| Size | Price | Stock | Qty |
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| 1mg |
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| 2mg | |||
| 5mg | |||
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| Targets |
Vitamin D receptor (VDR).
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| ln Vitro |
In vitro, calcitetrol binds to and activates the vitamin D receptor (VDR), leading to a series of changes in gene expression. It enhances the absorption of dietary calcium and phosphate from the gastrointestinal tract and promotes renal tubular reabsorption of calcium in the kidneys. The compound stimulates the release of calcium stores from the skeletal system. VDR is present in caveolae-enriched plasma membranes and binds 1alpha,25(OH)2-vitamin D3 in vivo and in vitro.
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| ln Vivo |
In vivo, calcitetrol regulates calcium and phosphate homeostasis. It promotes intestinal calcium absorption, bone mineralization, and suppresses parathyroid hormone secretion. The compound increases blood calcium levels through its actions on the intestine, kidney, and bone. Calcitetrol is the hormonally active form of vitamin D with three hydroxyl groups.
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| Enzyme Assay |
VDR binding assays are performed using cytosolic or nuclear extracts from cells expressing VDR (e.g., intestinal epithelial cells, osteoblasts). Extracts are incubated with radiolabeled [3H]-1alpha,25-dihydroxyvitamin D3 (0.5-2 nM) and varying concentrations of unlabeled calcitetrol (0.01 nM-10 microM) in binding buffer (10 mM Tris-HCl, pH 7.4, containing 300 mM KCl, 1 mM DTT, 1 mM EDTA, and protease inhibitors) at 4degC for 2-4 hours. Non-specific binding is determined in the presence of 1000-fold excess unlabeled 1alpha,25-dihydroxyvitamin D3. Bound and free ligand are separated by hydroxylapatite adsorption or by charcoal dextran method. Radioactivity is counted and binding parameters are calculated.
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| Cell Assay |
VDR transcriptional activity is assessed using reporter gene assays in cells expressing VDR (e.g., HEK-293, COS-7, or osteoblast-like cells). Cells are transfected with a VDR expression plasmid and a luciferase reporter construct containing vitamin D response elements (VDRE). After 24 hours, cells are treated with calcitetrol at concentrations ranging from 0.01 nM to 1 microM for 24 hours. Luciferase activity is measured using a luminescence plate reader. EC₅0 values are calculated from dose-response curves. For calcium uptake studies, intestinal epithelial cells or osteoblasts are treated with the compound and calcium uptake is measured using ⁴⁵Ca2+ or fluorescent calcium indicators.
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| Animal Protocol |
In vivo studies are performed in vitamin D-deficient rodent models or in normal animals. Calcitetrol is administered orally or intraperitoneally at doses ranging from 0.01-1 microg/kg daily. Serum calcium and phosphate levels are measured at multiple time points. Bone mineral density is assessed by dual-energy X-ray absorptiometry (DXA) or micro-CT. Parathyroid hormone levels are measured by ELISA. Intestinal calcium absorption is measured using ⁴⁵Ca2+ gavage followed by serum radioactivity measurement. Gene expression in target tissues (intestine, kidney, bone) is analyzed by qPCR for VDR target genes (e.g., TRPV6, calbindin, osteocalcin).
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| ADME/Pharmacokinetics |
Calcitetrol has molecular formula C2₇H44O4 and molecular weight 432.64. As a vitamin D metabolite, it is highly lipophilic and has limited aqueous solubility. Formulation in oils, organic solvents, or cyclodextrin-based vehicles is required for administration. The compound is rapidly metabolized to less active forms. Half-life is relatively short (hours) compared to vitamin D precursors. Elimination occurs via hepatic metabolism and biliary excretion.
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| Toxicity/Toxicokinetics |
As a vitamin D metabolite, calcitetrol has calcemic activity and can cause hypercalcemia at high doses. Potential adverse effects include hypercalcemia, hypercalciuria, nephrolithiasis, and soft tissue calcification. Monitoring of serum calcium is essential. The compound is for research use only and not for clinical use.
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| References |
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| Additional Infomation |
See also: 1,24,25-trihydroxyvitamin D3 (note moved to).
Calcitetrol (1alpha, 24, 25-Trihydroxyvitamin D3) is the hormonally active form of vitamin D with three hydroxyl groups. It is a vitamin D receptor (VDR) agonist and a potent regulator of calcium and phosphate homeostasis. Calcitetrol is used in research to study vitamin D metabolism, calcium homeostasis, and VDR-mediated gene regulation. It is not an approved therapeutic agent; it is a research compound for studying vitamin D biology. The compound is available as a research-grade product. |
| Molecular Formula |
C₂₇H₄₄O₄
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|---|---|
| Molecular Weight |
432.64
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| Exact Mass |
432.324
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| CAS # |
72203-93-1
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| PubChem CID |
9910685
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| Appearance |
White to off-white solid powder
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| LogP |
4.675
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
31
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| Complexity |
721
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| Defined Atom Stereocenter Count |
6
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| SMILES |
C[C@H](CCC(C(C)(C)O)O)[C@H]1CC[C@@H]\2[C@@]1(CCC/C2=C\C=C/3\C[C@H](C[C@@H](C3=C)O)O)C
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| InChi Key |
WFZKUWGUJVKMHC-QPGHTDHKSA-N
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| InChi Code |
InChI=1S/C27H44O4/c1-17(8-13-25(30)26(3,4)31)22-11-12-23-19(7-6-14-27(22,23)5)9-10-20-15-21(28)16-24(29)18(20)2/h9-10,17,21-25,28-31H,2,6-8,11-16H2,1,3-5H3/b19-9+,20-10-/t17-,21-,22-,23+,24+,25?,27-/m1/s1
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| Chemical Name |
(1R,3S,5Z)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(2R)-5,6-dihydroxy-6-methylheptan-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol
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| Synonyms |
1α, 24, 25-Trihydroxy VD31alpha, 24, 25-Trihydroxy VD3
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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. |
| 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 : ~100 mg/mL (~231.14 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3114 mL | 11.5570 mL | 23.1139 mL | |
| 5 mM | 0.4623 mL | 2.3114 mL | 4.6228 mL | |
| 10 mM | 0.2311 mL | 1.1557 mL | 2.3114 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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