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

CAS: 427-51-0 Cat. No.: C408807 Formule: C₂₄H₂₉ClO₄ Poids moléculaire: 416.94 Numéro 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

Vue d’ensemble

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

Synonymes

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

Spécifications et pureté

Moligand™, 10mM in DMSO

Mécanismes biochimiques et physiologiques

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.

Conditions de stockage de stockage

Store at -80°C

Expédié en

Dry ice packs + Cold packs

Ce produit nécessite l'expédition en chaîne froide. Les services terrestres et autres services économiques ne sont pas disponibles.

Grade

Moligand™

Type d'action

ANTAGONIST

Mécanisme d'action

Progesterone receptor agonist

Propriétés du produit

• ALogP: 3.6

Noms et identifiants

• Isomères 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
• Poids moléculaire: 416.94
• Reaxy-Rn: 24731968
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=24731968&ln=

Cibles associées (humaines)

AR Tclin Androgen receptor (3 Activities)

Discover Target: AR

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

Propriétés chimiques et physiques

• Rotation spécifique [α]: 152° (C=1,CHCl3)
• Point de fusion (°C): 209 °C