| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
5beta-Dihydrocortisol has multiple targets. As a metabolite of cortisol, it can act as a potential mineralocorticoid, influencing sodium and water balance. It can potentiate the activity of glucocorticoids, such as raising intraocular pressure. Furthermore, it has been shown to act as an apoptosis activator, inducing cell death in certain types of breast cancer cells. Its mechanism involves the estrogen receptor (ER) pathway in some contexts.
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| ln Vitro |
5β-Dihydrocortisol (10-100 μM; 48 h) reduces the viability of MCF-7 cells with an IC50 of 27.59 μM[2]. In MCF-7 cells, 5β-Dihydrocortisol (14 μM; 24 h) causes 2.5% late and 35.6% early apoptosis[2]. Human serum albumin (HAS) exhibits intrinsic fluorescence with a maximum emission peak at 360 nm. It can be quenched with 5β-Dihydrocortisol (1-10 μM; 48 h) without causing any change in the fluorescence peak.
In vitro, 5beta-Dihydrocortisol has been shown to induce apoptosis in breast cancer cells. This suggests that the compound is not merely an inactive catabolite but has significant biological activity. By inducing apoptosis, it may play a role in regulating cell turnover in hormone-sensitive tissues. Additionally, it can potentiate glucocorticoid activity, as measured by its ability to increase intraocular pressure in cellular models of the eye. |
| ln Vivo |
In juvenile rabbits, the intraocular pressure (IOP) is raised by topical application of Dexamethasone (0.06%) more effectively when 5β-Dihydrocortisol (0.1-1.0%; 18 d) is used[3].
In vivo, 5beta-Dihydrocortisol has been shown to be a potential mineralocorticoid, meaning it can influence renal function and electrolyte balance. It also enhances glucocorticoid activity, which contributes to raising intraocular pressure. These properties make it a significant compound in the study of conditions like glaucoma (via its effects on the eye) and breast cancer (via its apoptosis-inducing properties). It is a naturally occurring steroid that is measured as a biomarker. |
| Enzyme Assay |
For in vitro receptor binding and activity assays, 5beta-Dihydrocortisol is dissolved in an organic solvent like DMSO. For mineralocorticoid receptor (MR) assays, it is diluted in assay buffer and tested in a competitive binding assay using [3H]-aldosterone and MR-expressing cells or isolated receptors. For apoptosis studies, breast cancer cell lines (e.g., MCF-7) are treated with the compound, and cell viability is measured using the MTT assay or flow cytometry. To study its effect on intraocular pressure, human trabecular meshwork cells are cultured and treated, and the expression of glaucoma-related genes is measured via qPCR.
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: MCF-7 and HEK 293 cells Tested Concentrations: 10, 20, 40, 60, 80, 100 μM Incubation Duration: 48 hrs (hours) Experimental Results: Inhibited the viability of MCF-7 cells in a dose -dependent manner. No toxicity in terms of cell viability was observed with HEK293 cell line. Apoptosis Analysis[2] Cell Types: MCF-7 cells Tested Concentrations: 14 μM Incubation Duration: 24 hrs (hours) Experimental Results: Induced 35.6% and 2.5% of early and late apoptosis. For in vitro cell-based experiments to study apoptosis, breast cancer cells (e.g., MCF-7 or T47D) are seeded in 96-well plates. The next day, they are treated with various concentrations of 5beta-Dihydrocortisol (e.g., 0.1-100 uM). After 24-72 hours of incubation, cell viability is assessed using the MTT or CellTiter-Glo assay. An increase in apoptosis can be confirmed using an Annexin V-FITC/PI staining kit and flow cytometry. For intraocular pressure studies, human trabecular meshwork cells are treated with the compound, and markers of glaucoma (e.g., myocilin, MMPs) are measured by qPCR or Western blot. |
| Animal Protocol |
For in vivo animal experiments, 5beta-Dihydrocortisol can be used to study its effects on blood pressure, electrolyte balance, or intraocular pressure. For blood pressure studies, an animal model (e.g., a rat) is fitted with a telemetry probe or tail-cuff. The compound is administered, often intravenously (i.v.) or intraperitoneally (i.p.), in a suitable vehicle. Blood pressure and heart rate are monitored continuously. For intraocular pressure studies, a rodent model (mouse or rat) is used, and the compound is administered via topical eye drops or intravitreal injection. Intraocular pressure is measured using a tonometer (e.g., TonoLab) before and after administration.
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| ADME/Pharmacokinetics |
5beta-Dihydrocortisol is an endogenous steroid metabolite. As an endogenous compound, it does not have classical pharmacokinetic parameters like an administered drug. It is produced and cleared continuously by the liver and other tissues. In the liver, it is synthesized from cortisol by the enzyme 5beta-reductase and can be further metabolized by conjugation (glucuronidation) before being eliminated in the bile or urine. Its half-life in circulation is short, on the order of minutes to an hour, as it is rapidly cleared.
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| Toxicity/Toxicokinetics |
5beta-Dihydrocortisol is an endogenous steroid and is not considered acutely toxic. At high concentrations, it has been shown to induce apoptosis in breast cancer cells, which is a therapeutic potential rather than an off-target toxicity. For research use, standard laboratory safety precautions for handling organic compounds should be followed. This product is for research use only and not intended for human consumption.
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| References | |
| Additional Infomation |
5β-dihydrocortisol is a 17α-hydroxy-C21-steroid, formed by the hydrogenation of the 4-5 double bond in cortisol to produce the corresponding 5β-steroid. It is a 21-hydroxysteroid, 17α-hydroxy-C21-steroid, 11β-hydroxysteroid, 3-oxo-5β-steroid, primary α-hydroxy ketone, triol, secondary alcohol, diketone, 20-oxosteroid, and tertiary α-hydroxy ketone.
5beta-Dihydrocortisol is not an approved drug. It is an endogenous metabolite and a research biochemical. Its primary applications are in pharmaceutical research and clinical diagnostics. It is used to study the action of the enzyme 5-beta-reductase, which is important for bile acid synthesis and steroid hormone clearance. It is also used as a potential biomarker in metabolomic studies. Its ability to induce apoptosis in cancer cells and raise intraocular pressure makes it a valuable tool for studying breast cancer and the molecular mechanisms underlying glaucoma. |
| Molecular Formula |
C21H32O5
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|---|---|
| Molecular Weight |
364.48
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| Exact Mass |
364.225
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| CAS # |
1482-50-4
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| PubChem CID |
164838
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| Appearance |
White to off-white solid powder
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| Density |
1.249g/cm3
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| Boiling Point |
544.5ºC at 760mmHg
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| Flash Point |
297.1ºC
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| Index of Refraction |
1.569
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| LogP |
1.861
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
26
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| Complexity |
632
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| Defined Atom Stereocenter Count |
8
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| SMILES |
C[C@]12CCC(=O)C[C@H]1CC[C@@H]3[C@@H]2[C@H](C[C@]4([C@H]3CC[C@@]4(C(=O)CO)O)C)O
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| InChi Key |
ACSFOIGNUQUIGE-AIPUTVCKSA-N
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| InChi Code |
InChI=1S/C21H32O5/c1-19-7-5-13(23)9-12(19)3-4-14-15-6-8-21(26,17(25)11-22)20(15,2)10-16(24)18(14)19/h12,14-16,18,22,24,26H,3-11H2,1-2H3/t12-,14+,15+,16+,18-,19+,20+,21+/m1/s1
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| Chemical Name |
(5R,8S,9S,10S,11S,13S,14S,17R)-11,17-dihydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-2,4,5,6,7,8,9,11,12,14,15,16-dodecahydro-1H-cyclopenta[a]phenanthren-3-one
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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 |
| 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: 125 mg/mL (342.95 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.71 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 20.8 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: ≥ 2.08 mg/mL (5.71 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7436 mL | 13.7182 mL | 27.4363 mL | |
| 5 mM | 0.5487 mL | 2.7436 mL | 5.4873 mL | |
| 10 mM | 0.2744 mL | 1.3718 mL | 2.7436 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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