| Size | Price | Stock | Qty |
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| 5mg |
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| Other Sizes |
| Targets |
Gamma-aminobutyric acid (GABA), the non-labeled parent compound, binds to ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors) in the adult mammalian brain. The 13C-labeled version retains the same receptor binding properties as the unlabeled compound. GABAA receptors are ligand-gated chloride channels that mediate fast inhibitory neurotransmission, while GABAB receptors are G-protein-coupled receptors that modulate slow inhibitory synaptic transmission. The compound's isotopic labeling does not alter its pharmacodynamic profile, making it a faithful tracer for GABAergic signaling studies. As a stable isotope-labeled reagent, its primary utility is in analytical and metabolic research rather than direct receptor targeting as a therapeutic.
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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].
In vitro, gamma-aminobutyric acid-13C4 is used as a tracer and internal standard in biochemical assays. Stable heavy isotopes of carbon have been incorporated into drug molecules largely as tracers for quantitation during the drug development process. The compound can be added to cell culture media, tissue homogenates, or biological fluids to enable accurate quantification of GABA levels by mass spectrometry. It is used in studies of GABA metabolism, neurotransmitter turnover, and GABAergic signaling pathways. The isotopically labeled compound behaves identically to native GABA in enzymatic and receptor binding assays, allowing for precise measurement of GABA concentrations in complex biological matrices without interference from endogenous GABA. |
| ln Vivo |
In vivo, gamma-aminobutyric acid-13C4 serves as a tracer for studying GABA metabolism and distribution in living organisms. When administered to animals, the 13C-labeled compound can be detected in plasma, cerebrospinal fluid, and brain tissues using mass spectrometry, enabling researchers to track GABA pharmacokinetics and brain penetration. The compound is used in metabolic flux analysis to study GABA synthesis, degradation, and recycling pathways in the central nervous system. Its stable isotope labeling allows for distinction between administered tracer and endogenous GABA, providing valuable insights into GABAergic neurotransmission in health and disease. The compound is not intended for therapeutic use in humans.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays using gamma-aminobutyric acid-13C4 typically involve incubating the compound with GABA receptors or GABA-metabolizing enzymes (GABA transaminase, glutamate decarboxylase) in appropriate buffer systems. The compound is dissolved in aqueous buffer at physiological pH and diluted to working concentrations (typically 0.1-1000 μM). Binding affinity to GABAA or GABAB receptors can be assessed using radioligand displacement assays with tritiated GABA or receptor-specific ligands. Enzyme activity is measured by quantifying the conversion of labeled GABA to its metabolites using LC-MS/MS. The isotopic label enables simultaneous detection of the tracer and its metabolic products, providing detailed kinetic information.
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| Cell Assay |
Cellular assays for gamma-aminobutyric acid-13C4 typically involve culturing neuronal cell lines or primary neurons in growth medium at 37°C with 5% CO₂. Cells are treated with varying concentrations of the labeled compound (typically 0.1-1000 μM) for defined time periods. GABA uptake is measured by quantifying intracellular labeled GABA levels using LC-MS/MS. GABA release assays can be performed by stimulating cells with depolarizing agents and measuring labeled GABA in the extracellular medium. The compound's isotopic label allows for precise quantification of GABA transport and metabolism in cellular systems. Cell viability is assessed using standard assays to ensure effects are not due to toxicity.
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| Animal Protocol |
In vivo animal studies for gamma-aminobutyric acid-13C4 typically involve administering the compound to rodents via intravenous injection, intraperitoneal injection, or oral gavage. Doses are determined based on preliminary pharmacokinetic studies. Blood samples are collected at various time points, and brain tissues are harvested at designated endpoints. Plasma and tissue GABA levels are quantified using LC-MS/MS, with the 13C label allowing for distinction between exogenous tracer and endogenous GABA. Pharmacokinetic parameters such as half-life, volume of distribution, and brain penetration are calculated. The compound is also used in metabolic flux studies to trace GABA synthesis and degradation pathways in vivo.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for gamma-aminobutyric acid-13C4 is consistent with that of unlabeled GABA. The compound has a molecular weight of 107.09 g/mol and a molecular formula of ¹³C₄H₉NO₂. It appears as a solid and is stored at room temperature. GABA is rapidly cleared from the circulation with a short half-life due to efficient uptake by GABA transporters and metabolism by GABA transaminase. The compound is soluble in water and aqueous buffers. As a small polar molecule, GABA does not readily cross the blood-brain barrier, though it can be transported by specific carriers. The isotopic label does not alter the compound's pharmacokinetic properties.
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| Toxicity/Toxicokinetics |
Gamma-aminobutyric acid-13C4 is classified for research use only and is not intended for human or veterinary therapeutic applications. The compound is generally considered safe for laboratory use at typical working concentrations. Standard safety precautions include handling with appropriate personal protective equipment (gloves, lab coat, safety goggles) in a well-ventilated area. The compound should be stored in a dry, cool place away from incompatible materials. Acute toxicity data is not readily available in the public literature. As with all research chemicals, appropriate laboratory safety practices should be followed. No specific LD₅₀ values or detailed toxicological profiles are available in the public domain.
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| References | |
| Additional Infomation |
Gamma-aminobutyric acid-13C4 (4-Aminobutyric acid-13C4, CAS 120728-53-6) is a stable isotope-labeled biochemical reagent with the molecular formula ¹³C₄H₉NO₂. It is the 13C-labeled form of GABA, the major inhibitory neurotransmitter in the adult mammalian brain. The compound is used as a tracer and internal standard for mass spectrometry-based quantification of GABA in biological samples. It is classified as a research-use-only compound not intended for diagnostic or therapeutic purposes. The product is available from multiple commercial suppliers in various pack sizes. No clinical trials or approved drug status exist for this compound as it is not a therapeutic agent. Its applications are limited to analytical chemistry, metabolic research, and neuroscience studies.
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| Molecular Formula |
13C4H9NO2
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|---|---|
| Molecular Weight |
107.09
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| Related CAS # |
γ-Aminobutyric acid;56-12-2
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| Appearance |
White to off-white solid powder
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 :≥ 50 mg/mL (~466.90 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 | 9.3379 mL | 46.6897 mL | 93.3794 mL | |
| 5 mM | 1.8676 mL | 9.3379 mL | 18.6759 mL | |
| 10 mM | 0.9338 mL | 4.6690 mL | 9.3379 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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