Cyproterone Acetate

ArtNr	S2042-100
Hersteller	Selleckchem
CAS-Nr.	427-51-0
Menge	100 mg
Quantity options	100 mg 10 mM/1 mL 250 mg
Kategorie	Oncology Food Safety Hormones Inhibitors & Compound Libraries Small Molecules By Organ Testicular & Prostate Cancer
Typ	Inhibitors
Specific against	other
Smiles	CC(=O)C1(CCC2C1(CCC3C2C=C(C4=CC(=O)C5CC5C34C)Cl)C)OC(=O)C
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	427-51-0'
Similar products	Cyproterone
Lieferbar
Manufacturer - Targets	AR
Storage Conditions	2 years -80 in solvent
Molecular Weight	416, 94
Administration	Administered via s.c.
Animal Models	Castrate male SD rat
Clinical Trials	Cyproterone acetate has entered in a phase III clinical trial in the treatment of anxiety disorder, prostate cancer, sexual dysfunction, urinary complications and long-term effects secondary to cancer therapy in adults.
Dosages	0.2 mg /kg/day
Formulation	Ethanol
IC50	7.1 nM [1], 7.1 nM [1], 7.1 nM [1], 7.1 nM [1], 7.1 nM [1], 7.1 nM [1]
In vitro	Cyproterone acetate clearly shows antagonistic properties, while being a partial agonist also, showing agonism for the AR, with EC50 of 4.0 uM, at relatively high concentrations. [1] In the presence of 10 nM Testosterone, low concentrations of Cyproterone acetate inhibits T-stimulated transcription of 3XHRE-LUC, but at higher concentrations, transcription is stimulated. [2]
In vivo	LH levels in Cyproterone acetate-treated rats do not dip below pretreatment levels, although they does not increase as much in the rats treated with 3.2 mg Cyproterone acetate/kg/day as in those which received 0.2 mg Cyproterone acetate/kg/day. [2] Cyproterone acetate exhibits direct negative effect on reproductive organs weight and significant reducing effect on sperm count and Ca2+ contents. SOD and GST activities significantly decrease in addition to significant increase in NO, MDA contents reflecting the oxidative status of testis in Cyproterone acetate treated rats. [3] Cyproterone acetate treatment plus artificial long days in autumn has a negative effect on sperm motility and sperm morphology. [4] Androgen receptor occupation by Cyproterone acetate preferentially reduces the levels of spermatidal protamine in testis and spermatozoa involved in nuclear chromatin condensation. [5]
Kinase Assay	AR and ERalpha CALUX bioassays, U2-OS cells are transfected with 3 HRE-TATA-Luc and pSG5-neo-hAR, using calcium phosphate precipitation to generate AR CALUX cells. AR and ERalpha CALUX cells are plated in 96-well plates (6000 cells/well) with phenol red-free DF medium supplemented with 5% dextran-coated charcoal-stripped FCS (DCC-FCS) at a volume of 200 uL per well. Two days later, the medium is refreshed, and cells are incubated with human or fetal serum (0â€“10% [v/v]) or Cyproterone acetate (dissolved in ethanol or DMSO) in triplicate at a 1:1000 dilution. In case of serum incubation, final serum concentration is 10% (v/v), and lower percentages of the tested sera are supplemented with DCC-FCS. After 24 hours the medium is removed, cells are lysed in 30 uL Triton-lysis buffer and measured for luciferase activity using a luminometer for 0.1 min/well.
Solubility (25C)	DMSO >=83 mg/mL, Water <1 mg/mL, Ethanol >=10 mg/mL
Information	Cyproterone acetate is an androgen receptor (AR) antagonist with IC50 of 7.1 nM, as well as a weak progesterone receptor agonist with weak pro-gestational and glucocorticoid activity.

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