| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Folate-dependent enzymes, such as methionine synthase (MS). 5-Methyltetrahydrofolic acid (5-MTHF) is the primary circulating form of folate and the donor of methyl groups for the conversion of homocysteine to methionine, a reaction catalyzed by methionine synthase (MS) requiring vitamin B12 as a cofactor. This one-carbon metabolism is essential for DNA synthesis, repair, and methylation. The labeled compound serves as a tracer for this pathway.
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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 an internal standard, the 13C-labeled compound has no biological activity of its own. The unlabeled parent, 5-Methyltetrahydrofolic acid (5-MTHF), is the biologically active form of folate. It is a methylated derivative of tetrahydrofolate and is the predominant natural dietary folate and the principal form of folate in plasma and cerebrospinal fluid. It plays an important role in the synthesis of methionine from homocysteine by donating a methyl group. It is also essential for DNA synthesis and repair. |
| ln Vivo |
As an internal standard, the labeled compound is not used for in vivo activity assessment. The unlabeled parent, 5-Methyltetrahydrofolic acid, is essential for normal cellular function. It is used as a dietary supplement to prevent folate deficiency and neural tube defects during pregnancy. In vivo, it reduces homocysteine levels, which is a risk factor for cardiovascular disease. The labeled standard is an analytical tool.
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| Enzyme Assay |
A standard LC-MS/MS protocol is used: a known amount of the 13C5-labeled internal standard is spiked into biological samples (e.g., plasma, urine, tissue). After protein precipitation and solid-phase extraction (SPE), the sample is injected onto a C18 column. The analyte and internal standard are detected in MRM mode. The peak area ratio is used for precise quantification of endogenous or supplemented 5-MTHF.
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| Cell Assay |
For cell-based assays, the internal standard is added to cell homogenates to quantify the cellular uptake and metabolism of folate. Cells are lysed, and the 13C5 internal standard is added. After protein precipitation, the supernatant is analyzed by LC-MS/MS. This allows researchers to study the bioavailability of different folate forms or the effects of drugs on folate metabolism.
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| Animal Protocol |
The internal standard is not administered in animal studies. In a pharmacokinetic or nutritional study, plasma, blood, or tissue samples are collected from animals. The 13C5-labeled internal standard is spiked into these samples before LC-MS/MS analysis. This allows for the accurate measurement of endogenous folate levels or the concentration of a supplemented folate compound. This is essential for studying folate absorption, distribution, metabolism, and excretion (ADME).
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| ADME/Pharmacokinetics |
The compound has a purity of ≥98.0% and is an off-white to light yellow solid. The molecular formula is C1913C5H23N7O6, and the molecular weight is 464.38 (labeled). It is soluble in water and organic solvents such as DMSO and methanol. For storage, the powder should be kept at -20degC, protected from light and moisture. Stable for at least 12 months under recommended conditions.
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| Toxicity/Toxicokinetics |
The labeled compound is non-toxic at the trace concentrations used for analytical purposes. The unlabeled parent, 5-Methyltetrahydrofolic acid, is a naturally occurring vitamin and is considered safe and well-tolerated. High doses may cause gastrointestinal disturbances. The product is "For research use only" and not for human therapeutic or diagnostic use.
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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]. Wright AJ, et al. Comparison of (6 S)-5-methyltetrahydrofolic acid v. folic acid as the reference folate in longer-term human dietary intervention studies assessing the relative bioavailability of natural food folates: comparative changes in folate status following a 16-week placebo-controlled study in healthy adults. Br J Nutr. 2010 Mar;103(5):724-9. |
| Additional Infomation |
5-Methyltetrahydrofolic acid-13C5 is a research-grade stable isotope-labeled chemical used as an internal standard for LC-MS/MS quantitation. It is not a drug and has no FDA approval for therapeutic use. It is used in pharmaceutical research for biomarker quantitation of folate metabolism and to support the development of folate-based therapies. It is an essential tool for method validation in bioanalysis.
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| Molecular Formula |
C1513C5H25N7O6
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|---|---|
| Molecular Weight |
464.42
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| Related CAS # |
5-Methyltetrahydrofolic acid;134-35-0
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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 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) |
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 | 2.1532 mL | 10.7661 mL | 21.5322 mL | |
| 5 mM | 0.4306 mL | 2.1532 mL | 4.3064 mL | |
| 10 mM | 0.2153 mL | 1.0766 mL | 2.1532 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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