| Size | Price | Stock | Qty |
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| 50g |
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| 100g |
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| Other Sizes |
| Targets |
As a sarcosine derivative, H-Sar-OtBu.HCl does not have a defined primary drug target in the context of therapeutic development. However, sarcosine (N-methylglycine) is known to act as an inhibitor of the glycine transporter GlyT1, which plays a role in glycine reuptake in the central nervous system. By inhibiting GlyT1, sarcosine can increase synaptic glycine levels, potentiating NMDA receptor function. This mechanism has been explored in schizophrenia research, as NMDA receptor hypofunction is implicated in the disorder. The compound may also interact with glycine receptors and other components of the glycine signaling pathway. In peptide synthesis applications, the sarcosine moiety serves as a building block for introducing N-methylated glycine residues into peptide sequences.
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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].
N-methylated amino acid derivatives, including sarcosine-based compounds, have been studied in vitro for their effects on neurotransmitter systems. Sarcosine has been shown to increase extracellular glycine levels in the brain by inhibiting GlyT1, leading to enhanced NMDA receptor activity. In cell-based assays, sarcosine derivatives may be evaluated for their ability to modulate glycine transporter function, NMDA receptor signaling, and neuronal excitability. As a protected sarcosine derivative, this compound may be used in cell-based assays to investigate the effects of N-methylated glycine residues on peptide stability, receptor binding, and biological activity. The compound can also be utilized in studies examining the role of glycine and sarcosine in neurotransmission and psychiatric disorders. |
| ln Vivo |
In vivo studies on sarcosine have demonstrated potential therapeutic effects in schizophrenia models. Sarcosine has been shown to improve cognitive function and reduce negative symptoms in animal models and clinical studies when used as an adjunctive treatment. As a protected sarcosine derivative, this compound may be administered in animal studies to evaluate the effects of sarcosine supplementation or to study the pharmacokinetics and bioavailability of sarcosine derivatives. However, specific in vivo pharmacological data for the tert-butyl ester hydrochloride salt form is limited, as it is primarily supplied as a research chemical for peptide synthesis. Any in vivo effects would be attributed to the active sarcosine released after ester hydrolysis.
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| Enzyme Assay |
Non-cell-based enzyme or receptor binding assays for this compound typically involve studies with purified glycine transporters (GlyT1) or glycine receptors. Standard protocols include radioligand binding assays using membrane preparations from cells expressing recombinant GlyT1 or brain tissue. The compound can be tested for its ability to compete with radiolabeled glycine for transporter binding. For enzyme studies, the compound may be evaluated as a substrate or inhibitor for enzymes involved in sarcosine metabolism, such as sarcosine dehydrogenase, using spectrophotometric or chromatographic detection methods. For peptide synthesis applications, the compound is evaluated in coupling reactions using standard peptide synthesis chemistry to assess reactivity and coupling efficiency. The tert-butyl ester can be removed under acidic conditions (e.g., TFA).
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| Cell Assay |
Cell-based assays for this sarcosine derivative typically utilize neuronal cell lines or primary neurons to evaluate compound effects on glycine transporter function and NMDA receptor activity. Standard protocols involve culturing cells in appropriate media at 37°C in 5% CO₂, followed by treatment with varying concentrations of the compound (typically 0.1-100 μM) for various time periods. Glycine uptake assays using radiolabeled glycine can measure GlyT1 inhibition. NMDA receptor activity can be assessed using calcium imaging or electrophysiological recordings. Cell viability is assessed using MTT or LDH release assays. For peptide synthesis applications, the compound is used as a building block in solid-phase peptide synthesis protocols.
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| Animal Protocol |
In vivo animal studies for sarcosine derivatives typically involve administration via oral gavage, intraperitoneal injection, or intravenous injection in rodent models (mice or rats). Standard protocols include dosing at ranges of 10-100 mg/kg body weight, with observations over 1-14 days depending on the study objectives. For studies evaluating the effects on schizophrenia-related behaviors, animals may be administered the compound and monitored for cognitive performance, social interaction, or prepulse inhibition of startle. Pharmacodynamic assessments may include brain tissue collection for glycine and neurotransmitter measurement, as well as monitoring of body weight and general health parameters. All animal studies must comply with institutional ethical guidelines and be conducted in accordance with applicable regulations.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties for this sarcosine ester can be inferred from structurally related compounds. As a small molecule (molecular weight 181.66 g/mol), it is expected to have reasonable oral bioavailability. The tert-butyl ester is likely to be hydrolyzed in vivo to release the active sarcosine. The hydrochloride salt form enhances aqueous solubility. For in vivo administration, formulations using suitable vehicles may be employed. The compound is stable at room temperature during shipping and should be stored as powder at -20°C for long-term preservation. Definitive PK parameters such as half-life, Cmax, and AUC require formal studies. The compound's metabolism likely involves ester hydrolysis followed by sarcosine metabolism via sarcosine dehydrogenase.
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| Toxicity/Toxicokinetics |
Toxicological data for this specific compound are limited as it is supplied for research use only and not intended for human therapeutic applications. Sarcosine is a naturally occurring compound and is generally considered to have low inherent toxicity. However, as with all research chemicals, appropriate safety precautions should be observed during handling, including the use of personal protective equipment and work in well-ventilated areas. The compound may cause skin and eye irritation upon contact. Acute toxicity studies in animal models would be required to establish LD₅₀ values and no-observed-adverse-effect levels. For in vitro cytotoxicity assessment, the compound can be tested in mammalian cell lines using standard MTT or LDH release assays.
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| References | |
| Additional Infomation |
H-Sar-OtBu.HCl is a sarcosine derivative featuring a tert-butyl ester protecting group. Sarcosine (N-methylglycine) is a naturally occurring amino acid derivative that acts as an inhibitor of the glycine transporter GlyT1 and has been studied in the context of schizophrenia and other neurological disorders. The tert-butyl ester protects the C-terminus during peptide synthesis, allowing for selective deprotection under acidic conditions. This compound is used as a building block in solid-phase peptide synthesis for introducing N-methylated glycine residues into peptide sequences. It is not an approved drug and has not undergone clinical trials as a therapeutic agent; it is strictly for research purposes. The compound's mechanism of action, when studied, relates to its role as a sarcosine precursor or as a building block for sarcosine-containing peptides.
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| Molecular Formula |
C7H16CLNO2
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|---|---|
| Molecular Weight |
181.66
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| Exact Mass |
181.086
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| CAS # |
136088-69-2
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| PubChem CID |
11252350
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| Appearance |
White to off-white solid powder
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| Boiling Point |
168.5ºC at 760 mmHg
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| Flash Point |
55.7ºC
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| LogP |
1.74
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
11
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| Complexity |
115
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl[H].O(C(C([H])([H])N([H])C([H])([H])[H])=O)C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H]
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| InChi Key |
RNLQHMIDSCYLAK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C7H15NO2.ClH/c1-7(2,3)10-6(9)5-8-4;/h8H,5H2,1-4H3;1H
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| Chemical Name |
tert-butyl 2-(methylamino)acetate;hydrochloride
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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: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 | 5.5048 mL | 27.5239 mL | 55.0479 mL | |
| 5 mM | 1.1010 mL | 5.5048 mL | 11.0096 mL | |
| 10 mM | 0.5505 mL | 2.7524 mL | 5.5048 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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