| Size | Price | Stock | Qty |
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| 500mg |
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| Other Sizes |
| Targets |
Glycylsarcosine targets peptide transporters, particularly the proton-coupled oligopeptide transporters PEPT1 and PEPT2. It serves as a model substrate for studying the mechanisms of these transporters due to its stability and resistance to hydrolysis by peptidases. The compound is used to investigate the substrate specificity, transport kinetics, and regulation of peptide transporters. It does not have a therapeutic target but is a valuable research tool for studying peptide transport and absorption in the intestine and kidney.
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| ln Vitro |
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 vitro, Glycylsarcosine is used as a substrate in cellular assays to study peptide transporter activity. It is commonly employed in transport studies using cell lines such as Caco-2 cells, which express PEPT1, or in isolated membrane vesicles. The uptake of Gly-Sar is measured to assess transporter function, and its transport kinetics (Km, Vmax) are determined. The compound's stability against enzymatic hydrolysis makes it an ideal substrate for these studies. It does not exhibit pharmacological activities such as receptor binding or enzyme inhibition. |
| ln Vivo |
Glycylsarcosine is not a pharmacologically active compound and therefore does not have defined in vivo activity as a therapeutic agent. When administered to animals, it is used as a probe to study peptide transporter function in vivo. It is absorbed via PEPT1 in the intestine and can be used to assess the bioavailability of peptide-based drugs. Its in vivo effects are limited to its utility as a transport substrate. Its primary value remains in research, where it serves as a tool for studying peptide absorption and drug delivery.
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| Enzyme Assay |
In vitro receptor binding assays are not applicable for Glycylsarcosine, as it does not target a receptor. Instead, transport assays are performed to study its interaction with peptide transporters. A standard protocol involves incubating cells expressing PEPT1 or PEPT2 with radiolabeled or fluorescently labeled Gly-Sar. The uptake is measured over time, and the effect of inhibitors or competitors is assessed. The transport kinetics are calculated, and the specificity of the transporter is characterized. These assays are used to screen for compounds that modulate peptide transporter activity.
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| Cell Assay |
In vitro cellular assays for Glycylsarcosine are conducted to study peptide transporter function. A typical protocol involves culturing cells that express peptide transporters, such as Caco-2 or MDCK cells, in multi-well plates. Cells are incubated with Gly-Sar at varying concentrations, and the intracellular accumulation of the dipeptide is measured. The uptake is quantified by HPLC or using radiolabeled or fluorescently labeled Gly-Sar. The effect of pH, inhibitors, and other substrates on transport is assessed. These assays are used to characterize the substrate specificity and kinetics of peptide transporters.
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| Animal Protocol |
In vivo animal studies with Glycylsarcosine are conducted to investigate peptide transporter function and drug absorption. A typical protocol involves oral or intravenous administration of the compound to rodents, followed by blood and tissue sampling. The concentration of Gly-Sar in plasma and tissues is measured to assess its absorption, distribution, and elimination. The compound's bioavailability and the role of peptide transporters in its disposition are evaluated. These studies help to understand the mechanisms of peptide absorption and to predict the oral bioavailability of peptide-based drugs.
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| ADME/Pharmacokinetics |
As a small, stable dipeptide, Glycylsarcosine is expected to be absorbed via PEPT1 in the intestine after oral administration. Its pharmacokinetic properties are characterized by rapid absorption and distribution. The compound is resistant to hydrolysis by peptidases, contributing to its stability in the gastrointestinal tract and plasma. It is primarily excreted unchanged in the urine. The pharmacokinetic profile of Gly-Sar is used as a model to study the absorption and disposition of peptide-based drugs. Detailed PK data are available in the literature for specific experimental conditions.
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| Toxicity/Toxicokinetics |
Glycylsarcosine is generally considered to have low toxicity, consistent with its use as a research reagent. It is a dipeptide composed of the endogenous amino acids glycine and sarcosine. Acute toxicity is expected to be minimal. The compound may cause mild irritation upon contact with skin, eyes, or mucous membranes. It is not classified as a carcinogen, mutagen, or reproductive toxicant. Standard laboratory safety precautions, including the use of personal protective equipment, are recommended. No significant systemic toxicity is anticipated at typical research doses.
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| References | |
| Additional Infomation |
Glycylsarcosine is a dipeptide formed by the condensation of the carboxyl group of glycine and the amino group of sarcosine. It is the zwitterion tautomer of glycylsarcosine.
Glycylsarcosine (Gly-Sar, CAS 29816-01-1) is a dipeptide composed of glycine and sarcosine. It is a white powder with a molecular formula of C₅H₁₀N₂O₃ and a molecular weight of 146.14 g/mol. It is widely used as a model substrate for studying peptide transporters such as PEPT1 and PEPT2 due to its stability and resistance to hydrolysis. It is a valuable research tool for investigating peptide absorption, drug delivery, and transporter function, but it is not an approved drug for therapeutic use. |
| Molecular Formula |
C5H10N2O3
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|---|---|
| Molecular Weight |
146.1445
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| Exact Mass |
146.069
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| CAS # |
29816-01-1
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| PubChem CID |
93131
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| Appearance |
White to off-white solid powder
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| Density |
1.284g/cm3
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| Boiling Point |
333.5ºC at 760mmHg
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| Melting Point |
198-202 °C (dec.)
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| Flash Point |
155.5ºC
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| Vapour Pressure |
2.6E-05mmHg at 25°C
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| Index of Refraction |
1.51
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| LogP |
-3.9
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
10
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| Complexity |
146
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C([H])([H])N([H])[H])N(C([H])([H])[H])C([H])([H])C(=O)O[H]
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| InChi Key |
VYAMLSCELQQRAE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C5H10N2O3/c1-7(3-5(9)10)4(8)2-6/h2-3,6H2,1H3,(H,9,10)
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| Chemical Name |
2-[(2-aminoacetyl)-methylamino]acetic acid
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
H2O : ~41.67 mg/mL (~285.12 mM)
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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 | 6.8428 mL | 34.2138 mL | 68.4275 mL | |
| 5 mM | 1.3686 mL | 6.8428 mL | 13.6855 mL | |
| 10 mM | 0.6843 mL | 3.4214 mL | 6.8428 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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