| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g | |||
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| Other Sizes |
Purity: ≥98%
| Targets |
Prefolic A targets the folate biosynthetic pathway. As a pteridine derivative, it is a precursor in the synthesis of folic acid and related compounds. It is involved in the pteridine branch of the folate pathway and is converted to dihydropteroate and then to folate. It is used as a substrate for enzymes involved in folate biosynthesis.
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| ln Vitro |
In vitro, Prefolic A is used as a substrate for enzymes involved in folate biosynthesis. It is converted to dihydropteroate by dihydropteroate synthase and then to folate by dihydrofolate synthase. It is also used in studies of pteridine metabolism and as a reference standard in analytical chemistry.
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| ln Vivo |
In healthy adults aged 18-65 years, oral administration of Prefolic A at 453 nmol/d for 16 weeks resulted in a mean increase in plasma folate concentration of 15.10 nmol/l (SEM 1.94), an increase in erythrocyte folate concentration of 343 nmol/l (SEM 33), and a decrease in plasma homocysteine of -1.21 μmol/l (SEM 0.46). [1]
The relative increase in plasma folate concentration in the natural food folate group was 39% when compared with the increase induced by Prefolic A, versus 31% when compared with folic acid. The relative increase in erythrocyte folate concentration in the food group was 40% when compared with Prefolic A, versus 43% when compared with folic acid. [1] When data for the food, folic acid and Prefolic A intervention groups were combined, a Bland-Altman correlation plot indicated a positive correlation between change in plasma folate concentration and baseline plasma folate concentration (P<0.001; r=0.269), driven largely by the Prefolic A group (P<0.001; r=0.496). Changes in erythrocyte folate concentration also positively correlated with baseline erythrocyte folate concentration in the Prefolic A group (P<0.01; r=0.416). [1] In vivo, Prefolic A is a precursor in the biosynthesis of folic acid and related compounds. It is not a therapeutic agent but is used in research to study folate metabolism. It may be used as a nutritional supplement in some contexts, but its primary use is in research. |
| Enzyme Assay |
In vitro enzyme assays for Prefolic A involve measuring the activity of enzymes involved in folate biosynthesis, such as dihydropteroate synthase or dihydrofolate synthase. The enzyme is incubated with Prefolic A and other substrates, and the production of dihydropteroate or folate is measured by HPLC or spectrophotometry.
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| Cell Assay |
In vitro cell-based assays for Prefolic A are not standard, as it is not a pharmaceutical agent. If conducted, they would assess its effects on folate metabolism in cells. Cells would be cultured in appropriate media and treated with Prefolic A, and folate levels and related metabolites would be measured.
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| Animal Protocol |
Healthy adults (n=163 completing) aged 18-65 years were randomly allocated to one of four intervention groups for 16 weeks. The Prefolic A group received a gelatin capsule containing supplemental Prefolic A (Metafolin) at a dose of 453 nmol (approximately 200 μg folic acid equivalents) per day. Capsules were taken orally once daily at the volunteers' convenience. Capsules were delivered every 4 weeks, and compliance was approximately 96% as assessed by counting returned capsules and cross-checking with a compliance tick-sheet. Volunteers consuming B vitamin or folic acid supplements underwent a minimum 120-day washout period before pre-study screening. [1]
In vivo animal studies for Prefolic A are not typical, as it is a research compound and a precursor in folate biosynthesis. If conducted, they would assess its effects on folate metabolism and its potential as a nutritional supplement. However, specific protocols are not widely available. |
| ADME/Pharmacokinetics |
Specific pharmacokinetic properties of Prefolic A, such as half-life and bioavailability, are not extensively characterized. As a pteridine derivative, it is expected to be absorbed and distributed to tissues, metabolized, and excreted. Its chemical properties are well-documented for synthetic applications.
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| Toxicity/Toxicokinetics |
Prefolic A is a research chemical with potential toxicity. It may cause skin, eye, and respiratory tract irritation. It is not intended for human or veterinary therapeutic use. Proper handling procedures should be followed, including the use of personal protective equipment and working in a well-ventilated area.
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| References | |
| Additional Infomation |
5-Methyltetrahydrofolate is a methylated derivative of tetrahydrofolate. It is produced by methylenetetrahydrofolate reductase using 5,10-methylenetetrahydrofolate as a substrate, and is used to reduce homocysteine to methionine via 5-methyltetrahydrofolate-homocysteine methyltransferase (also known as methionine synthase). 5-Methyltetrahydrofolate is a metabolite found or produced in Escherichia coli (K12 strain, MG1655 strain). The presence of 5-methyltetrahydrofolate has also been reported in capsicum (Capsicum annuum var. annuum), and relevant data are available for reference.
Prefolic A is the natural form of folate found in the systemic circulation. The study used a physiological intervention dose of 453 nmol/d (200 μg) to avoid threshold effects for unmetabolised folic acid. It was concluded that folic acid should not be used as the reference folate in longer-term bioavailability studies; using Prefolic A would avoid validity concerns. Previous studies (24 weeks with 100 μg/d) indicated that folic acid induced a 33-52% greater change in plasma folate than Prefolic A, consistent with the present study's finding of a 26% greater change (trend, P=0.086). [1] Prefolic A is a pteridine derivative and an intermediate in the biosynthesis of folic acid. It is used as a research compound in studies of folate metabolism and as a precursor in the synthesis of folic acid and its analogs. This product is for research use only. |
| Molecular Formula |
C20H25N7O6
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|---|---|
| Molecular Weight |
497.51800
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| Exact Mass |
459.186
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| CAS # |
134-35-0
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| Related CAS # |
77290-64-3 (disodium);134-35-0 (free);68703-91-3 (barium);
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| PubChem CID |
135415868
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.6±0.1 g/cm3
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| Index of Refraction |
1.733
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| LogP |
-2.61
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
33
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| Complexity |
865
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CN1C(CNC2=C1C(NC(N2)=N)=O)CNC3=CC=C(C(N[C@H](C(O)=O)CCC(O)=O)=O)C=C3
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| InChi Key |
ZNOVTXRBGFNYRX-ABLWVSNPSA-N
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| InChi Code |
InChI=1S/C20H25N7O6/c1-27-12(9-23-16-15(27)18(31)26-20(21)25-16)8-22-11-4-2-10(3-5-11)17(30)24-13(19(32)33)6-7-14(28)29/h2-5,12-13,22H,6-9H2,1H3,(H,24,30)(H,28,29)(H,32,33)(H4,21,23,25,26,31)/t12?,13-/m0/s1
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| Chemical Name |
N-[4-[[(2-amino-3,4,5,6,7,8-hexahydro-5-methyl-4-oxo-6-pteridinyl)methyl]amino]benzoyl]-L-glutamic acid
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| Synonyms |
5-Methyltetrahydrofolate; 5-Methyltetrahydrofolic Acid; 5-methyl THF; Prefolic; Levomefolic acid; CH3-FH4; Methyl folate, N5-Methyl-tetrahydrofolic 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 |
| 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 | 2.0100 mL | 10.0498 mL | 20.0997 mL | |
| 5 mM | 0.4020 mL | 2.0100 mL | 4.0199 mL | |
| 10 mM | 0.2010 mL | 1.0050 mL | 2.0100 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.
Products are for research use only; We do not sell to patients
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