| Size | Price | |
|---|---|---|
| 250mg | ||
| 500mg | ||
| 1g | ||
| 2g |
Purity: ≥98%
Levoleucovorin disodium is the sodium salt of Levoleucovorin which is the pharmacologically and enantiomerically active form of leucovorin, is a folate analog with anticancer activity. . Commercially available leucovorin is composed of 1 racemic mixture of the dextrorotary and levorotary isomers, while levoleucovorin contains only the pharmacologically active levo-isomer. In vitro, the levo-isomer has been shown to be rapidly converted to the biologically available methyl-tetrahydrofolate form while the dextro form is slowly excreted by the kidneys. Despite this difference in activity, the two commercially available forms have been shown to be pharmacokinetically identical and may be used interchangeably with limited differences in efficacy or side effects. As folate analogues, levoleucovorin and leucovorin are both used to counteract the toxic effects of folic acid antagonists, such as methotrexate, which act by inhibiting the enzyme dihydrofolate reductase (DHFR). They are indicated for use as rescue therapy following use of high-dose methotrexate in the treatment of osteosarcoma or for diminishing the toxicity associated with inadvertent overdosage of folic acid antagonists.
| ln Vitro |
When five different concentrations (5-100 mg/ml) of MTX were applied for six hours, the percentage of aberrant cells (Abs) (36 %-77%) and micronucleated binucleated cells (MNBN) (40%-68%) was dramatically reduced by disodium leucovorin (5, 50 µg/ml; 40 hours) [1].
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|---|---|
| ln Vivo |
This growth inhibition appears to be reversed by treatment with disodium leucovorin (7.0 mg/kg; i.p.; every other day; for 3 weeks; Balb/c young growing male mice) after methotrexate (MTX) administration (Long-term administration of MTX reduces bone growth in mice) [2].
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| Animal Protocol |
Animal/Disease Models: 24 3weeks old Balb/c young male mice (11.88±0.25g) [2]
Doses: 7.0mg/kg Route of Administration: intraperitoneal (ip) injection; every other day; continued for 3 weeks Experimental Results: MTX administration This growth inhibition appeared to be reversed. |
| References |
[1]. Keshava, C., et al., Inhibition of methotrexate-induced chromosomal damage by folinic acid in V79 cells. Mutat Res, 1998. 397(2): p. 221-8.
[2]. Iqbal MP, et al. Effect of methotrexate and folinic acid on skeletal growth in mice. Acta Paediatr. 2003 Dec;92(12):1438-44. [3]. Francini G, et al. Folinic acid and 5-fluorouracil as adjuvant chemotherapy in colon cancer. Gastroenterology. 1994 Apr;106(4):899-906. |
| Molecular Formula |
C20H21N7NA2O7
|
|---|---|
| Molecular Weight |
517.4095
|
| CAS # |
163254-40-8
|
| Related CAS # |
Folinic acid;58-05-9;Folinic acid-d4 calcium hydrate
|
| SMILES |
O=C(CC[C@H](NC(C1=CC=C(C=C1)NC[C@@H]2N(C3=C(NC2)N=C(NC3=O)N)C=O)=O)C([O-])=O)[O-].[Na+].[Na+]
|
| InChi Key |
FSDMNNPYPVJNAT-NJHZPMQHSA-L
|
| InChi Code |
InChI=1S/C20H23N7O7.2Na/c21-20-25-16-15(18(32)26-20)27(9-28)12(8-23-16)7-22-11-3-1-10(2-4-11)17(31)24-13(19(33)34)5-6-14(29)30/h1-4,9,12-13,22H,5-8H2,(H,24,31)(H,29,30)(H,33,34)(H4,21,23,25,26,32)/q2*+1/p-2/t12-,13-/m0../s1
|
| Chemical Name |
sodium (4-((((S)-2-amino-5-formyl-4-oxo-3,4,5,6,7,8-hexahydropteridin-6-yl)methyl)amino)benzoyl)-L-glutamate
|
| Synonyms |
Levoleucovorin disodium Disodium levofolinate
|
| 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)
|
| 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.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9327 mL | 9.6635 mL | 19.3270 mL | |
| 5 mM | 0.3865 mL | 1.9327 mL | 3.8654 mL | |
| 10 mM | 0.1933 mL | 0.9664 mL | 1.9327 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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