Leucovorin (Folinic acid)

Alias: Leucovorin; Folinic acid; HSDB-6544; HSDB6544; HSDB 6544
Cat No.:V17929 Purity: ≥98%
Leucovorin (Folinic acid), the active metabolite of folic acid, is used primarily as the calcium salt form as an antidote/rescue agent to folic acid antagonists which block the conversion of folic acid to folinic acid.
Leucovorin (Folinic acid) Chemical Structure CAS No.: 58-05-9
Product category: Thymidylate Synthase
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
25mg
50mg
100mg
250mg
500mg
Other Sizes

Other Forms of Leucovorin (Folinic acid):

  • Leucovorin Calcium
  • Leucovorin calcium hydrate
  • Levoleucovorin disodium
  • Folinic acid calcium hydrate
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Leucovorin (Folinic acid), the active metabolite of folic acid, is primarily used as the calcium salt form of a folic acid antagonist, which prevents the conversion of folic acid to folinic acid, as an antidote or rescue agent. Methotrexate (MTX) and pyrimethamine's toxic effects are lessened by this medication. It can also be used to treat anemia caused by a folate deficiency, methanol poisoning, and colorectal cancer when combined with 5-fluorouracil.

Biological Activity I Assay Protocols (From Reference)
Targets
Thymidylate Synthase
ln Vitro
The percentage of aberrant cells (Abs) and micronucleated binucleated cells (MNBN) increased concentration-dependently when methotrexate (MTX) was used alone. The nuclear division index (NDI) falls as MTX concentration rises. Similarly, in all experiments, the addition of 50 μg/mL leucovorin dramatically decreased the percentages of MNBN (40-68%) and Abs (36-77%). Additionally, at 5 μg/mL leucovorin, inhibitory effects were noted (12% to 54% for MNBN and 20% to 61% for Abs) [1].
ln Vivo
Leucovorin (7.0 mg/kg; i.p.; every other day; for 3 weeks; Balb/c Juvenile Solution) medication is administered after methotrexate (MTX) and seems to reverse the growth inhibition of MTX (Long-Term Give attention to MTX Fed rabbits atherosclerosis progresses slowly when given dextrapril (5–20 mg/kg) [2]. Delapril (1-2 mg/kg, po, once daily for 5 weeks) When studying hypertension in an animal model: Fed rabbits cholesterol [2]
Animal Protocol
Animal/Disease Models: 24 3weeks old Balb/c young growing male mice (11.88±0.25 g) [2]
Doses: 7.0 mg/kg
Route of Administration: intraperitoneal (ip) injection; every other day; for 3 weeks
Experimental Results: After MTX administration appears to reverse this growth inhibition.
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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C20H23N7O7
Molecular Weight
473.446
Exact Mass
473.1659
Elemental Analysis
C, 50.74; H, 4.90; N, 20.71; O, 23.65
CAS #
58-05-9
Related CAS #
Folinic acid calcium;1492-18-8;Folinic acid calcium salt pentahydrate;6035-45-6;Folinic acid disodium;163254-40-8;Folinic acid calcium hydrate;1097832-14-8;Folinic acid-d4 calcium hydrate
Appearance
Solid powder
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
InChi Key
VVIAGPKUTFNRDU-ABLWVSNPSA-N
InChi Code
InChI=1S/C20H23N7O7/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)/t12?,13-/m0/s1
Chemical Name
(2S)-2-[[4-[(2-amino-5-formyl-4-oxo-3,6,7,8-tetrahydropteridin-6-yl)methylamino]benzoyl]amino]pentanedioic acid
Synonyms
Leucovorin; Folinic acid; HSDB-6544; HSDB6544; HSDB 6544
HS Tariff Code
2934.99.9001
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 Data
Solubility (In Vitro)
DMSO: 95~250 mg/mL (200.7~528.1 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.39 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.08 mg/mL (4.39 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.08 mg/mL (4.39 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.1122 mL 10.5608 mL 21.1216 mL
5 mM 0.4224 mL 2.1122 mL 4.2243 mL
10 mM 0.2112 mL 1.0561 mL 2.1122 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.

Calculator

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04060017 Active
Recruiting
Drug: Levoleucovorin Calcium
Other: Placebo
Autism Spectrum Disorder
Language Disorders
Rossignol Medical Center September 22, 2020 Phase 2
NCT02839915 Active
Recruiting
Other: Placebo
Drug: Folinic Acid
Autism Spectrum Disorder Rossignol Medical Center August 13, 2020 Phase 2
NCT03750786 Active
Recruiting
Drug: Arfolitixorin
Drug: Leucovorin
Colo-rectal Cancer Isofol Medical AB December 18, 2018 Phase 3
NCT00082706 Active
Recruiting
Drug: Leucovorin
Drug: 5-Fluorouracil
(5-FU)
Bladder Cancer
Urethral Cancer
M.D. Anderson Cancer Center April 23, 2003 Phase 2
NCT00217737 Active
Recruiting
Drug: Oxaliplatin
Drug: Leucovorin Calcium
Lynch Syndrome
Stage IIA Colon Cancer
AJCC v7
National Cancer Institute
(NCI)
August 4, 2005 Phase 3
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