Tetrahydrocortisol

Name: Tetrahydrocortisol
Brand: MedChemExpress
SKU: HY-129630
Rating: 4.5 (0 reviews)

Cat. No.: HY-129630 Purity: 99.91%: Data Sheet
COA

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Tetrahydrocortisol is a metabolite of Hydrocortisone (HY-N0583) that fails to activate glucocorticoid receptor. Tetrahydrocortisol inhibits Dexamethasone (HY-14648)-induced formation of cross-linked actin networks. Tetrahydrocortisol acts as a synergist to enhance the activity of anticancer agents. Tetrahydrocortisol can be used in the research of primary open-angle glaucoma, ocular hypertension, lung cancer and breast cancer.

For research use only. We do not sell to patients.

Tetrahydrocortisol Chemical Structure

CAS No. : 53-02-1

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
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Other Forms of Tetrahydrocortisol:

Tetrahydrocortisol-d₅ In-stock

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

Human Endogenous Metabolite

In Vitro

Tetrahydrocortisol (0.01-1 μM; 2-14 days) inhibits dexamethasone-induced formation of actin cross-linked networks in human primary trabecular meshwork cells, with an IC₅₀ of 0.57 μM after 14 days of treatment. When used alone, it increases microfilament bundling and partially reverses dexamethasone-induced microtubule disorganization^[1].
Tetrahydrocortisol (5-500 μM; 24 h) exhibits extremely weak cytotoxicity against EMT-6 mouse breast tumor cells, yet at 100 μM for 24 h, it protects normoxic EMT-6 cells from the cytotoxic effects of various anticancer agents and X-rays. Its protective effect is attenuated under acidic pH or hypoxic conditions^[2].
Tetrahydrocortisol (0.1 mM; 48 h) slightly increases the packed cell volume of quiescent SM-C1 fibroblasts isolated from rat carrageenan granulomas, and simultaneously induces minor changes in the content and distribution ratio of intracellular free amino acids^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Tetrahydrocortisol (125 mg/kg; s.c.; continuous infusion; 14 days) alone produces a modest 0.6-day tumor growth delay in Lewis lung carcinoma-bearing mice, reduces CDDP (HY-17394) and Melphalan (HY-17575)-induced tumor growth delay, enhances Cyclophosphamide (HY-17420) and radiation-induced tumor growth delay, and does not affect lung metastasis number or size when administered alone or with cytotoxic therapies^[2].
Tetrahydrocortisol (125 mg/kg; s.c.; continuous infusion; 14 days) in combination with β-Cyclodextrin tetradecasulfate (HY-107201) and minocycline (HY-17412A) produces a 1.2-day tumor growth delay alone, greatly enhances cytotoxic therapy-induced tumor growth delay, reduces the percentage of large lung metastases when administered alone, and further reduces lung metastasis number and size when combined with most cytotoxic therapies^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	C57BL (8-10-week-old male; s.c. implantation of 2 × 10⁶ Lewis lung carcinoma cells)^[2]
Dosage:	125 mg/kg (1:1 molar ratio with β-cyclodextrin tetradecasulfate)
Administration:	s.c.; continuous infusion; 14 days (days 4 to 18 post-tumor implantation)
Result:	Produced a tumor growth delay of 0.6 days. Reduced the CDDP-induced tumor growth delay from 4.5 days to 2.2 days. Reduced the melphalan-induced tumor growth delay from 2.7 days to 1.1 days. Increased the single-dose cyclophosphamide-induced tumor growth delay from 7.2 days to 16.2 days. Increased the three-dose cyclophosphamide-induced tumor growth delay from 21.5 days to 36.8 days. Increased the single-dose radiation-induced tumor growth delay from 6.2 days to 8.3 days. Increased the fractionated radiation-induced tumor growth delay from 4.4 days to 7.1 days. Did not alter the total number of lung metastases (mean 14.5) or the percentage of large (vascularized) metastases (69%) compared to untreated controls. Did not alter the number of lung metastases produced by CDDP, melphalan, cyclophosphamide, or radiation.

Molecular Weight

366.49

Formula

C₂₁H₃₄O₅

CAS No.

53-02-1

Appearance

Solid

Color

White to off-white

SMILES

C[C@@]12[C@](C(CO)=O)(O)CC[C@@]1([H])[C@]3([H])CC[C@]4([H])C[C@H](O)CC[C@]4(C)[C@@]3([H])[C@@H](O)C2

Structure Classification

Steroids

Initial Source

Endogenous metabolite

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (136.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

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Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (3.41 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (3.41 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.25 mg/mL (3.41 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.91%

Select Batch:

Data Sheet (280 KB) SDS (736 KB)

COA (251 KB) HNMR (315 KB) RP-HPLC (240 KB) LCMS (122 KB) Elemental Analysis Report (109 KB)

Handling Instructions (2659 KB)

References

[1]. Clark AF, et al. Inhibition of dexamethasone-induced cytoskeletal changes in cultured human trabecular meshwork cells by tetrahydrocortisol. Invest Ophthalmol Vis Sci. 1996;37(5):805-813. [Content Brief]

[2]. Teicher BA, et al. beta-cyclodextrin tetradecasulfate/tetrahydrocortisol +/- minocycline as modulators of cancer therapies in vitro and in vivo against primary and metastatic Lewis lung carcinoma. Cancer Chemother Pharmacol. 1993;33(3):229-238. [Content Brief]

[3]. Sei-itsu Murota, et al. Effects of cortisol and tetrahydrocortisol on the cloned fibroblast derived from rat carrageenin granuloma. Biochemical Pharmacology. Volume 25, Issue 9, 1 May 1976.

[4]. Feng L, et al. Discovery of Natural Resorcylic Acid Lactones as Novel Potent Copper Ionophores Covalently Targeting PRDX1 to Induce Cuproptosis for Triple-Negative Breast Cancer Therapy. ACS Cent Sci. 2025 Feb 10;11(2):357-370.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.7286 mL	13.6429 mL	27.2859 mL	68.2147 mL
	5 mM	0.5457 mL	2.7286 mL	5.4572 mL	13.6429 mL
	10 mM	0.2729 mL	1.3643 mL	2.7286 mL	6.8215 mL
	15 mM	0.1819 mL	0.9095 mL	1.8191 mL	4.5476 mL
	20 mM	0.1364 mL	0.6821 mL	1.3643 mL	3.4107 mL
	25 mM	0.1091 mL	0.5457 mL	1.0914 mL	2.7286 mL
	30 mM	0.0910 mL	0.4548 mL	0.9095 mL	2.2738 mL
	40 mM	0.0682 mL	0.3411 mL	0.6821 mL	1.7054 mL
	50 mM	0.0546 mL	0.2729 mL	0.5457 mL	1.3643 mL
	60 mM	0.0455 mL	0.2274 mL	0.4548 mL	1.1369 mL
	80 mM	0.0341 mL	0.1705 mL	0.3411 mL	0.8527 mL
	100 mM	0.0273 mL	0.1364 mL	0.2729 mL	0.6821 mL