| Size | Price | Stock | Qty |
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| Targets |
Tetrahydrocortisol acts as an antagonist at the GABAA receptor. It dose-dependently inhibits dexamethasone-induced actin network formation in human trabecular meshwork cells (IC50 = 5.7 × 10⁻⁷ M). By antagonizing GABAA receptors, this neurosteroid modulates neuronal excitability. Additionally, Tetrahydrocortisol has been shown to partially reverse microtubule changes, indicating cytoskeletal modulation. Its ability to lower intraocular pressure suggests involvement in ocular physiology.
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| ln Vitro |
Tetrahydrocortisol demonstrates in vitro activity in human trabecular meshwork cells. It dose-dependently inhibits dexamethasone (10⁻⁷ M)-induced actin network formation with an IC50 of 5.7 × 10⁻⁷ M over a treatment period of up to 14 days. The compound also partially reverses microtubule changes induced by dexamethasone, indicating its role in cytoskeletal modulation. These in vitro effects suggest that Tetrahydrocortisol can influence cellular structure and function through its antagonism of GABAA receptors and modulation of the cytoskeleton.
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| ln Vivo |
In vivo, Tetrahydrocortisol has been shown to lower intraocular pressure. As a metabolite of cortisol and a neurosteroid, it may contribute to the physiological effects of glucocorticoid metabolism. The compound is naturally present in the body and is generated by lymphocytes. Its levels are reported to be elevated in patients with cancer, suggesting a potential role in disease pathology or as a biomarker. Detailed in vivo pharmacological studies, including specific animal models and dose-response relationships, are not extensively provided in the available literature.
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| Enzyme Assay |
In vitro receptor binding assays for Tetrahydrocortisol at the GABAA receptor can be performed using membrane preparations from rat brain or recombinant GABAA receptors expressed in cell lines. Radiolabeled ligands such as [³H]muscimol (for the GABA binding site) or [³H]flunitrazepam (for the benzodiazepine site) are used. Membrane aliquots are incubated with the radioligand and varying concentrations of Tetrahydrocortisol at 4°C for 60-120 minutes. Non-specific binding is determined in the presence of excess unlabeled GABA or diazepam. Bound radioactivity is collected by filtration and quantified by scintillation counting. IC50 or Ki values are calculated from competition curves.
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| Cell Assay |
For in vitro cell-based assays, human trabecular meshwork cells are cultured in appropriate medium. Cells are treated with dexamethasone (10⁻⁷ M) to induce actin network formation, followed by co-treatment with Tetrahydrocortisol at various concentrations (typically 0.1-10 μM) for up to 14 days. Actin filament organization is visualized by phalloidin staining and fluorescence microscopy. Microtubule changes are assessed by immunostaining for β-tubulin. Image analysis software is used to quantify actin network formation and microtubule organization. Cell viability is monitored throughout the treatment period. IC50 values are calculated from dose-response curves.
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| Animal Protocol |
In vivo animal studies for Tetrahydrocortisol are not extensively detailed in the available literature. As a naturally occurring cortisol metabolite, its effects on intraocular pressure could be studied in animal models of glaucoma or ocular hypertension using topical or systemic administration. Rodent models are commonly used to assess effects on intraocular pressure, with measurements taken using a tonometer before and after treatment. The compound's role in cancer metabolism could be investigated in tumor-bearing animal models. Standard protocols would involve dose-response studies and assessment of pharmacokinetic and pharmacodynamic parameters.
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| ADME/Pharmacokinetics |
Tetrahydrocortisol is soluble in DMSO (40 mg/mL, 109.14 mM). For in vivo administration, it can be formulated in 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% saline at 1 mg/mL (2.73 mM). The compound should be stored at low temperature, away from moisture, with powder stable at -20°C for 3 years and in solvent at -80°C for 1 year. Detailed pharmacokinetic parameters (absorption, distribution, metabolism, excretion, half-life) for Tetrahydrocortisol are not extensively characterized in the available literature, as it is an endogenous metabolite rather than a xenobiotic drug.
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| Toxicity/Toxicokinetics |
Tetrahydrocortisol is an endogenous metabolite and is generally considered to have low toxicity. As a neurosteroid and GABAA receptor antagonist, it may modulate neuronal excitability, but adverse effects are not well-documented. The compound is naturally present in the body and is generated by lymphocytes. Elevated levels in cancer patients suggest a possible association with disease, but causality and toxicity are not established. Standard toxicology studies would be required for therapeutic applications, but specific toxicity data are not provided in the available references.
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| References |
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| Additional Infomation |
Tetrahydrocorticosteroids are 3α-hydroxysteroids, 11β-hydroxysteroids, 17α-hydroxysteroids, 21-hydroxysteroids, 20-oxosteroids, glucocorticoids, primary α-hydroxy ketones, and tertiary α-hydroxy ketones. They are derived from the hydrogenation of 5β-pregnane.
Tetrahydrocortisol (tetrahydrohydrocortisone) is a neurosteroid and a metabolite of cortisol. It acts as a GABAA receptor antagonist and has been shown to lower intraocular pressure. The compound is naturally generated by lymphocytes and is more prevalent in cancer patients, suggesting potential as a biomarker for cancer or metabolomics research. Tetrahydrocortisol dose-dependently inhibits dexamethasone-induced actin network formation in human trabecular meshwork cells (IC50 = 5.7 × 10⁻⁷ M) and partially reverses microtubule changes, indicating cytoskeletal modulation. No approved therapeutic status is reported. |
| Molecular Formula |
C21H34O5
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|---|---|
| Molecular Weight |
366.49
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| Exact Mass |
366.241
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| CAS # |
53-02-1
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| Related CAS # |
Tetrahydrocortisol-d5
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| PubChem CID |
5864
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| Appearance |
White to off-white solid powder
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| Density |
1.253g/cm3
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| Boiling Point |
65-67ºC(lit.)
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| Melting Point |
-108ºC(lit.)
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| Flash Point |
297.6ºC
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| Index of Refraction |
n20/D 1.407(lit.)
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| LogP |
1.653
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| Hydrogen Bond Donor Count |
4
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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 |
593
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| Defined Atom Stereocenter Count |
9
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| SMILES |
C[C@]12CC[C@H](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)O
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| InChi Key |
AODPIQQILQLWGS-GXBDJPPSSA-N
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| InChi Code |
InChI=1S/C21H34O5/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/h12-16,18,22-24,26H,3-11H2,1-2H3/t12-,13-,14+,15+,16+,18-,19+,20+,21+/m1/s1
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| Chemical Name |
2-hydroxy-1-[(3R,5R,8S,9S,10S,11S,13S,14S,17R)-3,11,17-trihydroxy-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,14,15,16-tetradecahydrocyclopenta[a]phenanthren-17-yl]ethanone
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| Synonyms |
Ba 2682; Urocortisol; Tetrahydrocortisol
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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 : ~50 mg/mL (~136.43 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (3.41 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 12.5 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: ≥ 1.25 mg/mL (3.41 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 12.5 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: ≥ 1.25 mg/mL (3.41 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 | 2.7286 mL | 13.6429 mL | 27.2859 mL | |
| 5 mM | 0.5457 mL | 2.7286 mL | 5.4572 mL | |
| 10 mM | 0.2729 mL | 1.3643 mL | 2.7286 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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