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

CAS: 427-51-0 Cat. No.: C408807 Fórmula: C₂₄H₂₉ClO₄ Peso molecular: 416.94 Número CE: 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

Visão geral

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

Sinónimos

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

Especificações e pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos e fisiológicos

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.

Condições de armazenamento de armazenamento

Store at -80°C

Enviado em

Dry ice packs + Cold packs

Este produto requer transporte de cadeia fria. Serviços terrestres e outros serviços econômicos não estão disponíveis.

Grau

Moligand™

Tipo de ação

ANTAGONIST

Mecanismo de ação

Progesterone receptor agonist

Propriedades do produto

• ALogP: 3.6

Nomes e identificadores

• SMILES isoméricas: 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
• Peso molecular: 416.94
• Reaxy-Rn: 24731968
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=24731968&ln=

Alvos associados (humanos)

AR Tclin Androgen receptor (3 Activities)

Discover Target: AR

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

Propriedades químicas e físicas

• Rotação específica [α]: 152° (C=1,CHCl3)
• Ponto de fusão (°C): 209 °C