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.
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- CAS. Nr.: 33765-68-3
- Formel: C20H30O2
- Molecular Weight:302.46
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
In Vitro
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.
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. Nr. 33765-68-3
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Molecular Weight 302.46
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Formel 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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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.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Oxendolone Related Classifications
HY-106391 Related Classifications
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