Oxendolone
Oxendolone (TSAA-291) is a steroidal antiandrogen with partial agonist properties, exhibiting a Ki value of 1.4 nM for the androgen receptor. Oxendolone exerts tissue-specific androgen receptor activity, induces unique androgen receptor conformational changes, and drives differential cofactor recruitment. Oxendolone is recruited to the androgen receptor in a PIAS1-dependent manner. Oxendolone increases levator ani muscle weight in castrated mice. Oxendolone can be used for research on benign prostatic hyperplasia.
For research use only. We do not sell to patients.
- CAS No.: 33765-68-3
- Formula: C20H30O2
- Molecular Weight:302.46
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
Oxendolone (4 h) acts as a partial androgen receptor agonist in COS-7 cells, with activity reaching approximately 50% of the maximal activity of 1 μM dihydrotestosterone (DHT); in the presence of 0.1 μM DHT, it acts as an antagonist[1].
Oxendolone (0.1 pM-1 μM; 24 h) exhibits tissue-selective androgen receptor agonist activity, with higher relative potency in human skeletal muscle (SkMC) cells (reaching 87.6% of 100 nM DHT activity at 100 nM), whereas in human prostate epithelial (PrEC) cells it is only 47.5% of 100 nM DHT activity (at 100 nM)[1].
Oxendolone (24 h) induces a unique androgen receptor cofactor recruitment profile in 293T cells, recruiting 12 cofactors (including PIAS1) in a manner distinct from DHT, while recruiting 43 cofactors in a ligand-independent manner that is completely consistent with DHT[1].
Oxendolone (100 nM; 24 h) enhances its androgen receptor transcriptional activity in 293T cells through forcibly expressed PIAS1[1].
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:Crj:ICR (male, 5 weeks old, castrated)[1]
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Dosage:3 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:s.c.; daily; 14 days
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Result:Increased levator ani muscle weight in a dose-dependent manner at 10 mg/kg and 30 mg/kg.
Increased levator ani muscle weight to 78% of that in intact animals at 30 mg/kg.
Showed no marked weight increase in the prostate or seminal vesicle at doses up to 30 mg/kg.
Chemical Information
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CAS No. 33765-68-3
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Molecular Weight 302.46
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Formula C20H30O2
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SMILES
C[C@@]12[C@]([C@]3([C@@]([C@@]4(C(CC3)=CC(=O)CC4)[H])(CC1)[H])[H])(C[C@H](CC)[C@@H]2O)[H]
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Synonyms
TSAA-291
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Oxendolone Related Classifications
HY-106391 Related Classifications
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