Calcifediol (25-hydroxy Vitamin D3)

Alias: 25-hydroxyvitamin D3;25-hydroxy VD3; 25-hydroxy Cholecalciferol; U 32070E; Rovimix Hy-D; 25-hydroxy Vitamin D3; 25-OH Vitamin D3; Calcifediol; RO 8-8892
Cat No.:V2435 Purity: ≥98%
Calcifediol (also known as 25-hydroxyvitamin D3; 25-hydroxy VD3)is the major circulating metabolite of vitamin D3 in the blood and is the form that is tested inmedicine to determine vitamin D deficiency, namely, the test of 25-hydroxy vitamin D (calcifediol) levels to evaluate how much vitamin D is in the body.
Calcifediol (25-hydroxy Vitamin D3) Chemical Structure CAS No.: 19356-17-3
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
5mg
10mg
25mg
50mg
100mg
250mg
Other Sizes

Other Forms of Calcifediol (25-hydroxy Vitamin D3):

  • Calcifediol monohydrate (25-hydroxyvitamin D3; 25-hydroxy VD3)
  • Calcifediol-d3 (25-hydroxy Vitamin D3-d3)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Calcifediol (also known as 25-hydroxyvitamin D3; 25-hydroxy VD3) is the major metabolite of vitamin D3 that circulates in the blood and is the form that is tested in medicine to estimate the amount of vitamin D in the body (specifically, 25-hydroxy vitamin D, or calcifediol) and identify vitamin D deficiency. Calcifediol has an apparent Ki of 3.9 μM and functions as a competitive inhibitor. Additionally, it inhibits mRNA (ED50=2 nM) and PTH secretion. CYP24A1 expression was induced by calcifediol, with an EC50 of 70 nM. With an EC50 of 10-100 nM, calcifediol induced the expression of thrombomodulin. Confocal microscopy showed that calcifediol at concentrations between 0.1 and 10 μM dose-dependently caused VDR translocation into the nucleus; the VDR localization pattern in calcitriol-treated cells was comparable.

Biological Activity I Assay Protocols (From Reference)
Targets
Human Endogenous Metabolite
ln Vitro
Calcifediol induced CYP24A1 expression with EC50 at 70 nM. Thrombin expression was induced by calcifediol, with an EC50 of 10-100 nM. The VDR localization pattern in cells treated with calcitriol was similar, and calcifediol at 0.1–10 μM induced VDR translocation into the nucleus in a dose-dependent manner, according to confocal microscopy findings.
ln Vivo
For three days, 50 ng/d of calcifediol or vehicle alone was injected into spontaneously hypertensive rats and normotensive Wistar-Kyoto (WKY) rats. In the control SHR, cellular Ca2+ flux and calbindin-D9K were found to be reduced. Calcifediol elevated brush border and total cell calbindin-D9K. On the other hand, for plasma calcitriol levels comparable to those in WKY rats, Ca2+ flux, which rose in vit-D animals, stayed lower in SHR.
Animal Protocol
50 ng/d; injection
Rats
References

[1]. Calcifediol-loaded liposomes for local treatment of pulmonary bacterial infections. Eur J Pharm Biopharm. 2016 Nov 22.

[2]. Vitamin D-induced vitamin D receptor expression induces tamoxifen sensitivity in MCF-7 stem cells via suppression of Wnt/β-catenin signaling. Biosci Rep. 2018 Dec 7;38(6):BSR20180595.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C27H44O2
Molecular Weight
400.64
Exact Mass
400.33
Elemental Analysis
C, 80.94; H, 11.07; O, 7.99
CAS #
19356-17-3
Related CAS #
Calcifediol monohydrate;63283-36-3;Calcifediol-d3;140710-94-7
Appearance
Solid powder
SMILES
C[C@H](CCCC(C)(C)O)[C@H]1CC[C@@H]\2[C@@]1(CCC/C2=C\C=C/3\C[C@H](CCC3=C)O)C
InChi Key
JWUBBDSIWDLEOM-DTOXIADCSA-N
InChi Code
InChI=1S/C27H44O2/c1-19-10-13-23(28)18-22(19)12-11-21-9-7-17-27(5)24(14-15-25(21)27)20(2)8-6-16-26(3,4)29/h11-12,20,23-25,28-29H,1,6-10,13-18H2,2-5H3/b21-11+,22-12-/t20-,23+,24-,25+,27-/m1/s1
Chemical Name
(1S,3Z)-3-[(2E)-2-[(1R,3aS,7aR)-1-[(2R)-6-hydroxy-6-methylheptan-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexan-1-ol
Synonyms
25-hydroxyvitamin D3;25-hydroxy VD3; 25-hydroxy Cholecalciferol; U 32070E; Rovimix Hy-D; 25-hydroxy Vitamin D3; 25-OH Vitamin D3; Calcifediol; RO 8-8892
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: ~80 mg/mL (~199.7 mM)
Water: <1 mg/mL
Ethanol: ~20 mg/mL (~49.9 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.24 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 25.0 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 (5.19 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 (5.19 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.


Solubility in Formulation 4: 2% DMSO +30% PEG 300 +5% Tween+ddH2O: 5mg/mL

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.4960 mL 12.4800 mL 24.9601 mL
5 mM 0.4992 mL 2.4960 mL 4.9920 mL
10 mM 0.2496 mL 1.2480 mL 2.4960 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
NCT03602261 Active
Recruiting
Drug: Calcifediol Oral Capsule
Drug: Placebo oral capsule
Chronic Kidney Diseases
Vitamin D Deficiency
OPKO Health, Inc. July 9, 2018 Phase 2
NCT05398939 Recruiting Diagnostic Test: Blood test
and skin evaluation
Acne Vulgaris
Vitamin D Deficiency
National Taiwan University
Hospital
June 6, 2022
NCT05431920 Recruiting Dietary Supplement: Vitamin D₃
(25-hydroxy vitamin D)
Obesity
Non-allergic Asthma
Hospital Infantil de Mexico
Federico Gomez
October 1, 2022 Not Applicable
NCT03401541 Completed Drug: Calcifediol
Drug: Calciferol
Vitamin D Deficiency
Fat Malabsorption
Boston University October 1, 2018 Early Phase 1
NCT02805907 Completed Drug: Calcifediol
Drug: Placebo
Asthma, Bronchial MurciaSalud June 2016 Phase 4
Biological Data
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