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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| Targets |
Ercalcidiol is a precursor to the active form of vitamin D2, ercalcitriol (1α,25-dihydroxyvitamin D2). It binds to the vitamin D binding protein (DBP) in the circulation and is transported to the kidney, where it is converted to the active hormone by the enzyme CYP27B1 (1α-hydroxylase). The active hormone then binds to the vitamin D receptor (VDR) to regulate gene transcription involved in calcium and phosphate homeostasis, bone metabolism, and immune function.
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| ln Vitro |
As the primary prescription form of vitamin D, ercalciferol (25(OH)D2) must be distinguished from 25(OH)D3 in order to properly monitor vitamin D therapy. Because ercalciferol binds poorly to vitamin D-binding proteins and has a shorter half-life than 25(OH)D3, it is less effective than vitamin D3 and requires considerably higher doses. When attempting to monitor vitamin D2 therapy, certain tests now in use have a limited capacity to detect iacalcidiol, which could result in severe overdoses [2].
In vitro, ercalcidiol has a shorter half-life than 25(OH)D3 and binds less well to the vitamin D binding protein, making it less potent and requiring much higher doses than vitamin D3. Its activity can be assessed in cell-based assays measuring VDR-mediated gene expression in cells treated with ercalcidiol. The compound's ability to induce the expression of VDR target genes (e.g., CYP24A1) can be quantified by qPCR. |
| ln Vivo |
In vivo, ercalcidiol is used as a biomarker to monitor vitamin D status and the efficacy of vitamin D2 therapy. It is commonly employed for managing disorders of calcium and phosphate homeostasis. As a circulating metabolite, its levels reflect the body's vitamin D stores. Ercalcidiol is used in clinical settings to assess vitamin D deficiency and to monitor the response to vitamin D supplementation.
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| Enzyme Assay |
Non-cellular assays for ercalcidiol are typically analytical in nature, using techniques such as liquid chromatography-tandem mass spectrometry (LC-MS/MS) or high-performance liquid chromatography (HPLC) to quantify the compound in biological samples. Its binding affinity for the vitamin D binding protein can be assessed using competitive binding assays. The compound's physicochemical properties can be characterized using standard analytical techniques.
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| Cell Assay |
In vitro cellular assays for ercalcidiol involve treating cells expressing the vitamin D receptor (VDR) with the compound and measuring VDR-mediated gene expression. Cells are treated with varying concentrations of ercalcidiol for 24-48 hours, and the expression of VDR target genes (e.g., CYP24A1, osteocalcin) is quantified by qPCR or reporter gene assays. The compound's ability to induce VDR activation is compared to that of calcitriol (1,25-dihydroxyvitamin D3).
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| Animal Protocol |
In vivo animal experiments are not typically conducted with ercalcidiol as a therapeutic agent. It is primarily used as a biomarker in clinical studies. Vitamin D status in animal models can be assessed by measuring serum ercalcidiol levels using LC-MS/MS or immunoassays. The compound's role in maintaining bone density and calcium-phosphate homeostasis is studied in models of vitamin D deficiency or metabolic bone disease.
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| ADME/Pharmacokinetics |
Ercalcidiol has a molecular weight of 412.66 and a molecular formula of C₂₈H₄₄O₂. It is a solid powder with a purity of >98%. The compound is soluble in DMF (20 mg/ml), DMSO (20 mg/ml), and ethanol (20 mg/ml). It is typically stored at -20°C, protected from light and moisture. The compound is stable under recommended storage conditions.
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| Toxicity/Toxicokinetics |
Ercalcidiol is a research compound for laboratory use only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling the compound. It may cause skin, eye, and respiratory irritation. Appropriate personal protective equipment should be used. The compound is intended for research and analytical applications only.
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| References |
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| Additional Infomation |
25-Hydroxyvitamin D2 is a hydroxycalcium alcohol, which is the structure of vitamin D2 where the hydrogen atom at position 25 is replaced by a hydroxyl group. It plays a role in maintaining bone density, as a nutritional supplement, and as an exogenous metabolite in the human body. It is a hydroxycalcium alcohol, an ergosterol, and a form of vitamin D. Functionally, it is related to vitamin D2. 9,10-Ergosterol-5,7,10(19),22-Tetraen-3,25-diol is a bioactive metabolite of vitamin D2, and its activity in treating rickets is higher than that of its parent compound. This compound is believed to bind to the same receptor as vitamin D2 and 25-hydroxyvitamin D3.
Ercalcidiol (25-hydroxy Vitamin D2; CAS 21343-40-8) is a metabolite of vitamin D2 and a biomarker of vitamin D nutritional status. It has a shorter half-life than 25(OH)D3 and binds less well to the vitamin D binding protein, making it less potent and requiring higher doses than vitamin D3. Ercalcidiol is used to monitor vitamin D therapy and manage disorders of calcium and phosphate homeostasis. |
| Molecular Formula |
C28H44O2
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|---|---|
| Molecular Weight |
412.65
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| Exact Mass |
412.334
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| CAS # |
21343-40-8
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| Related CAS # |
Calcifediol-d6;78782-98-6;25-Hydroxy VD2-d6;1262843-46-8;Ercalcidiol-d3;1217467-39-4
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| PubChem CID |
5710148
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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 |
542.3±38.0 °C at 760 mmHg
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| Melting Point |
45-51ºC
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| Flash Point |
225.9±21.4 °C
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| Vapour Pressure |
0.0±3.3 mmHg at 25°C
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| Index of Refraction |
1.543
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| LogP |
7.56
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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 |
5
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| Heavy Atom Count |
30
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| Complexity |
725
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| Defined Atom Stereocenter Count |
6
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| SMILES |
C[C@H](/C=C/[C@H](C)C(C)(C)O)[C@H]1CC[C@@H]\2[C@@]1(CCC/C2=C\C=C/3\C[C@H](CCC3=C)O)C
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| InChi Key |
KJKIIUAXZGLUND-FOZBYKFWSA-N
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| InChi Code |
InChI=1S/C28H44O2/c1-19-10-14-24(29)18-23(19)13-12-22-8-7-17-28(6)25(15-16-26(22)28)20(2)9-11-21(3)27(4,5)30/h9,11-13,20-21,24-26,29-30H,1,7-8,10,14-18H2,2-6H3/b11-9+,22-12+,23-13-/t20-,21+,24-,25-,26+,28-/m1/s1
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| Chemical Name |
(R,Z)-3-(2-((1R,3aS,7aR,E)-1-((2R,5S,E)-6-hydroxy-5,6-dimethylhept-3-en-2-yl)-7a-methyloctahydro-4H-inden-4-ylidene)ethylidene)-4-methylenecyclohexan-1-ol
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| Synonyms |
25-Hydroxyecalciferol 25-Hydroxyergocalciferol 25-Hydroxyvitamin D 25-Hydroxyvitamin D2 25-OH Vitamin D2.
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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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. (3). 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)
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| Solubility (In Vitro) |
DMSO : ~200 mg/mL (~484.67 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.06 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: ≥ 2.5 mg/mL (6.06 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 25.0 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: ≥ 2.5 mg/mL (6.06 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4234 mL | 12.1168 mL | 24.2336 mL | |
| 5 mM | 0.4847 mL | 2.4234 mL | 4.8467 mL | |
| 10 mM | 0.2423 mL | 1.2117 mL | 2.4234 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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