| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
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.
| Targets |
VDR/vitamin D receptor; Human Endogenous Metabolite
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| 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.
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| 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.
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| Cell Assay |
MCF-7 cells were treated with 1,25(OH)2D3 and their levels of VDR expression, viability, and apoptosis were detected. CD133+ MCF-7 stem cells were identified and transfected with a VDR-overexpression plasmid. The tamoxifen concentration that reduced MCF-7 cell viability by 50% (IC50) was determined. The activation of Wnt/β-catenin signaling was also investigated[2].
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| Animal Protocol |
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Readily absorbed. Metabolism / Metabolites Calcidiol undergoes hydroxylation in the mitochondria of kidney tissue, and this reaction is activated by the renal 25-hydroxyvitamin D3-1-(alpha)-hydroxylase to produce calcitriol (1,25- dihydroxycholecalciferol), the active form of vitamin D3. Calcidiol undergoes hydroxylation in the mitochondria of kidney tissue, and this reaction is activated by the renal 25-hydroxyvitamin D3-1-(alpha)-hydroxylase to produce calcitriol (1,25- dihydroxycholecalciferol), the active form of vitamin D3. Half Life: 288 hours Biological Half-Life 288 hours |
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| Toxicity/Toxicokinetics |
Toxicity Summary
Calcidiol is transformed in the kidney by 25-hydroxyvitamin D3-1-(alpha)-hydroxylase to calcitriol, the active form of vitamin D3. Calcitriol binds to intracellular receptors that then function as transcription factors to modulate gene expression. Like the receptors for other steroid hormones and thyroid hormones, the vitamin D receptor has hormone-binding and DNA-binding domains. The vitamin D receptor forms a complex with another intracellular receptor, the retinoid-X receptor, and that heterodimer is what binds to DNA. In most cases studied, the effect is to activate transcription, but situations are also known in which vitamin D suppresses transcription. Calcitriol increases the serum calcium concentrations by: increasing GI absorption of phosphorus and calcium, increasing osteoclastic resorption, and increasing distal renal tubular reabsorption of calcium. Calcitriol appears to promote intestinal absorption of calcium through binding to the vitamin D receptor in the mucosal cytoplasm of the intestine. Subsequently, calcium is absorbed through formation of a calcium-binding protein. |
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| References |
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| Additional Infomation |
Pharmacodynamics
Calcidiol is the precursor of vitamin D3. Vitamin D3 is a steroid hormone that has long been known for its important role in regulating body levels of calcium and phosphorus, in mineralization of bone, and for the assimilation of vitamin A. The classical manifestations of vitamin D deficiency is rickets, which is seen in children and results in bony deformaties including bowed long bones. Deficiency in adults leads to the disease osteomalacia. Both rickets and osteomalacia reflect impaired mineralization of newly synthesized bone matrix, and usually result from a combination of inadequate exposure to sunlight and decreased dietary intake of vitamin D. Common causes of vitamin D deficiency include genetic defects in the vitamin D receptor, severe liver or kidney disease, and insufficient exposure to sunlight. Vitamin D plays an important role in maintaining calcium balance and in the regulation of parathyroid hormone (PTH). It promotes renal reabsorption of calcium, increases intestinal absorption of calcium and phosphorus, and increases calcium and phosphorus mobilization from bone to plasma. |
| Molecular Formula |
C27H44O2
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| Molecular Weight |
400.64
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| Exact Mass |
400.334
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| Elemental Analysis |
C, 80.94; H, 11.07; O, 7.99
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| CAS # |
19356-17-3
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| Related CAS # |
Calcifediol monohydrate;63283-36-3;Calcifediol-d3;140710-94-7
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| PubChem CID |
5283731
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| Appearance |
White to off-white solid powder
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| Density |
1.0±0.1 g/cm3
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| Boiling Point |
529.2±33.0 °C at 760 mmHg
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| Melting Point |
74-76oC
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| Flash Point |
221.4±20.0 °C
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| Vapour Pressure |
0.0±3.2 mmHg at 25°C
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| Index of Refraction |
1.536
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| LogP |
7.53
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
29
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| Complexity |
655
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| Defined Atom Stereocenter Count |
5
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| SMILES |
O([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])C([H])([H])C([H])([H])[C@@]([H])(C([H])([H])[H])[C@@]1([H])C([H])([H])C([H])([H])[C@@]2([H])/C(=C(\[H])/C(/[H])=C3\C(=C([H])[H])C([H])([H])C([H])([H])[C@@]([H])(C\3([H])[H])O[H])/C([H])([H])C([H])([H])C([H])([H])[C@]12C([H])([H])[H]
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| InChi Key |
JWUBBDSIWDLEOM-DTOXIADCSA-N
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| 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
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| 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
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| Synonyms |
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| 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 |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| 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. View More
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. Solubility in Formulation 4: 2% DMSO +30% PEG 300 +5% Tween+ddH2O: 5mg/mL |
| 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.
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.
| 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 |
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