| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
PPARγ
Vitamin D Receptor (VDR), Aryl Hydrocarbon Receptor (AhR), Liver X Receptor alpha/beta (LXRalpha/beta), and Peroxisome Proliferator-Activated Receptor gamma (PPARgamma). 25-Hydroxytachysterol3 is an activator of these receptors. |
|---|---|
| ln Vitro |
In cell-free assays, 25-Hydroxytachysterol3 activates VDR, AhR, LXRs, and PPARgamma, stimulating the expression of CYP24A1, a target gene of VDR. It inhibits the proliferation of epidermal keratinocytes and dermal fibroblasts, stimulates the expression of differentiation- and antioxidant-related genes in keratinocytes. Specific IC₅0 values are not provided.
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| ln Vivo |
This entry is not available. As a Vitamin D3 metabolite, 25-Hydroxytachysterol3 is expected to have in vivo effects on calcium homeostasis, cell proliferation, and immune modulation through its activity on VDR and other nuclear receptors. A general in vivo activity is the regulation of CYP24A1 expression in the kidney and other target tissues.
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| Enzyme Assay |
A general cell-free protocol for assessing VDR activation: A time-resolved fluorescence resonance energy transfer (TR-FRET) assay is used. Recombinant GST-tagged human VDR protein (2 nM) is incubated with a biotinylated SRC2-2 peptide (100 nM) and a fluorescently labeled vitamin D response element (VDRE) probe (10 nM) in a buffer (50 mM Tris-HCl, pH 7.4, 150 mM NaCl, 1 mM DTT, 0.01% Tween-20) at room temperature for 2 hours. The reaction also contains Europium-labeled anti-GST antibody (2 nM) and streptavidin-conjugated XL665 (20 nM). Varying concentrations of 25-Hydroxytachysterol3 (0.1 nM to 10 uM) are added to assess agonist activity. The TR-FRET signal is measured by a microplate reader. An increase in FRET signal indicates VDR activation and recruitment of the coactivator peptide. The EC₅0 is calculated from the dose-response curve.
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| Cell Assay |
A general cellular protocol for assessing VDR activity: HaCaT human keratinocytes are seeded in 96-well plates at 10,000 cells/well. After 24 hours, the cells are treated with various concentrations of 25-Hydroxytachysterol3 (0.1 nM to 10 uM) for 48 hours. Cell proliferation is assessed using a BrdU incorporation assay. For gene expression analysis, HaCaT cells are treated with the compound (100 nM) for 24 hours. Total RNA is extracted, and the expression of CYP24A1, involucrin (differentiation marker), and heme oxygenase-1 (antioxidant marker) is measured by qRT-PCR using TaqMan probes. Normalization is performed using GAPDH as a housekeeping gene.
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| Animal Protocol |
A general in vivo protocol for studying the effects of vitamin D metabolites: Eight-week-old female C57BL/6 mice are administered 25-Hydroxytachysterol3 via intraperitoneal injection at doses of 0.1, 0.3, and 1.0 ug/kg body weight daily for 7 days. The vehicle control group receives an equal volume of vehicle (e.g., 10% ethanol in propylene glycol). Blood samples are collected at the end of the treatment period. Serum calcium and phosphate levels are measured using colorimetric kits. The kidneys are harvested, and total RNA is extracted for qRT-PCR analysis of CYP24A1 and CYP27B1 expression. Skin tissues are collected for histopathological examination to assess epidermal thickness, and for RNA extraction to measure gene expression of differentiation markers (keratin 1, loricrin, filaggrin) and proliferation markers (Ki-67).
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| ADME/Pharmacokinetics |
General pharmacokinetic protocol for vitamin D metabolites: Male Sprague-Dawley rats are administered 25-Hydroxytachysterol3 via oral gavage (PO, 50 ug/kg) and intravenous (IV, 5 ug/kg) injection. The compound is formulated in a vehicle such as 10% ethanol, 40% propylene glycol, and 50% PBS. Blood samples are collected at 0.083, 0.25, 0.5, 1, 2, 4, 8, 12, and 24 hours post-dose. Plasma concentrations are quantified by LC-MS/MS with a lower limit of quantitation of 0.1 ng/mL. PK parameters (Cmax, Tmax, AUC, t½, clearance, Vd, and oral bioavailability) are calculated. As a lipophilic secosteroid, the compound is expected to have a long half-life and extensive tissue distribution.
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| Toxicity/Toxicokinetics |
General toxicity protocol for vitamin D metabolites: A 28-day repeated-dose oral toxicity study is performed in Sprague-Dawley rats. 25-Hydroxytachysterol3 is administered via oral gavage at doses of 0.1, 0.5, and 2.5 ug/kg/day. Clinical signs, body weight, and food consumption are recorded daily. Blood samples are collected at the end of the study for hematology (CBC) and serum chemistry (calcium, phosphate, magnesium, BUN, creatinine, ALT, AST, total protein, albumin). Urine is collected for measurement of calcium and creatinine levels. Gross necropsy is performed, and organ weights (kidney, liver, heart, lung, spleen) are recorded. Histopathological examination of the kidneys (to assess calcification), bone (femur and tibia), and other organs is conducted. Hypercalcemia and soft tissue calcification are common toxicity endpoints for excessive vitamin D receptor activation.
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| References | |
| Additional Infomation |
25-Hydroxytachysterol 3 is a form of vitamin D.
25-Hydroxytachysterol3 is the metabolite of Vitamin D3 . The molecular formula is C2₇H44O2, and the molecular weight is 400.64. The compound has a density of 1.1+/-0.1 g/cm3 and a boiling point of 528.8+/-33.0degC. 25-Hydroxytachysterol3 is soluble in organic solvents such as ethanol and DMSO. For storage, the compound should be kept at -20degC, protected from light, and stored under nitrogen. The purity is 98.89%. This compound is a reference standard for studying vitamin D metabolism and its biological activities. The product is for research use only, not for human or veterinary use. |
| Molecular Formula |
C27H44O2
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|---|---|
| Molecular Weight |
400.64
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| Exact Mass |
400.334
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| CAS # |
39932-44-0
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| PubChem CID |
101670588
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| Appearance |
Solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
528.8±33.0 °C at 760 mmHg
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| Flash Point |
221.2±20.0 °C
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| Vapour Pressure |
0.0±3.2 mmHg at 25°C
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| Index of Refraction |
1.590
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| LogP |
7.51
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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 |
7
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| Heavy Atom Count |
29
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| Complexity |
668
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| Defined Atom Stereocenter Count |
5
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| SMILES |
OC(C)(C)CCC[C@@H](C)[C@H]1CC[C@H]2C(/C=C/C3=C(C)CC[C@@H](C3)O)=CCC[C@]12C
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| InChi Key |
UVVWRMXOHIVZBN-RPAZCORHSA-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/h9,11-12,20,23-25,28-29H,6-8,10,13-18H2,1-5H3/b12-11+/t20-,23+,24-,25+,27-/m1/s1
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| Chemical Name |
(1S)-3-[(E)-2-[(1R,3aR,7aR)-1-[(2R)-6-hydroxy-6-methylheptan-2-yl]-7a-methyl-1,2,3,3a,6,7-hexahydroinden-4-yl]ethenyl]-4-methylcyclohex-3-en-1-ol
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.4960 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.
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