Cholecalciferol (Vitamin D3)

Alias: Activated 7-dehydrocholesterol; Cholecalciferol; Calciol; Vitamin D3; Colecalciferol; Arachitol; Ricketon; Trivitan; Vigorsan; Deparal; Vigantol
Cat No.:V5283 Purity: ≥98%
Cholecalciferol (Vitamin D3; Colecalciferol),a secosteroid (a steroid molecule with one ring open), is a naturally occuring form of vitamin D; Upon metabolic activation, cholecalciferol is converted to the active form, 1,25-dihydroxy vitamin D3, which induces cell differentiation and prevents proliferation of cancer cells.
Cholecalciferol (Vitamin D3) Chemical Structure CAS No.: 67-97-0
Product category: VD VDR
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
500mg
1g
2g
5g
10g
Other Sizes

Other Forms of Cholecalciferol (Vitamin D3):

  • Vitamin D3-d7 (vitamin D3 d7)
  • 3-epi-Vitamin D3
  • Vitamin D3-d3
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Cholecalciferol (Vitamin D3; Colecalciferol), a secosteroid (a steroid molecule with one ring open), is a naturally occurring form of vitamin D. When it is metabolically activated, cholecalciferol transforms into 1,25-dihydroxy vitamin D3, the active form that promotes cell differentiation and inhibits the growth of cancer cells. A steroid hormone called vitamin D3/cholecalciferol is created in the skin in response to UV light exposure or is acquired through diet. 1,25-dihydroxycholecalciferol, the active form of cholecalciferol, is crucial for preserving blood calcium and phosphorus levels as well as bone mineralization. Cholecalciferol that has been activated binds to vitamin D receptors and changes the expression of certain genes.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Vitamin D3 is an in vivo inactive molecule of vitamin D. To activate vitamin D3, it goes through two hydroxylation processes. The enzyme 25-hydroxylase (CYP27A1) and possibly other enzymes (such as CYP2R1) hydroxylate vitamin D3 in the liver to create the circulating prohormone 25-hydroxy vitamin D3 [25(OH)D3][1]. The kidneys use the enzyme 1-alpha-hydroxylase to carry out the second hydroxylation, resulting in 1,25-dihydroxycholecalciferol, or calcitriol, the biologically active form of vitamin D[1]. Vitamin D3 (2-10 μM; 24-48 hours) shows effects against proliferation that are dependent on both time and dose. After treating with 10 μM vitamin D3, the viability of 62% (IK), 52% (RL-95-2), and 55% (Hec-1A) is at its lowest point after 72 hours. However, there is no discernible decrease in viable cells after a 24-hour exposure[2]. Cholecalciferol (10 μM; 24-48 hours) exhibits notable increases in nuclear VDR staining and causes IK cells to become activated locally for VDR[1].
ln Vivo
Cholecalciferol (oral gavage; 5 mg/kg; 7 days) increases the toxicity of CCl4 exclusively in the liver, as shown by elevated plasma levels of ALT and AST, two biochemical indicators of hepatic injury. Although renal calcium content does not significantly differ between mice, it significantly raises renal calcium levels in mice[3].
Animal Protocol
Male ddY mice on CCl4 toxicity[3]
5 mg/kg
Oral gavage; 5 mg/kg; 7 days
References

[1]. Nazik Al-Hashimi, et al. Cholecalciferol.

[2]. Role of local bioactivation of vitamin D by CYP27A1 and CYP2R1 in the control of cell growth in normal endometrium and endometrial carcinoma. Lab Invest. 2014 Jun;94(6):608-22.

[3]. Vitamin D3-induced hypercalcemia increases carbon tetrachloride-induced hepatotoxicity through elevated oxidative stress in mice. PLoS One. 2017 Apr 27;12(4):e0176524.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C27H44O
Molecular Weight
384.6377
Exact Mass
384.34
Elemental Analysis
C, 84.31; H, 11.53; O, 4.16
CAS #
67-97-0
Related CAS #
Vitamin D3-d7;1627523-19-6;3-epi-Vitamin D3;57651-82-8;Vitamin D3-13C3;Vitamin D3-d3;80666-48-4;Vitamin D3-13C5
Appearance
White to off-white solid powder
SMILES
C[C@H](CCCC(C)C)[C@H]1CC[C@@H]\2[C@@]1(CCC/C2=C\C=C/3\C[C@H](CCC3=C)O)C
InChi Key
QYSXJUFSXHHAJI-YRZJJWOYSA-N
InChi Code
InChI=1S/C27H44O/c1-19(2)8-6-9-21(4)25-15-16-26-22(10-7-17-27(25,26)5)12-13-23-18-24(28)14-11-20(23)3/h12-13,19,21,24-26,28H,3,6-11,14-18H2,1-2,4-5H3/b22-12+,23-13-/t21-,24+,25-,26+,27-/m1/s1
Chemical Name
(1S,3Z)-3-[(2E)-2-[(1R,3aS,7aR)-7a-methyl-1-[(2R)-6-methylheptan-2-yl]-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexan-1-ol
Synonyms
Activated 7-dehydrocholesterol; Cholecalciferol; Calciol; Vitamin D3; Colecalciferol; Arachitol; Ricketon; Trivitan; Vigorsan; Deparal; Vigantol
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 : ~100 mg/mL (~259.98 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.41 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 (5.41 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
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 (5.41 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 2.5998 mL 12.9992 mL 25.9983 mL
5 mM 0.5200 mL 2.5998 mL 5.1997 mL
10 mM 0.2600 mL 1.2999 mL 2.5998 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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g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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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
NCT05613192 Recruiting Drug: Cholecalciferol Non-Alcoholic Fatty Liver
Disease
Ain Shams University October 31, 2022 Phase 3
NCT03613116 Recruiting Dietary Supplement: Vitamin D3 Vitamin D Deficiency
Cognitive Decline
University of California, Davis March 18, 2019 Phase 2
NCT04229368 Recruiting Dietary Supplement: Vitamin D3 Hip Arthropathy
Knee Arthropathy
Brigham and Women's Hospital September 1, 2019 Not Applicable
NCT05586529 Recruiting Dietary Supplement:
Cholecalciferol
Hypocalcemia Pak Emirates Military Hospital November 1, 2022 Not Applicable
NCT06054919 Active
Recruiting
Drug: Cholecalciferol Vitamin D Deficiency Indonesia University April 1, 2021 Phase 2
Phase 3
Biological Data
  • Cholecalciferol (VD3) treatment is sufficient to suppress the growth in EC cell lines. Lab Invest . 2014 Jun;94(6):608-22.
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