Metyrapone (Synonyms: NSC 25265, SU 4885) |
Catalog No.GC17411
One-Click Copy Product Info
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Metyrapone is a potent oral 11β-hydroxylase inhibitor and autophagy activator that also inhibits aldosterone production. It can be used in the study of depression, atherosclerosis and cancer.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 54-36-4
Sample solution is provided at 25 µL, 10mM.
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Metyrapone is a potent oral 11β-hydroxylase inhibitor and autophagy activator that also inhibits aldosterone production. It can be used in the study of depression, atherosclerosis and cancer[1,2].
Metyrapone (100μM; 2h) hyperactivates autophagy in HepG2, and delays the activation of apoptosis at severe endoplasmic reticulum (ER) stress[3]. In H295R cells, treatment with Metyrapone (20μM; 48h) for 48 hours significantly reduced cortisol levels, which were 25.2±4.3μg/L in untreated cells and decreased to 18.9±0.3μg/L after Metyrapone treatment[4].
Neuronal loss in the hippocampal CAl region was significantly reduced in the 4VO model in rats administered Metyrapone (200 mg/kg; sc; 30 min before ischaemia)[5]. There was significant impairment of ovarian and uterine development in the young female Metyrapone-treated (100mg/kg; ip; 30d) mice with the incidence of corpora lutea being reduced 82%. Seminal vesicle and body weights were significantly reduced in juvenile males[6]. Metyrapone (100mg/kg; ip; 4 weeks) treatment reduced the relative mRNA expression levels of phosphoenolpyruvate carboxykinase, a gluconeogenic GR target gene, in the liver and was associated with increased relative mRNA expression levels of the adrenal high-density lipoprotein receptor, SR-BI, and the steroidogenic enzymes, CYP11A1 and CYP11B[7].
References:
[1]. Roozendaall B, Bohus B, McGaugh J L. Dose-dependent suppression of adrenocortical activity with metyrapone: effects on emotion and memory[J]. Psychoneuroendocrinology, 1996, 21(8): 681-693.
[2]. Jahn H, Schick M, Kiefer F, et al. Metyrapone as additive treatment in major depression: a double-blind and placebo-controlled trial[J]. Archives of general psychiatry, 2004, 61(12): 1235-1244.
[3]. Holczer M, Márton M, Kurucz A, et al. A comprehensive systems biological study of autophagy‐apoptosis crosstalk during endoplasmic reticulum stress[J]. BioMed research international, 2015, 2015(1): 319589.
[4]. Germano A, Saba L, De Francia S, et al. CYP11B1 has no role in mitotane action and metabolism in adrenocortical carcinoma cells[J]. PloS one, 2018, 13(5): e0196931.
[5]. Lidhar N K, Darvish-Ghane S, Sivaselvachandran S, et al. Prelimbic cortex glucocorticoid receptors regulate the stress-mediated inhibition of pain contagion in male mice[J]. Neuropsychopharmacology, 2021, 46(6): 1183-1193.
[6]. Pasley J N, McKinney R D, Blue L R. Effects of metyrapone on reproductive organs of house mice[J]. Proceedings of the Society for Experimental Biology and Medicine, 1975, 148(2): 333-336.
[7]. van der Sluis R J, van den Aardweg T, Sijsenaar T J P, et al. Metyrapone Treatment Protects Low-Density Lipoprotein Receptor Knockout Mice against Hypercorticosteronemia Development without Changing Atherosclerosis Susceptibility[J]. Biomolecules, 2023, 13(9): 1287.
| Cell experiment [1]: | |
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Cell lines |
Normal human epidermal keratinocytes cells |
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Preparation Method |
H295R cells were seeded into 96-well plates in triplicates and treated with Metyrapone (20μM) used alone for 48h. |
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Reaction Conditions |
20μM; 48h |
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Applications |
In H295R cells, treatment with Metyrapone (20μM; 48h) for 48 hours significantly reduced cortisol levels, which were 25.2±4.3μg/L in untreated cells and decreased to 18.9±0.3μg/L after Metyrapone treatment. |
| Animal experiment [2]: | |
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Animal models |
four-vessel occlu sion (4VO) model |
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Preparation Method |
Male Wistar rats were used for the four-vessel occlu sion (4VO) model of transient global forebrain ischemia, Metyrapone was dissolved in sterile saline and injected subcutane ously in a volume of 1.5ml, (200mg/kg body wt). |
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Dosage form |
200mg/kg; sc; 30min before ischaemia |
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Applications |
In the 4VO model, neuronal loss in region CAl of the hippocampus was significantly reduced in rats administered Metyrapone. Seizure-induced damage to hippocampal pyramidal neurons was significantly reduced in rats administered Metyrapone. |
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References: |
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| Cas No. | 54-36-4 | SDF | |
| Synonyms | NSC 25265, SU 4885 | ||
| Chemical Name | 2-methyl-1,2-di(pyridin-3-yl)propan-1-one | ||
| Canonical SMILES | O=C(C1=CC=CN=C1)C(C)(C)C2=CC=CN=C2 | ||
| Formula | C14H14N2O | M.Wt | 226.27 |
| Solubility | ≥ 13.45mg/mL in Water | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.4195 mL | 22.0975 mL | 44.195 mL |
| 5 mM | 883.9 μL | 4.4195 mL | 8.839 mL |
| 10 mM | 441.9 μL | 2.2097 mL | 4.4195 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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.)
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 saline, 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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 29 reference(s) in Google Scholar.)