Plomestane
Plomestane is an orally active second-generation steroidal aromatase inhibitor that, as an enzyme-activated pseudosubstrate, is converted via NADPH-dependent catalysis into a reactive intermediate, which covalently binds to aromatase to produce irreversible inhibition, thereby persistently suppressing peripheral aromatase activity. Plomestane can be used for the study of hormone-dependent breast cancer.
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- CAS No.: 77016-85-4
- Formule: C21H26O2
- Masse moléculaire:310.44
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
In Vitro
Plomestane (5 nM; up to 40 min preincubation) is a high-affinity, irreversible, active-site-directed mechanism-based inactivator of human placental aromatase, with a Ki (inact.) of 3.2 nM[2].
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.
Chemical Information
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CAS No. 77016-85-4
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Masse moléculaire 310.44
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Formule C21H26O2
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SMILES
C(C#C)[C@@]12[C@@]3([C@]([C@]4([C@](C)(CC3)C(=O)CC4)[H])(CCC1=CC(=O)CC2)[H])[H]
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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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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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)