| Size | Price | Stock | Qty |
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| Targets |
Vitamin D receptor (VDR) and histone deacetylases (HDACs). Triciferol acts as a dual ligand: it agonizes VDR and antagonizes HDAC activity. The VDR agonism promotes calcium homeostasis and cell differentiation, while HDAC inhibition enhances gene expression and has anticancer effects.
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| ln Vitro |
Triciferol (0–1000 nM; 0-72 hours) is a far more effective agent in inhibiting the growth of human MDA-MB231 breast cancer cells that do not express estrogen receptors[1]. Equimolar doses of 1,25D elicit ≼2.5-fold lower rates of cell death in MCF-7 cells treated with triciferol (100-1000 nM)[1].
Triciferol binds directly to VDR with an IC₅0 of 87 nM and acts as an agonist with 1,25D-like potency on several 1,25D target genes. It induces significant tubulin hyperacetylation. It has antiproliferative and cytotoxic activities. |
| ln Vivo |
No detailed in vivo activity data has been reported for triciferol in available literature. It has been investigated for applications in osteoporosis, chronic kidney disease-related mineral disorders, and dermatological conditions.
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| Enzyme Assay |
VDR binding assays: Triciferol is incubated with purified VDR protein and its radiolabeled ligand (e.g., 3H-1,25D). Binding affinity is measured by scintillation counting or fluorescence polarization. IC₅0 values are calculated from competition curves. HDAC activity assays are performed using fluorogenic substrates.
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: MDA-MB231 breast cancer cells Tested Concentrations: 0-10000 nM Incubation Duration: 0-72 hrs (hours) Experimental Results: Growth inhibition was statistically Dramatically different from that of 1,25D at concentrations of 1 nM or above. Cell-based assays: Cells are treated with triciferol, and VDR target gene expression is measured by qPCR or reporter gene assays. HDAC inhibition is assessed by measuring histone acetylation levels by Western blot. Antiproliferative activity is measured using MTT or CellTiter-Glo assays. |
| Animal Protocol |
Animal models of osteoporosis or chronic kidney disease could be used to evaluate triciferol in vivo. The compound is designed to maintain therapeutic benefits of vitamin D while minimizing hypercalcemia risk.
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| ADME/Pharmacokinetics |
Triciferol has a molecular weight of 429.59 and a molecular formula of C2₆H3₉NO4. It is a synthetic vitamin D analog designed to have combined VDR agonist and HDAC antagonist activities. Detailed PK parameters have not been reported.
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| Toxicity/Toxicokinetics |
No detailed toxicity data has been published for triciferol. Its modified structure aims to maintain therapeutic benefits of vitamin D while minimizing risks of hypercalcemia during prolonged treatment. As a research compound, it is not intended for human therapeutic use.
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| References | |
| Additional Infomation |
Triciferol is a multiple ligand with combined VDR agonist and HDAC antagonist activities. It binds directly to VDR (IC₅0 = 87 nM) and functions as an agonist with 1,25D-like potency. It has been investigated for osteoporosis, chronic kidney disease, and dermatological conditions. The compound is for research use only.
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| Molecular Formula |
C26H39NO4
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|---|---|
| Molecular Weight |
429.592168092728
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| Exact Mass |
429.287
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| CAS # |
957214-00-5
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| PubChem CID |
17757734
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| Appearance |
White to off-white solid powder
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| LogP |
4.3
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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 |
5
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| Heavy Atom Count |
31
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| Complexity |
768
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| Defined Atom Stereocenter Count |
6
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| SMILES |
C[C@@]12[C@@H]([C@H](C)/C=C(\C)/C=C/C(=O)NO)CC[C@H]1/C(/CCC2)=C/C=C1/C[C@@H](O)C[C@H](O)C/1
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| InChi Key |
QOEMKJVIXGOYHR-SYOSPHLFSA-N
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| InChi Code |
InChI=1S/C26H39NO4/c1-17(6-11-25(30)27-31)13-18(2)23-9-10-24-20(5-4-12-26(23,24)3)8-7-19-14-21(28)16-22(29)15-19/h6-8,11,13,18,21-24,28-29,31H,4-5,9-10,12,14-16H2,1-3H3,(H,27,30)/b11-6+,17-13+,20-8+/t18-,21-,22-,23-,24+,26-/m1/s1
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| Chemical Name |
(2E,4E,6R)-6-[(1R,3aS,4E,7aR)-4-[2-[(3R,5R)-3,5-dihydroxycyclohexylidene]ethylidene]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-1-yl]-N-hydroxy-4-methylhepta-2,4-dienamide
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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 (232.78 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 | 2.3278 mL | 11.6390 mL | 23.2780 mL | |
| 5 mM | 0.4656 mL | 2.3278 mL | 4.6556 mL | |
| 10 mM | 0.2328 mL | 1.1639 mL | 2.3278 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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