Glycine transporter type 1 (GlyT1) inhibitor; Positive allosteric modulator of NMDA receptors [1][2]

Sarcosine enhanced NMDA receptor-mediated excitatory postsynaptic field potentials (fEPSPs) in rat hippocampal slices. This potentiation was blocked by the NMDA antagonist AP5, confirming NMDA receptor dependence [2]

Sarcosine (100–300 μM) increased the amplitude and slope of fEPSPs in a concentration-dependent manner without affecting non-NMDA receptor-mediated responses [2]

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Commercial ergot supplements have been made from amino acids and their derivatives. They affect the release of anabolic hormones, the availability of fuel for activity, the ability to think clearly under pressure, and the prevention of muscular damage brought on by exertion. They are regarded as advantageous synergistic food ingredients [1].

In the pentylenetetrazol (PTZ)-induced seizure model, intraperitoneal Sarcosine (600 mg/kg) significantly delayed seizure onset latency (by 48%) and reduced mortality rate (from 100% to 30%) compared to controls [1]

In maximal electroshock (MES) tests, Sarcosine (600 mg/kg i.p.) decreased seizure duration by 35% and protected 40% of mice from tonic hindlimb extension [1]
The electroconvulsive threshold is markedly elevated by Sarcosine (400–800 mg/kg; ip) [2].

Animal/Disease Models: Albino Swiss mouse body weight (25-30 g)[2]
Doses: 100 mg/kg, 200 mg/kg, 400 mg/kg, 800 mg/kg
Route of Administration: intraperitoneal (ip) injection
Experimental Results: in mice MEST In trials, epilepsy thresholds were elevated at doses of 400 mg/kg and 800 mg/kg.

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For PTZ seizures: Mice received PTZ (85 mg/kg, s.c.) 30 min after Sarcosine (300 or 600 mg/kg, i.p.) dissolved in saline. Seizure latency and mortality were monitored for 30 min [1]

For MES seizures: Mice were pretreated with Sarcosine (600 mg/kg i.p.) 30 min before electrical stimulation (50 mA, 0.2 sec). Tonic extension duration and protection rates were recorded [1]

For hippocampal slice studies: Rats were sacrificed, and brain slices (400 μm) were perfused with artificial CSF. fEPSPs were evoked by Schaffer collateral stimulation [2]

Metabolism / Metabolites
Sarcosine is metabolized to glycine by the enzyme sarcosine dehydrogenase, while glycine-N-methyl transferase generates sarcosine from glycine.

Toxicity Summary
Sarcosine is an oncometabolite. Sarcosine appears to upregulate the expression of the potent oncoprotein called human epidermal growth factor receptor 2 (HER2/neu) in androgen-dependent prostate cancer cells upon exposure to exogenous sarcosine. Thus, sarcosine may induce prostate cancer progression by increased HER2/neu expression.

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Toxicity Data
NA

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No mortality or behavioral toxicity (e.g., ataxia, sedation) observed at anticonvulsant doses (≤600 mg/kg) in mice [1]

[1]. Effects of sarcosine, a glycine transporter type 1 inhibitor, in two mouse seizure models. Pharmacol Rep. Mar-Apr 2010;62(2):392-7.

[2]. Effects of sarcosine and N, N-dimethylglycine on NMDA receptor-mediated excitatory field potentials. J Biomed Sci. 2017; 24: 18.

Deliquescent crystals or powder. Has a sweetish taste. (NTP, 1992)
Sarcosine is a N-alkylglycine that is the N-methyl derivative of glycine. It is an intermediate in the metabolic pathway of glycine. It has a role as a glycine transporter 1 inhibitor, a glycine receptor agonist, a human metabolite, an Escherichia coli metabolite and a mouse metabolite. It is a N-alkylglycine, a N-methyl-amino acid and a member of N-methylglycines. It is a conjugate base of a sarcosinium. It is a conjugate acid of a sarcosinate. It is a tautomer of a sarcosine zwitterion.
Sarcosine has been investigated for the treatment of Schizophrenia.
Sarcosine is a metabolite found in or produced by Escherichia coli (strain K12, MG1655).
Sarcosine has been reported in Sarcococca saligna, Drosophila melanogaster, and other organisms with data available.
Sarcosine is an amino acid that is an intermediate and byproduct in glycine synthesis and degradation with potential anti-depressant and anti-schizophrenic activities. Sarcosine is a product of dietary consumption of choline and creatine and is rapidly converted into glycine. Oral administration of sarcosine with certain antipsychotics may cause increased glycine concentration in the brain, which may lead to increased NMDA receptor activation and a reduction in symptoms.
Sarcosine is the N-methyl derivative of glycine. Sarcosine is metabolized to glycine by the enzyme sarcosine dehydrogenase, while glycine-N-methyl transferase generates sarcosine from glycine. Sarcosine is a natural amino acid found in muscles and other body tissues. In the laboratory it may be synthesized from chloroacetic acid and methylamine. Sarcosine is naturally found in the metabolism of choline to glycine. Sarcosine is sweet to the taste and dissolves in water. It is used in manufacturing biodegradable surfactants and toothpastes as well as in other applications. Sarcosine is ubiquitous in biological materials and is present in such foods as egg yolks, turkey, ham, vegetables, legumes, etc. Sarcosine is formed from dietary intake of choline and from the metabolism of methionine, and is rapidly degraded to glycine. Sarcosine has no known toxicity, as evidenced by the lack of phenotypic manifestations of sarcosinemia, an inborn error of sarcosine metabolism. Sarcosinemia can result from severe folate deficiency because of the folate requirement for the conversion of sarcosine to glycine (Wikipedia). Sarcosine has recently been identified as a biomarker for invasive prostate cancer. It was found to be greatly increased during prostate cancer progression to metastasis and could be detected in urine. Sarcosine levels were also increased in invasive prostate cancer cell lines relative to benign prostate epithelial cells (A3519).
An amino acid intermediate in the metabolism of choline.

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Sarcosine (N-methylglycine) is an endogenous glycine derivative that inhibits GlyT1, increasing synaptic glycine levels to potentiate NMDA receptor function [1][2]

Demonstrates anticonvulsant effects in PTZ and MES models, supporting potential therapeutic use in epilepsy [1]

NMDA receptor potentiation suggests applications in neurological disorders involving NMDA hypofunction (e.g., schizophrenia) [2]
An amino acid intermediate in the metabolism of choline.

C3H8CLNO2

125.55

125.024

637-96-7

107-97-1; 2-(Methylamino)acetic acid-d3 hydrochloride;347840-04-4;2-(Methylamino)acetic acid-d5 hydrochloride;1219794-62-3

69483

White to off-white solid powder

1.48 g/cm3

195.1ºC at 760 mmHg

173-175 °C(lit.)

71.8ºC

0.483

3

3

2

7

52.8

0

Cl[H].O([H])C(C([H])([H])N([H])C([H])([H])[H])=O

WVKIFIROCHIWAY-UHFFFAOYSA-N

InChI=1S/C3H7NO2.ClH/c1-4-2-3(5)6;/h4H,2H2,1H3,(H,5,6);1H

2-(methylamino)acetic acid;hydrochloride

Sarcosine hydrochloride; Glycine, N-methyl-, hydrochloride; n-methylglycine hydrochloride; CCRIS 3353; Sarcosine, hydrochloride; EINECS 211-310-2; UNII-W50V8R1ZE9; ...; 637-96-7;

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

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

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.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*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).

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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)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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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).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)