155180-53-3
Chemical Structure
RU 59063
- CAS 番号: 155180-53-3
- Formula:C17H18F3N3O2S
- Molecular Weight:385.40
IUPAC Name: 4-(3-(4-hydroxybutyl)-4,4-dimethyl-5-oxo-2-thioxoimidazolidin-1-yl)-2-(trifluoromethyl)benzonitrile
InChIKey: FIDNKDVRTLFETI-UHFFFAOYSA-N
SMILES: N#CC1=CC=C(C=C1C(F)(F)F)N(C2=O)C(N(C2(C)C)CCCCO)=S
Biological Activity: RU 59063 is a high-affinity, selective nonsteroidal androgen receptor (AR) ligand that acts as a partial AR agonist/antagonist in CV-1 cell transcription assays. RU 59063 has a Ka value of 6.2×109 M-1 for human AR. RU 59063 induces a conformation of AR that can bind to the androgen response element (ARE), triggers partial AR-dependent transcriptional activation, and antagonizes testosterone-induced AR transcriptional activity. RU 59063 inhibits testosterone propionate-induced ornithine decarboxylase activity in mouse kidneys and testosterone propionate-induced prostate weight gain in rats. RU 59063 can be used in studies related to prostate cancer[1][2][3].
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RU 59063 | 98.61% | RU 59063 is a high-affinity, selective nonsteroidal androgen receptor (AR) ligand that acts as a partial AR agonist/antagonist in CV-1 cell transcription assays. RU 59063 has a Ka value of 6.2×109 M-1 for human AR. RU 59063 induces a conformation of AR that can bind to the androgen response element (ARE), triggers partial AR-dependent transcriptional activation, and antagonizes testosterone-induced AR transcriptional activity. RU 59063 inhibits testosterone propionate-induced ornithine decarboxylase activity in mouse kidneys and testosterone propionate-induced prostate weight gain in rats. RU 59063 can be used in studies related to prostate cancer. | ||||||||||||||||||||
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- [1]. Karvonen U, et al. Interaction of Androgen Receptors with Androgen Response Element in Intact Cells: Roles of Amino- and Carboxyl-terminal Regions and the Ligand. J Biol Chem. 1997;272(25):15973-15979.
- [2]. Teutsch G, et al. Non-steroidal antiandrogens: synthesis and biological profile of high-affinity ligands for the androgen receptor. The Journal of steroid biochemistry and molecular biology. 1994 Jan;48(1):111-9. [Content Brief]
- [3]. Gim HJ, et al. Conformational dynamics of androgen receptors bound to agonists and antagonists. Scientific reports. 2021 Aug 05;11(1):15887. [Content Brief]
Keywords
