| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg | |||
| Other Sizes |
| Targets |
Vitamin D receptor (VDR) / calcium channels.
|
|---|---|
| ln Vitro |
Tachysterol 3 was found in human serum at a concentration of 7.3 ± 2.5 ng/mL [2]. Tachysterol 3-hydroxy derivatives interact with the ligand-binding domains (LBD) of liver ) exhibits high affinity binding [2]. Tachysterol 3 can be hydroxylated by CYP11A1 and CYP27A1 [2].
Experimentally, tachysterol causes an increase in intestinal calcium absorption and urinary excretion of calcium, as well as a rise in serum calcium concentration; it shares some calcium-regulating activity with vitamin D but appears to be less potent; its mechanism is similar to dihydrotachysterol in mobilizing bone calcium. |
| ln Vivo |
In animal studies (including anephric rat models), tachysterol demonstrates the ability to elevate serum calcium levels and enhance calcium absorption and urinary excretion; it is effective even in the absence of functional renal tissue, indicating that it does not require renal hydroxylation for activity.
|
| Enzyme Assay |
Binding to the vitamin D receptor (VDR) can be evaluated by competitive radioligand binding assays using recombinant VDR protein; tachysterol is incubated with 3H-1,25-dihydroxyvitamin D3; after separation of bound and free ligand, radioactivity is measured to calculate relative binding affinity.
|
| Cell Assay |
Calcium transport activity is typically assessed using intestinal cell lines such as Caco-2; cells are seeded on permeable filters, treated with tachysterol, and calcium flux across the monolayer is measured using 45Ca or fluorescent indicators; alternatively, everted gut sacs from treated animals are used.
|
| Animal Protocol |
Rodent models (including anephric rats) are used; animals receive tachysterol via oral or intraperitoneal administration; blood samples are collected to measure serum calcium levels; intestinal calcium transport is assessed by in situ ligated loop or everted gut sac techniques; urinary calcium excretion is collected and quantified.
|
| ADME/Pharmacokinetics |
PK properties not fully detailed; as a vitamin D-like sterol, tachysterol is expected to be lipid-soluble with slow clearance, distributed to adipose tissue; metabolism likely involves hydroxylation steps; specific half-life, oral bioavailability, and plasma protein binding are not well characterized.
|
| Toxicity/Toxicokinetics |
Toxicity: comprehensive toxicological data are lacking; as a vitamin D analog, high doses may lead to hypercalcemia and potential soft tissue calcification; no formal toxicity studies have been published; historically used in experimental settings without reported significant acute toxicity.
|
| References |
[1]. Cecilia Cisneros, et al. The Role of Tachysterol in Vitamin D Photosynthesis - A Non-Adiabatic Molecular Dynamics Study. Phys Chem Chem Phys. 2017 Feb 22;19(8):5763-5777.
[2]. Slominski AT, et al. Metabolic activation of tachysterol3 to biologically active hydroxyderivatives that act on VDR, AhR, LXRs, and PPARγ receptors. FASEB J. 2022 Aug;36(8):e22451. |
| Additional Infomation |
Tachysterol 3 is a hydroxyl-opening ring-sterol produced by photoisomerization of vitamin D3 precursor. It plays a metabolic role in the human body. It is an open-ring cholesterane, a hydroxyl-opening ring-sterol, and a secondary alcohol.
Tachysterol is a research tool compound used primarily in vitamin D metabolism and photochemistry studies; it is not an approved therapeutic; it has no clinical trials or regulatory approval (FDA/EMA); it is used as a reference standard and for investigating the structure-activity relationship of vitamin D analogs in calcium homeostasis. |
| Molecular Formula |
C27H44O
|
|---|---|
| Molecular Weight |
384.63766
|
| Exact Mass |
384.339
|
| CAS # |
17592-07-3
|
| Related CAS # |
Previtamin D3;1173-13-3
|
| PubChem CID |
5283713
|
| Appearance |
Colorless to light yellow oil
|
| Vapour Pressure |
6.45E-12mmHg at 25°C
|
| Source |
Endogenously produced metabolite
|
| LogP |
7.619
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
1
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
28
|
| Complexity |
622
|
| Defined Atom Stereocenter Count |
5
|
| SMILES |
CC(CCCC(C1CCC2C(=CCCC12C)/C=C/C1CC(O)CCC=1C)C)C
|
| InChi Key |
YUGCAAVRZWBXEQ-FMCTZRJNSA-N
|
| InChi Code |
InChI=1S/C27H44O/c1-19(2)8-6-9-21(4)25-15-16-26-22(10-7-17-27(25,26)5)12-13-23-18-24(28)14-11-20(23)3/h10,12-13,19,21,24-26,28H,6-9,11,14-18H2,1-5H3/b13-12+/t21-,24+,25-,26+,27-/m1/s1
|
| Chemical Name |
(1S)-3-[(E)-2-[(1R,3aR,7aR)-7a-methyl-1-[(2R)-6-methylheptan-2-yl]-1,2,3,3a,6,7-hexahydroinden-4-yl]ethenyl]-4-methylcyclohex-3-en-1-ol
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~260.0 mM; with ultrasonication)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.50 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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 (6.50 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Suspended solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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. Solubility in Formulation 3: ≥ 2.5 mg/mL (6.50 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 DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well.  (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5998 mL | 12.9992 mL | 25.9983 mL | |
| 5 mM | 0.5200 mL | 2.5998 mL | 5.1997 mL | |
| 10 mM | 0.2600 mL | 1.2999 mL | 2.5998 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.