Metyrapone (Synonyms: Su-4885)

Name: Metyrapone
Brand: MedChemExpress
SKU: HY-B1232
Rating: 5.0 (11 reviews)

Cat. No.: HY-B1232 Purity: 99.70%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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.

CAS No. : 54-36-4

Size	Stock	Quantity
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
100 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
1 g	Get quote
5 g	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of Metyrapone:

Metyrapone Tartrate Get quote
Metyrapone (Standard) Get quote

11 Publications Citing Use of MCE Metyrapone

Bio/Physico-chemical Assay

In Vivo Efficacy Study

Histological Imaging/Staining

: 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.

: 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.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Endogenous Metabolite Isoform Specific Products:

View All Isoforms

Human Endogenous Metabolite Microbial Metabolite

View All Cytochrome P450 Isoform Specific Products:

View All Isoforms

CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

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

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

Molecular Weight

226.27

Formula

C₁₄H₁₄N₂O

CAS No.

54-36-4

Appearance

Solid

Color

White to yellow

SMILES

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

Structure Classification

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

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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
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)

Volume _(start)

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: ≥ 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.
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: ≥ 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.
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: ≥ 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.

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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Calculation results:

Working solution concentration: 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

Purity: 99.83%

Select Batch:

Data Sheet (279 KB) SDS (396 KB)

COA (248 KB) LCMS (94 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]

Complete Stock Solution Preparation Table

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.

Metyrapone Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Your Recently Viewed Products:

Product Name

Requested Quantity *

Applicant Name *

Salutation

Email Address *

Phone Number *

Department

Organization Name *

City

State

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

Metyrapone (Synonyms: Su-4885)

Customer Review

Other Forms of Metyrapone:

Metyrapone Related Antibodies

11 Publications Citing Use of MCE Metyrapone

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Endogenous Metabolite Isoform Specific Products:

View All Cytochrome P450 Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Metyrapone Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Metyrapone Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report