Metyrapone Tartrate
Based on 12 publication(s) in Google Scholar
Metyrapone (Su-4885) Tartrate is a potent and orally active 11β-hydroxylase inhibitor and an autophagy activator, also inhibits the production of aldosterone. Metyrapone Tartrate inhibits synthesis of endogenous adrenal corticosteroid, decreases glucocorticoid levels, and also affects behavior and emotion. In addition, Metyrapone Tartrate increases the efficiency of autophagic process via downregulation of mTOR pathway, and interacts with Pseudomonas putida cytochrome P-450. Metyrapone Tartrate can be used for researching Cushing's syndrome and depression.
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- CAS. Nr.: 908-35-0
- Formel: C22H26N2O13
- Molecular Weight:526.45
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Publications Citing Use of MedChemExpress (MCE) Metyrapone Tartrate
More- Immunity. 2024 Feb 13;57(2):364-378.e9. [Abstract]
- Nat Commun. 2025 Apr 17;16(1):3639. [Abstract]
- Nat Commun. 2024 Nov 28;15(1):10361. [Abstract]
- Adv Sci (Weinh). 2025 Jul 11:e14659. [Abstract]
- Proc Natl Acad Sci U S A. 2025 Mar 25;122(12):e2426107122. [Abstract]
- Antioxidants (Basel). 2026 Jun 26;15(7):800.
- Free Radic Biol Med. 2026 Jan:242:636-653. [Abstract]
- Brain Behav Immun. 2019 Nov:82:178-187. [Abstract]
- J Neuroendocrinol. 2022 Dec;34(12):e13212. [Abstract]
- iScience. 2025 Jan 17;28(2):111831. [Abstract]
- J Pharm Biomed Anal. 2023 May 10:228:115316. [Abstract]
- Biochem Biophys Res Commun. 2020 Jun 11;526(4):913-919. [Abstract]
Customer Validation & Images
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Bio/Physico-chemical Assay
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In Vivo Efficacy Study
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Bio/Physico-chemical Assay
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WB
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Histological Imaging/Staining
Biologische Aktivität
Beschreibung
IC50 & Target
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. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (n=179; 270-300g)[1]
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Dosage:25 or 50 mg/kg (in a volume of 2.0 ml/kg)
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Administration:SC, single dosage
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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.
Chemical Information
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CAS. Nr. 908-35-0
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Molecular Weight 526.45
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Formel C22H26N2O13
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SMILES
CC(C)(C(C1=CC=CN=C1)=O)C2=CC=CN=C2.O=C([C@@H]([C@H](C(O)=O)O)O)O.O=C([C@@H]([C@H](C(O)=O)O)O)O
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Synonyms
Su-4885 Tartrate
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Structure Classification
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Initial Source
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (12)
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Journal Impact Factor
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Most Recent
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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
2025 Apr 17;16(1):3639. PMID: 40240334
Metyrapone Tartrate 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 Tartrate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Apr 17;16(1):3639. [Abstract]
PWT and PWL of maleSC mice (n = 5; PWT: F1,8 = 6.027, p = 0.0396; PWL: F1,8 = 2.817, p = 0.1318). Metyrapone (5 mg/kg; i.h.; single dose) reversed conditioned contextual pain hypersensitivity in maleSC mice.
Metyrapone Tartrate 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 GlumPOA neurons in maleSC mice (n = 24 units for D0-saline group and n = 22 units for other groups from 4 mice; F1,44 = 14.85, p = 0.0004). Metyrapone (5 mg/kg; i.h.; single dose) reversed the hyperactivity of GlumPOA neurons in maleSC mice.
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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 Tartrate 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 Tartrate 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.
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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 -
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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 -
J Neuroendocrinol
Glucocorticoid regulation of diurnal spine plasticity in the murine ventromedial prefrontal cortex. [Abstract]2022 Dec;34(12):e13212. PMID: 36426781 -
iScience
Stimulation of TRPV1+ peripheral somatosensory nerves suppress inflammation via the somato-autonomic reflex. [Abstract]2025 Jan 17;28(2):111831. PMID: 39967868 -
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
Protokoll
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
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Autophagy
Autophagy is a process in which eukaryotic cells use lysosomes to degrade their own cytoplasmic proteins and damaged organelles under the regulation of autophagy related gene (Atg). Microtubule-associated proteins light chain 3 (LC3) is recognized as autophagy marker, which transfers from cytoplasmic LC3 (LC3-I) to membrane type (LC3-II). LC3-II/I ratio could be detected by Western Blot and fluorescence microscopy.
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Lysosome and acidic-vesicle live-cell staining
Lysosome and acidic-vesicle live-cell staining detects acidic intracellular compartments by using membrane-permeant acidotropic probes that accumulate in low-pH vesicles, including lysosomes, late endosomes, autolysosomes, and acidic phagosomes. LysoTracker staining is commonly used as an intensity-based readout of acidic lysosomal compartment abundance or enlargement, while acridine orange produces green fluorescence in less concentrated compartments and red fluorescence after concentration-dependent accumulation in acidic vesicular organelles. Loss or reduction of acridine-orange red signal can be used as a readout of lysosomal membrane permeabilization or reduced acidic-vesicle integrity. This protocol is designed for live cultured cells and can be adapted for fluorescence microscopy, high-content imaging, plate-reader readout, or flow cytometry when the selected literature supports the readout. Because these dyes report acidotropic accumulation rather than lysosome identity alone,
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Macroautophagy Solutions
Macroautophagy is a conserved lysosome-dependent degradation pathway in which cytoplasmic material is sequestered into double-membrane autophagosomes and delivered to lysosomes for degradation and recycling. The pathway supports cellular homeostasis during nutrient limitation, organelle stress, protein-aggregate accumulation, infection, differentiation, and tissue remodeling by coupling cargo sequestration, autophagosome maturation, lysosomal fusion, and degradation of cargo-derived macromolecules. The core molecular sequence includes initiation by nutrient- and stress-regulated autophagy machinery, autophagosome nucleation, LC3/ATG8-family conjugation to autophagosomal membranes, cargo selection through receptors such as SQSTM1/p62, autophagosome-lysosome fusion, and lysosomal degradation. LC3 was identified as a mammalian homolog of yeast Atg8 that localizes to autophagosomal membranes after processing, and p62/SQSTM1 was shown to connect ubiquitinated cargo with autophagic degradati
Reinheit & Dokumentation
Verweise
[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]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Metyrapone Tartrate Related Classifications
HY-B1232A Related Classifications
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