4,4',4''-(4-丙基-1H-吡唑-1,3,5-三基)三苯酚

用途

Propyl pyrazole triol (PPT) 是一种雌激素受体 α (ERσ) 激动剂。Propyl pyrazole triol (PPT) 对 ERα 的相对结合亲和力 (ERα: 49%) 是雌激素受体 β (ERβ: 0.12%) 的 410 倍。

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名称

[ CAS 号 ]:
263717-53-9

[ 中文名 ]:
4,4',4''-(4-丙基-1H-吡唑-1,3,5-三基)三[苯酚]

[ 英文名 ]:
PPT

[英文别名 ]:

1,3,5-tris(4-hydroxyphenyl)-4-propyl-1H-pyrazole
4,4',4''-(4-propylpyrazole-1,3,5-triyl)trisphenol
Propyl pyrazole triol

生物活性

[ 描述 ]:

Propyl pyrazole triol (PPT) 是一种雌激素受体 α (ERσ) 激动剂。Propyl pyrazole triol (PPT) 对 ERα 的相对结合亲和力 (ERα: 49%) 是雌激素受体 β (ERβ: 0.12%) 的 410 倍。

[ 相关类别 ]:

信号通路 >> 其他 >> 雌激素受体/ERR

研究领域 >> 癌症

[ 靶点 ]

Estrogen receptor alpha[1]

[体外研究]

ERα-U2OS-Luc细胞中丙基吡唑三醇对ERα依赖性反应的EC50为140 pM [1]。

[参考文献]

[1]. https://www.ncbi.nlm.nih.gov/pubmed/18644836/

[2]. Stauffer SR, et al. Pyrazole ligands: structure-affinity/activity relationships and estrogen receptor-alpha-selective agonists. J Med Chem. 2000 Dec 28;43(26):4934-47.

物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
630.0±55.0 °C at 760 mmHg

[ 熔点 ]:
230 ºC (decomp)

[ 分子式 ]:
C₂₄H₂₂N₂O₃

[ 分子量 ]:
386.44

[ 闪点 ]:
334.8±31.5 °C

[ 精确质量 ]:
386.163055

[ PSA ]:
78.51000

[ LogP ]:
5.95

[ 外观性状 ]:
solid,off-white

[ 蒸汽压 ]:
0.0±1.9 mmHg at 25°C

[ 折射率 ]:
1.642

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
Practically insoluble (0.016 g/L) (25 ºC)

MSDS

详细MSDS(安全技术说明书)

安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xi

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

文献

Development of phenotypic and transcriptional biomarkers to evaluate relative activity of potentially estrogenic chemicals in ovariectomized mice.

Environ. Health Perspect. 123(4) , 344-52, (2015)

Concerns regarding potential endocrine-disrupting chemicals (EDCs) have led to a need for methods to evaluate candidate estrogenic chemicals. Our previous evaluations of two such EDCs revealed a respo...

Chemotherapeutic effect of tamoxifen on temozolomide-resistant gliomas.

Anticancer Drugs 26(3) , 293-300, (2015)

Tamoxifen, a selective estrogen receptor modulator, is widely used in the chemotherapy of estrogen receptor-positive breast cancer. Recent studies have indicated that tamoxifen might have a potential ...

Estradiol and Estrogen Receptor Agonists Oppose Oncogenic Actions of Leptin in HepG2 Cells.

PLoS ONE 11 , e0151455, (2016)

Obesity is a significant risk factor for certain cancers, including hepatocellular carcinoma (HCC). Leptin, a hormone secreted by white adipose tissue, precipitates HCC development. Epidemiology data ...

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