| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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| 5g | |||
| 10g | |||
| Other Sizes |
Purity: ≥98%
| ADME/Pharmacokinetics |
After single oral administration of Levomefolate calcium 0.451 mg (alone or combined with ethinylestradiol/drospirenone) to healthy women, the following pharmacokinetic parameters for L-5-methyl-THF (the active moiety) were obtained (geometric mean, geometric coefficient of variation %). For Levomefolate calcium alone (reference): baseline-uncorrected Cmax = 61.8 nmol/L (29.2%), AUClast = 390 nmol·h/L (33.2%); baseline-corrected Cmax = 48.7 nmol/L (30.4%), AUClast = 239 nmol·h/L (26.5%). For Levomefolate calcium combined with EE/drospirenone (test): baseline-uncorrected Cmax = 65.2 nmol/L (30.7%), AUClast = 393 nmol·h/L (32.8%); baseline-corrected Cmax = 51.7 nmol/L (30.6%), AUClast = 236 nmol·h/L (26.3%). Median tmax was not reported specifically for levomefolate but was similar across treatments. The geometric mean ratios (test/reference) for baseline-uncorrected AUClast was 99.63% (90% CI 95.73-103.69%) and for Cmax 104.90% (90% CI 98.83-111.34%); for baseline-corrected AUClast 97.98% (90% CI 94.19-101.93%) and Cmax 106.19% (90% CI 99.18-113.68%). These were within the bioequivalence range of 80.00-125.00%. L-5-methyl-THF levels remained virtually unchanged from baseline after administration of EE/drospirenone alone, indicating no relevant influence of the study diet on endogenous concentrations [1].
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| Toxicity/Toxicokinetics |
Overall, 88.9% of subjects experienced at least one adverse event (AE); none were serious or rated as severe. Most AEs were mild or moderate. One significant AE (vasovagal syncope) deemed unlikely related to study medication led to withdrawal. Most frequent AE was decreased serum ferritin (62.2%), possibly related to frequent blood sampling (total ~457 mL). Other common AEs: nausea (31.1%), headache (28.9%), vomiting (26.7%), metrorrhagia (22.2%). Bleeding irregularities such as metrorrhagia were expected with single doses of sex hormone preparations. One unintended pregnancy occurred during second treatment period, considered related to insufficient use of non-hormonal contraception. No serious or severe AEs were reported [1].
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| References | |
| Additional Infomation |
L-methylfolate calcium is an organic calcium salt of (6S)-5-methyltetrahydrofolate. It has antidepressant effects. It contains (6S)-5-methyltetrahydrofolate (2-).
See also: Calcium cation (with active moiety); L-methylfolate calcium; Methylcobalamin; Turmeric (ingredient)... See more... Levomefolate calcium is an alternative folate form to folic acid, used in folate-supplemented oral contraceptives (e.g., SAFYRAL® containing EE 0.03 mg/drospirenone 3 mg/levomefolate calcium 0.451 mg, and Beyaz® with EE 0.02 mg/drospirenone 3 mg/levomefolate calcium 0.451 mg). On a molar basis, Levomefolate calcium 0.451 mg is equivalent to 0.416 mg L-5-methyl-THF, which is equimolar to 0.4 mg folic acid. The aim is to improve folate status in women of childbearing potential, reducing the risk of neural tube defects (NTDs) during early embryonic development. Unlike folic acid, it is directly bioavailable without needing metabolic activation, and has lower potential to mask vitamin B12 deficiency [1]. |
| Molecular Formula |
C20H23CAN7O6
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|---|---|
| Molecular Weight |
497.5179
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| Exact Mass |
497.133
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| CAS # |
151533-22-1
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| Related CAS # |
Levomefolic acid;31690-09-2;Levomefolate-13C5 calcium
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| PubChem CID |
135564391
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| Appearance |
Off-white to light yellow solid powder
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| Melting Point |
>300ºC
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
34
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| Complexity |
854
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CN1[C@H](CNC2=C1C(=O)NC(=N2)N)CNC3=CC=C(C=C3)C(=O)N[C@@H](CCC(=O)[O-])C(=O)[O-].[Ca+2]
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| InChi Key |
VWBBRFHSPXRJQD-QNTKWALQSA-L
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| InChi Code |
InChI=1S/C20H25N7O6.Ca/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);/q;+2/p-2/t12-,13-;/m0./s1
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| Chemical Name |
calcium (4-((((S)-2-amino-5-methyl-4-oxo-1,4,5,6,7,8-hexahydropteridin-6-yl)methyl)amino)benzoyl)-L-glutamate
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| Synonyms |
BAY 86-7660; BAY-86-7660; BAY86-7660; BAY 867660; BAY-867660; BAY867660; Levomefolate calcium; LMCA; Bodyfolin, Deplin; L-Methylfolate calcium; Levomefolate calcium; Levomefolinate calcium
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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) |
H2O : ~4.4 mg/mL (~8.84 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 | 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.
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