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Metyrapone P450 (e.g. CYP17) inhibitor

Cat.No.S5416

Metyrapone (NSC-25265, SU-4885) is an inhibitor of the enzyme steroid 11-beta-monooxygenase (CYP11B1) that inhibits adrenal steroid synthesis.
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Quality Control

Batch: Purity: 99.97%
99.97

Solubility

In vitro
Batch:

DMSO : 46 mg/mL (203.29 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 226.27 Formula

C14H14N2O

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 54-36-4 -- Storage of Stock Solutions

Synonyms NSC-25265, SU-4885 SMILES CC(C)(C1=CN=CC=C1)C(=O)C2=CN=CC=C2

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
11β-HSD1
30 μM(Ki)
In vitro
Metyrapone is a well known inhibitor of 11β-hydroxylase, a key enzyme involved in the final step of cortisol biosynthesis. At higher concentrations, it also inhibits other steroidogenic enzymes such as cholesterol side chain cleavage enzyme. It is specific for 11β-HSD1 while it has little effect on 11β-HSD2 activity.
In vivo
The administration of metyrapone to man, and animals such as the dog and sheep thus leads to a decrease in circulating levels of cortisol.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-06-29)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07138274 NOT_YET_RECRUITING
Mild Autonomous Cortisol Secretion (MACS); Autonomous Cortisol Secretion (ACS)
Mayo Clinic
2026-08 PHASE2
NCT07494084 NOT_YET_RECRUITING
Shift Work Schedule; Circadian Rhythm; Insulin Resistance; Circadian Misalignment
Washington State University
2026-07-01 PHASE4
NCT06106295 ACTIVE_NOT_RECRUITING
Autonomous Cortisol Secretion; Mild Autonomous Cortisol Secretion (MACS)
Mayo Clinic
2023-12-19 PHASE2
NCT07268222 RECRUITING
Mild Autonomous Cortisol Secretion (MACS)
Laikο General Hospital, Athens
2025-12-01 PHASE4
NCT06556277 COMPLETED
Glucocorticoids; Overweight and Obesity; Overeating
Eleonora Seelig
2024-09-01
NCT06801249 RECRUITING
Adrenal Incidentalomas; Cushing Syndrome
IRCCS Azienda Ospedaliero-Universitaria di Bologna
2021-02-23 PHASE4

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