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Metyrapone P450 (e.g. CYP17) inhibitor

Name: Metyrapone
Brand: Selleck Chemicals
SKU: S5416
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S5416

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

Chemical Structure

Molecular Weight: 226.27

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Quality Control

Batch: Purity: 99.97%

99.97

Related Targets	Dehydrogenase HSP Transferase PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Drug Metabolite
Other P450 (e.g. CYP17) Inhibitors	Apigenin Baicalein Avasimibe Naringenin Diosmetin Sodium Danshensu Alizarin Naringin Benzbromarone Orteronel

Solubility

In vitro
Batch:

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

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.300mg/ml (10.16mM)	Taking the 1 mL working solution as an example, add 50 μL of 46 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.280mg/ml (1.24mM)	Taking the 1 mL working solution as an example, add 50 μL of 5.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

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	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	NSC-25265, SU-4885			Smiles	CC(C)(C1=CN=CC=C1)C(=O)C2=CN=CC=C2

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	[1] https://pubmed.ncbi.nlm.nih.gov/9393954/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03491696	Unknown status	Depressive Disorder\|Hormone Disturbance	Centre Hospitalier Rouffach\|University Hospital Strasbourg France	December 22 2018	Phase 4
NCT02406066	Completed	Cocaine Use Disorder\|Tobacco Use Disorder	Embera NeuroTherapeutics Inc.\|National Institute on Drug Abuse (NIDA)	March 2015	Phase 1

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