Aminoglutethimide phosphate
Aminoglutethimide phosphate (DL-Aminoglutethimide phosphate) is an orally active anticonvulsant with various endocrine-related side effects. Aminoglutethimide phosphate blocks multiple steroid hormone synthesis pathways by inhibiting several cytochrome P-450-dependent hydroxylases, such as aromatase, cholesterol side-chain cleavage enzyme, 11-hydroxylase, and 18-hydroxylase, with IC50 values of 0.3, 3.5, 120, and 20 μM, respectively. Aminoglutethimide phosphate reduces cortisol levels. Aminoglutethimide phosphate can be used in research on Cushing's syndrome, breast cancer, and other conditions.
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- CAS No.: 23734-88-5
- Formule: C13H19N2O6P
- Masse moléculaire:330.27
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
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Aromatase |
In Vitro
Aminoglutethimide phosphate inhibits human placental microsomal aromatase by targeting cytochrome P-450, preventing the oxygen-dependent conversion of androgens to estrogens[1].
Aminoglutethimide (0.05 mM; duration sufficient to produce complete steroidogenesis inhibition) phosphate completely inhibits steroidogenesis in monolayer cultures of functional adrenal tumour cells by directly targeting steroidogenic enzymes, without altering ACTH-induced cell morphology or glucose consumption[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
Aminoglutethimide (8 days) phosphate exhibits goitrogenic activity and interferes with thyroid metabolism in intact rats on a low iodine diet, as evidenced by increased thyroid weight and reduced radio-iodine uptake[4].
Aminoglutethimide phosphate induces thyromegaly, reduces thyroxine and di-iodotyrosine production, and increases thyroidal inorganic iodide levels in Rattus norvegicus[4].
Aminoglutethimide phosphate inhibits adrenal steroid biosynthesis in rats and puppies, inducing adrenal hypertrophy, decreased corticosterone production, increased plasma ACTH, and characteristic cortical histological changes[4].
Aminoglutethimide phosphate induces ovarian enlargement in intact rats and potential uterine enlargement in hypophysectomized rats[4].
Aminoglutethimide (large doses) phosphate disrupts ovarian function, halts oestrous cycles, induces sterility, and reduces oestrogen-related uterine weight in intact female rats[4].
Aminoglutethimide (10 mg/kg; i.v.) phosphate is active to inhibit cortisol secretion and block the steroidogenic response to ACTH in dogs[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Crlj:CD1(ICR) (male, 7 weeks old)[3]
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Dosage:125 mg/kg/day; 250 mg/kg/day; 500 mg/kg/day
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Administration:p.o.; once daily; 5 days
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Result:Induced cytoplasmic vacuolation in adrenal zona fasciculata cells at 125-500 mg/kg/day, with vacuole membranes staining positive for adipophilin and LAMP-2, increased LAMP-2-positive granules, and Sudan black-positive vacuole contents.
Observed single cell necrosis in zona fasciculata cells at 250-500 mg/kg/day.
Caused 3 of 4 mice to become moribund and require euthanasia on Day 3 at 500 mg/kg/day.
Revealed enlarged lipid droplets, increased primary lysosomes, mitochondrial vacuolation, and enlarged lysosomes containing damaged mitochondria and lamellar bodies in zona fasciculata cells across all doses via electron microscopy.
Chemical Information
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CAS No. 23734-88-5
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Masse moléculaire 330.27
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Formule C13H19N2O6P
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SMILES
O=C1NC(C(CC)(CC1)C2=CC=C(C=C2)N)=O.O=P(O)(O)O
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Synonyms
DL-Aminoglutethimide phosphate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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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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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
Pureté et documentation
Références
[1]. Santen RJ, et al. Aminoglutethimide: review of pharmacology and clinical use. Pharmacotherapy. 1981;1(2):95-120. [Content Brief]
[2]. Cocconi G, et al. First generation aromatase inhibitors--aminoglutethimide and testololactone. Breast Cancer Res Treat. 1994;30(1):57-80. [Content Brief]
[3]. Mutsuga M, et al. Aminoglutethimide-induced lysosomal changes in adrenal gland in mice. Exp Toxicol Pathol. 2017;69(7):424-429. [Content Brief]
[4]. Hughss SW, et al. Aminoglutethimide: a "side-effect" turned to therapeutic advantage. Postgrad Med J. 1970;46(537):409-416. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Aminoglutethimide phosphate Related Classifications
HY-115425 Related Classifications
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