix with fixed internal standard. Linearity (R2 >0.99), accuracy (85-115%), and precision (CV<15%) are required.
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| Animal Protocol |
For in vivo pharmacokinetic studies of neotame, laboratory animals (typically rats or dogs) are orally administered neotame. Blood samples are collected at predetermined time points (pre-dose, 0.25, 0.5, 1, 2, 4, 6, 8, 12, 24 hours post-dose). Plasma is separated by centrifugation. A fixed concentration of (R)-Neotame-d3 internal standard is added to each plasma sample before protein precipitation. After centrifugation, the supernatant is analyzed by LC-MS/MS to quantify neotame concentrations. Pharmacokinetic parameters are calculated by non-compartmental analysis.
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| ADME/Pharmacokinetics |
(R)-Neotame-d3 itself is not administered, but neotame (the non-deuterated sweetener) has known oral bioavailability in humans. Following oral consumption, neotame is rapidly and nearly completely absorbed from the gastrointestinal tract. It is extensively metabolized by esterases to de-esterified neotame, which is the primary circulating metabolite. Plasma protein binding of neotame is low. The half-life of neotame is short (approximately 2-6 hours). The compound is eliminated primarily through urinary excretion of metabolites.
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| Toxicity/Toxicokinetics |
Neotame is approved by the FDA as a general-purpose sweetener and has an extensive safety database. The acceptable daily intake (ADI) for neotame is 0-2 mg/kg body weight per day, as established by the FDA and JECFA. In toxicology studies, no carcinogenic, teratogenic, or genotoxic effects have been observed. Unlike aspartame, neotame does not produce phenylalanine during metabolism, making it safe for individuals with phenylketonuria (PKU). No significant adverse effects have been reported at approved consumption levels.
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| References |
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. Liang Chi, et al. Effects of the Artificial Sweetener Neotame on the Gut Microbiome and Fecal Metabolites in Mice. Molecules. 2018 Feb 9;23(2):367. [3]. Anuradha Kumari, et al. Stability of Aspartame and Neotame in Pasteurized and In-Bottle Sterilized Flavoured Milk. Food Chem. 2016 Apr 1;196:533-8. |
| Additional Infomation |
Neotame was approved by the US FDA in 2002 as a non-nutritive sweetener for use in foods and beverages. It is also approved in the EU, Australia, New Zealand, Canada, China, Mexico, and other countries. Neotame is approximately 7,000-13,000 times sweeter than sucrose. It is heat-stable and suitable for cooking and baking. Unlike other artificial sweeteners, neotame does not leave a bitter aftertaste. This deuterated (d3) form is for research use only and is not a food additive. The product is an analytical standard, not for human consumption.
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| Molecular Formula |
C20H27D3N2O5
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|---|---|
| Molecular Weight |
381.48
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| Related CAS # |
Neotame;165450-17-9
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| Appearance |
Typically exists as solid at room temperature
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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 | 2.6214 mL | 13.1068 mL | 26.2137 mL | |
| 5 mM | 0.5243 mL | 2.6214 mL | 5.2427 mL | |
| 10 mM | 0.2621 mL | 1.3107 mL | 2.6214 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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