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| 500mg |
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| 1g |
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| 2g |
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| 5g |
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| 10g |
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| 25g |
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Leucovorin calcium, a reduced folic acid and an active metabolite of folic acid (also known as folinic acid and citrovorum factor), is a derivative of folic acid which can be used to increase levels of folic acid under conditions favoring folic acid inhibition. Leucovorin administration increases the level of reduced folates in tissues, which promotes the inhibition of thymidylate synthase in two murine colon tumors. Leucovorin, Gemcitabine, Oxaliplatin, and 5-fluorouracil is a powerful antitumor and immunomodulating regimen that can make the tumor cells a suitable means to induce an Ag-specific CTL response.
| ln Vitro |
The percentage of aberrant cells (Abs) and micronucleated binucleated cells (MNBN) increased in a concentration-related manner when MTX was used alone. The nuclear division index (NDI) falls as MTX concentration rises. In a similar vein, the mitotic index (MI) dropped for every MTX concentration that was examined. Leucovorin added at 50 μg/mL dramatically decreased the Abs percentage (36–77%) and MNBN percentage (40–68%). Inhibitory effects are likewise produced by leucovorin at 5 μg/mL (12% to 54% for MNBN and 20% to 61% for Abs) [1].
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|---|---|
| ln Vivo |
This growth suppression (chronic administration of the drug MTX reduces bone growth in mice) appears to be reversed by treatment with leucovorin (7.0 mg/kg; i.p.; every other day; for 3 weeks; Balb/c young developing male 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; for 3 weeks Experimental Results: Administration of methamine This growth inhibition appears to be reversed by pterin (MTX). |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Leucovorin (folinic acid; 5-formyltetrahydrofolic acid) and its levo- isomer, levoleucovorin, are folic acid derivatives that are normal components of breastmilk. Because leucovorin and levoleucovorin are used as therapeutic agents with potentially toxic drugs such as fluorouracil or methotrexate, the LactMed record of the drug it is used with should be consulted. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
| References | |
| Additional Infomation |
The active metabolite of FOLIC ACID. Leucovorin is used principally as an antidote to FOLIC ACID ANTAGONISTS.
See also: Leucovorin Calcium (annotation moved to). |
| Molecular Formula |
C20H31CAN7O12
|
|---|---|
| Molecular Weight |
601.58
|
| Exact Mass |
601.165
|
| CAS # |
6035-45-6
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| Related CAS # |
Folinic acid calcium;1492-18-8;Folinic acid;58-05-9;Folinic acid calcium hydrate;1097832-14-8
|
| PubChem CID |
135802074
|
| Appearance |
Light yellow to yellow solid powder
|
| Melting Point |
240-250ºC
|
| Hydrogen Bond Donor Count |
10
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| Hydrogen Bond Acceptor Count |
15
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
40
|
| Complexity |
900
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| Defined Atom Stereocenter Count |
1
|
| SMILES |
C1C(N(C2=C(N1)N=C(NC2=O)N)C=O)CNC3=CC=C(C=C3)C(=O)N[C@@H](CCC(=O)[O-])C(=O)[O-].O.O.O.O.O.[Ca+2]
|
| InChi Key |
NPPBLUASYYNAIG-ZIGBGYJWSA-L
|
| InChi Code |
InChI=1S/C20H23N7O7.Ca.5H2O/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)5*1H2/q+2/p-2/t12?,13-/m0....../s1
|
| Chemical Name |
L-Glutamic acid,
N-(4-(((2-amino-5-formyl-1,4,5,6,7,8-hexahydro-4-oxo-6-pteridinyl)methyl)amino)benzoyl)-,
calcium salt (1
|
| Synonyms |
Folinic acid calcium salt pentahydrate Leucovorin calcium hydrate
|
| 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: (1). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. (2). This product is not stable in solution, please use freshly prepared working solution for optimal results. |
| 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 Vitro) |
H2O : ~10 mg/mL (~16.62 mM)
DMSO : ~1 mg/mL (~1.66 mM) |
|---|---|
| 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 | 1.6623 mL | 8.3114 mL | 16.6229 mL | |
| 5 mM | 0.3325 mL | 1.6623 mL | 3.3246 mL | |
| 10 mM | 0.1662 mL | 0.8311 mL | 1.6623 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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