| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
1alpha-Hydroxy VD4 targets the vitamin D receptor (VDR) as a 1α-hydroxyvitamin D analogue. By binding to VDR, it regulates gene expression involved in cell differentiation, calcium homeostasis, and bone metabolism. The compound effectively induces the differentiation of monoblastic leukemia cells, indicating its activity in cellular differentiation pathways.
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|---|---|
| ln Vitro |
In vitro, 1alpha-Hydroxy VD4 effectively induces the differentiation of monoblastic leukemia U937, P39/TSU, and P31/FUJ cells. The compound's ability to promote cell differentiation makes it a valuable tool for studying leukemic cell differentiation and vitamin D signaling pathways. No specific IC₅₀ values have been reported in the available literature.
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| ln Vivo |
In vivo activity of 1alpha-Hydroxy VD4 has not been extensively characterized in animal models. As a vitamin D analogue, it may have effects on calcium homeostasis and bone metabolism similar to other vitamin D compounds. However, specific in vivo efficacy studies have not been detailed in the available literature.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for 1alpha-Hydroxy VD4 typically involve studying its binding to the vitamin D receptor (VDR). The compound is incubated with purified VDR protein or cell lysates containing VDR, and binding affinity is assessed using radioligand binding assays or fluorescence-based assays. Competition assays with labeled 1,25-dihydroxyvitamin D₃ can be used to determine relative binding affinities.
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| Cell Assay |
In vitro cell-based assays for 1alpha-Hydroxy VD4 typically employ monoblastic leukemia cell lines including U937, P39/TSU, and P31/FUJ. Cells are cultured and treated with various concentrations of the compound. Cell differentiation is assessed by measuring expression of differentiation markers (e.g., CD11b, CD14) by flow cytometry, morphological changes, and functional assays such as nitroblue tetrazolium reduction. Cell viability is also assessed.
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| Animal Protocol |
In vivo animal studies with 1alpha-Hydroxy VD4 have not been extensively reported. As a vitamin D analogue, it may be studied in animal models of secondary hyperparathyroidism or metabolic bone disease. However, specific study protocols have not been detailed in the available literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of 1alpha-Hydroxy VD4 have not been characterized. As a vitamin D analogue, it is likely to be metabolized in the liver and kidneys. Specific PK parameters such as half-life, Cₘₐₓ, and bioavailability have not been determined. The compound is intended for research use only.
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| Toxicity/Toxicokinetics |
The toxicity profile of 1alpha-Hydroxy VD4 has not been characterized. As a vitamin D analogue, high doses may cause hypercalcemia and related toxicities. No specific toxicology data are available. The compound is intended for research use only and is not approved for human therapeutic applications.
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| References | |
| Additional Infomation |
1alpha-Hydroxy VD4 is a research-grade vitamin D analogue used in studies of cell differentiation and vitamin D signaling. It is not an approved therapeutic drug and has no clinical trial history. The compound is supplied as a solid powder. Synonyms include 1α-Hydroxy vitamin D4 and 1alpha-Hydroxyvitamin D4.
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| Molecular Formula |
C28H46O2
|
|---|---|
| Molecular Weight |
414.66364
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| Exact Mass |
414.35
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| CAS # |
143032-85-3
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| PubChem CID |
9909748
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| Appearance |
White to off-white solid powder
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| LogP |
6.835
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| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
30
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| Complexity |
672
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| Defined Atom Stereocenter Count |
7
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| SMILES |
C[C@H](CC[C@H](C)C(C)C)[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
|
| InChi Key |
NEETXMRNUNEBRH-GOTXBORWSA-N
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| InChi Code |
InChI=1S/C28H46O2/c1-18(2)19(3)9-10-20(4)25-13-14-26-22(8-7-15-28(25,26)6)11-12-23-16-24(29)17-27(30)21(23)5/h11-12,18-20,24-27,29-30H,5,7-10,13-17H2,1-4,6H3/b22-11+,23-12-/t19-,20+,24+,25+,26-,27-,28+/m0/s1
|
| Chemical Name |
(1R,3S,5Z)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(2R,5S)-5,6-dimethylheptan-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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| 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 : ~50 mg/mL (~120.58 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.03 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 (6.03 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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4116 mL | 12.0581 mL | 24.1161 mL | |
| 5 mM | 0.4823 mL | 2.4116 mL | 4.8232 mL | |
| 10 mM | 0.2412 mL | 1.2058 mL | 2.4116 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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