Cat. No.: HY-B1232

Metyrapone

(Synonyms: Su-4885)

11 Cited Publications

Customer Review

Based on 11 publication(s) in Google Scholar

Metyrapone (Su-4885) is a potent and orally active 11β-hydroxylase inhibitor and an autophagy activator, also inhibits the production of aldosterone. Metyrapone inhibits synthesis of endogenous adrenal corticosteroid, decreases glucocorticoid levels, and also affects behavior and emotion. In addition, Metyrapone increases the efficiency of autophagic process via downregulation of mTOR pathway, and interacts with Pseudomonas putida cytochrome P-450. Metyrapone can be used for researching Cushing's syndrome and depression.

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

Purity: 99.70%
CAS No.: 54-36-4
Formula: C₁₄H₁₄N₂O
Molecular Weight:226.27

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Metyrapone Chemical Structure

CAS No.: 54-36-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (11)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

11β-hydroxylase, Aldosterone, CYP450, Autophagy^[1]^[4]^[5]

All Endogenous Metabolite Isoforms :

All Cytochrome P450 Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
V79	IC₅₀	14.6 nM Compound: 2	Inhibition of human steroid-11beta-hydroxylase expressed in chinese hamster V79 cells using 11-deoxycorticosterone as substrate Inhibition of human steroid-11beta-hydroxylase expressed in chinese hamster V79 cells using 11-deoxycorticosterone as substrate	[PMID: 21129965]
V79	IC₅₀	15 nM Compound: MTP	Inhibition of human CYP11B1 expressed in hamster V79 MZ cells using [3H] 11 deoxycorticosterone as substrate by HPLC radioflow detector Inhibition of human CYP11B1 expressed in hamster V79 MZ cells using [3H] 11 deoxycorticosterone as substrate by HPLC radioflow detector	[PMID: 24900349]
V79	IC₅₀	72 nM Compound: 2	Inhibition of human aldosterone synthase expressed in chinese hamster V79 cells using 11-deoxycorticosterone as substrate Inhibition of human aldosterone synthase expressed in chinese hamster V79 cells using 11-deoxycorticosterone as substrate	[PMID: 21129965]
V79	IC₅₀	72 nM Compound: MTP	Inhibition of human CYP11B2 expressed in hamster V79 MZ cells using [3H] 11 deoxycorticosterone as substrate by HPLC radioflow detector Inhibition of human CYP11B2 expressed in hamster V79 MZ cells using [3H] 11 deoxycorticosterone as substrate by HPLC radioflow detector	[PMID: 24900349]

In Vitro

Metyrapone (100?μM; 2 h) hyperactivates autophagy in HepG2, and delays the activation of apoptosis at severe endoplasmic reticulum (ER) stress^[5].

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

In Vivo

Metyrapone (25 or 50 mg/kg; SC, single dosage) decreases the stress-induced increase in plasma corticosterone levels, significantly impairs acquisition performance at high dosage, and increases open arm activity at low dosage^[1].

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

Animal Model:

Male Sprague-Dawley rats (n=179; 270-300g)^[1]
Dosage:

25 or 50 mg/kg (in a volume of 2.0 mL/kg)
Administration:

SC, single dosage
Result:

Dose-dependently decreased the stress-induced increase in plasma corticosterone levels in the water maze test; the high level dose significantly impaired acquisition performance in the water maze and decreased fear-induced immobility; the lower dose increased open arm activity.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 54-36-4
Appearance Solid
Molecular Weight 226.27
Formula C₁₄H₁₄N₂O
Color White to yellow
SMILES

CC(C1=CC=CN=C1)(C)C(C2=CC=CN=C2)=O
Synonyms

Su-4885
Structure Classification
- Alkaloids
- Pyridine Alkaloids
Initial Source
- Endogenous metabolite
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (11)

All Bio/Physico-chemical AssayWBIn Vivo Efficacy StudyHistological Imaging/Staining

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Journal Impact Factor

Immunity

Small-molecule CBP/p300 histone acetyltransferase inhibition mobilizes leukocytes from the bone marrow via the endocrine stress response. [Abstract]

2024 Feb 13;57(2):364-378.e9. PMID: 38301651
Nat Commun

A neural circuit for sex-dependent conditioned pain hypersensitivity in mice. [Abstract]

2025 Apr 17;16(1):3639. PMID: 40240334

Metyrapone purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Apr 17;16(1):3639. [Abstract]

Summarized data for corticosterone and free-testosterone levels (n = 5; corticosterone, p = 0.0329; free-testosterone, p = 0.0042). The results showed that Metyrapone (5 mg/kg; i.h.; single dose) significantly reduced serum corticosterone and free testosterone levels in mice.

Metyrapone purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Apr 17;16(1):3639. [Abstract]

PWT and PWL of male^SC mice (n = 5; PWT: F_1,8 = 6.027, p = 0.0396; PWL: F_1,8 = 2.817, p = 0.1318). Metyrapone (5 mg/kg; i.h.; single dose) reversed conditioned contextual pain hypersensitivity in male^SC mice.

Metyrapone purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Apr 17;16(1):3639. [Abstract]

Raster plots with typical traces and quantitative data for spontaneous firing rates of Glu^mPOA neurons in male^SC mice (n = 24 units for D0-saline group and n = 22 units for other groups from 4 mice; F_1,44 = 14.85, p = 0.0004). Metyrapone (5 mg/kg; i.h.; single dose) reversed the hyperactivity of Glu^mPOA neurons in male^SC mice.
Nat Commun

A brain-to-liver signal mediates the inhibition of liver regeneration under chronic stress in mice. [Abstract]

2024 Nov 28;15(1):10361. PMID: 39609433
Adv Sci (Weinh)

Chronic Psychological Stress Induces Cardiomyocyte Hypertrophy Through Corticosterone-Glucocorticoid Receptor-LAMA5 Axis. [Abstract]

2025 Jul 11:e14659. PMID: 40642838

Metyrapone purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jul 11:e14659. [Abstract]

Representative Western blot images of pPI3K, PI3K, pAKT, AKT, and ITGB1 in heart tissue of each group of rats. Metyrapone (25 mg/kg; every 2 days for 12 weeks), relacorilant, and knockdown of LAMA5 partially inhibited the activation of the PI3K/AKT pathway.

Metyrapone purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jul 11:e14659. [Abstract]

Representative images and quantitative analysis of WGA staining in cardiac myocytes of each group of rats (n=4). WGA staining results showed that the surface area of cardiomyocytes in the hearts of rats in the CMS group was significantly increased compared to the control group, and Metyrapone (25 mg/kg; every 2 days for 12 weeks)/relacorilant/LAMA5KD could reverse the cardiomyocyte enlargement induced by CMS.
Proc Natl Acad Sci U S A

Androgen receptors in corticotropin-releasing hormone neurons mediate the sexual dimorphism in restraint-induced thymic atrophy. [Abstract]

2025 Mar 25;122(12):e2426107122. PMID: 40106355
Free Radic Biol Med

Chronic intermittent cold stress-induced lipophagy promotes foamy macrophage susceptibility to ferroptosis and exacerbates atherosclerosis. [Abstract]

2026 Jan:242:636-653. PMID: 41205774
Brain Behav Immun

Corticosterone-mediated microglia activation affects dendritic spine plasticity and motor learning functions in minimal hepatic encephalopathy. [Abstract]

2019 Nov:82:178-187. PMID: 31437533
iScience

Stimulation of TRPV1+ peripheral somatosensory nerves suppress inflammation via the somato-autonomic reflex. [Abstract]

2025 Jan 17;28(2):111831. PMID: 39967868
J Neuroendocrinol

Glucocorticoid regulation of diurnal spine plasticity in the murine ventromedial prefrontal cortex. [Abstract]

2022 Dec;34(12):e13212. PMID: 36426781
J Pharm Biomed Anal

LC-MS/MS method for simultaneous quantification of osilodrostat and metyrapone in human plasma from patients treated for Cushing's Syndrome. [Abstract]

2023 May 10:228:115316. PMID: 36868030
Biochem Biophys Res Commun

Myo-inositol enhances the low-salinity tolerance of turbot (Scophthalmus maximus) by modulating cortisol synthesis. [Abstract]

2020 Jun 11;526(4):913-919. PMID: 32279992

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (441.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : ≥ 38 mg/mL (167.94 mM)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.4195 mL

22.0975 mL

44.1950 mL

5 mM

0.8839 mL

4.4195 mL

8.8390 mL

10 mM

0.4419 mL

2.2097 mL

4.4195 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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: ≥ 2.5 mg/mL (11.05 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (11.05 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (11.05 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: PBS

Solubility: 100 mg/mL (441.95 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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) .

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Roozendaal B, et al. Dose-dependent suppression of adrenocortical activity with metyrapone: effects on emotion and memory. Psychoneuroendocrinology. 1996 Nov;21(8):681-93. [Content Brief]

[2]. Jahn H, et al. Metyrapone as additive treatment in major depression: a double-blind and placebo-controlled trial. Arch Gen Psychiatry. 2004 Dec;61(12):1235-44. [Content Brief]

[3]. Daniel E, et al. Effectiveness of Metyrapone in Treating Cushing's Syndrome: A Retrospective Multicenter Study in 195 Patients. J Clin Endocrinol Metab. 2015 Nov;100(11):4146-54. [Content Brief]

[4]. Peterson JA, Ullrich V, Hildebrandt AG. Methyrapone interaction with Pseudomonas putida cytochrome P-405. Arch Biochem Biophys. 1971 Aug;145(2):531-42. [Content Brief]

[5]. Holczer M, et al. A Comprehensive Systems Biological Study of Autophagy-Apoptosis Crosstalk during Endoplasmic Reticulum Stress. Biomed Res Int. 2015;2015:319589. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	4.4195 mL	22.0975 mL	44.1950 mL	110.4875 mL
	5 mM	0.8839 mL	4.4195 mL	8.8390 mL	22.0975 mL
	10 mM	0.4419 mL	2.2097 mL	4.4195 mL	11.0487 mL
	15 mM	0.2946 mL	1.4732 mL	2.9463 mL	7.3658 mL
	20 mM	0.2210 mL	1.1049 mL	2.2097 mL	5.5244 mL
	25 mM	0.1768 mL	0.8839 mL	1.7678 mL	4.4195 mL
	30 mM	0.1473 mL	0.7366 mL	1.4732 mL	3.6829 mL
	40 mM	0.1105 mL	0.5524 mL	1.1049 mL	2.7622 mL
	50 mM	0.0884 mL	0.4419 mL	0.8839 mL	2.2097 mL
	60 mM	0.0737 mL	0.3683 mL	0.7366 mL	1.8415 mL
	80 mM	0.0552 mL	0.2762 mL	0.5524 mL	1.3811 mL
	100 mM	0.0442 mL	0.2210 mL	0.4419 mL	1.1049 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Metyrapone

Anti-Infection Compound Library

Metabolism/Protease Compound Library

FDA-Approved Drug Library

Autophagy Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Antioxidant Compound Library

Oxygen Sensing Compound Library

Anti-COVID-19 Compound Library

Endoplasmic Reticulum Stress Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Alkaloids Library

Mitochondria-Targeted Compound Library

Rare Diseases Drug Library

Human Metabolite Library

Heterocyclic Compound Library

Off-patent Drug Library

Metabolic Enzyme Compound Library

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MCE Bioactive Compound Library

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Bioactive Compound Library

RO5 Drug-like Natural Product Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Chinese Baijiu Compound Library

Natural Product Diversity Scaffold Library

Publications Citing Use of MedChemExpress (MCE) Metyrapone

All Endogenous Metabolite Isoforms

All Cytochrome P450 Isoforms

Biological Activity

Chemical Information

Publications (11)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Metyrapone Related Classifications

Cat. No.: HY-B1232