Cyproterone Acetate - Moligand™, 10mM in DMSO , Progesterone receptor agonist, CAS No.427-51-0, Progesterone receptor agonist

CAS: 427-51-0 Cat. No.: C408807 Molecular Weight: 416.94 EC Number: 207-048-3

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

(1β,​2β)​-17-​(acetyloxy)​-​6-​chloro-​1,​2-​dihydro-​3'H-​cyclopropa[1,​2]​pregna-​1,​4,​6-​triene-​3,​20-​dione

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Cyproterone Acetate 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.
In vitro

Cyproterone acetate clearly shows antagonistic properties, while being a partial agonist also, showing agonism for the AR, with EC50 of 4.0 μM, at relatively high concentrations. 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.

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. 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. Cyproterone acetate treatment plus artificial long days in autumn has a negative effect on sperm motility and sperm morphology. Androgen receptor occupation by Cyproterone acetate preferentially reduces the levels of spermatidal protamine in testis and spermatozoa involved in nuclear chromatin condensation.
Cell Data

cell lines：Human colon carcinoma cell line WM480

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonyms

(1β, ​2β)​-17-​(acetyloxy)​-​6-​chloro-​1, ​2-​dihydro-​3'H-​cyclopropa[1, ​2]​pregna-​1, ​4, ​6-​triene-​3, ​20-​dione

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

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.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

ANTAGONIST

Mechanism of action

Progesterone receptor agonist

Product Properties

• ALogP: 3.6

Names and Identifiers

• Isomeric SMILES: CC(=O)[C@]1(CC[C@@H]2[C@@]1(CC[C@H]3[C@H]2C=C(C4=CC(=O)[C@@H]5C[C@@H]5[C@]34C)Cl)C)OC(=O)C
• Molecular Weight: 416.94
• Reaxy-Rn: 24731968
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=24731968&ln=

Associated Targets(Human)

AR Tclin Androgen receptor (3 Activities)

Discover Target: AR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Specific Rotation[α]: 152° (C=1,CHCl3)
• Melt Point(°C): 209 °C