醋酸环丙孕酮, 孕酮受体激动剂

Androgen Receptor Antagonists
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货号 (SKU) 包装规格 是否现货 价格 数量
C408807-1ml
1ml 现货 Stock Image
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Compound libraries (12332)

基本描述

英文别名 (1β,​2β)​-17-​(acetyloxy)​-​6-​chloro-​1,​2-​dihydro-​3'H-​cyclopropa[1,​2]​pregna-​1,​4,​6-​triene-​3,​20-​dione
规格或纯度 Moligand™, 10mM in DMSO
英文名称 Cyproterone Acetate
生化机理 醋酸环丙孕酮是一种雄激素受体(AR)拮抗剂,IC50 为 7.1 nM,也是一种弱孕酮受体激动剂,具有弱促妊娠活性和糖皮质激素活性。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 拮抗剂
作用机制 孕酮受体激动剂
产品介绍

Cyproterone Acetate是雄激素受体拮抗剂,IC50为7.1 nM,也是微弱的孕激素受体激动剂,具有微弱的孕激素和糖皮质激素活性。

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%

产品属性

ALogP 3.314
hba_count 4
Rotatable Bond 3

关联靶点(人)

AR Tclin 雄激素受体(Androgen receptor) (3 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

分子类型 小分子
Canonical SMILES CC(=O)OC1(CCC2C3C=C(Cl)C4=CC(=O)C5CC5C4(C)C3CCC12C)C(C)=O
分子量 416.94
Reaxy-Rn 24731968
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=24731968&ln=

化学和物理性质

DMSO(mg / mL) Max Solubility 83
DMSO(mM) Max Solubility 199.07
Water(mg / mL) Max Solubility <1

安全和危险性(GHS)

Reaxy-Rn 24731968
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=24731968&ln=

技术规格说明书

Concentration(Compounding value) 9-11(mmol/L)
Record the entire process by video Conform

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

溶液计算器

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