Prinaberel(Synonyms: 普林贝瑞; ERB-041)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Prinaberel (Synonyms: 普林贝瑞; ERB-041) 纯度: 98.62%

Prinaberel (ERB-041) 是一种有效的选择性雌激素受体 β (ERβ) 激动剂,对人,大鼠和小鼠 ERβ 的 IC50 分别为 5.4、3.1 和 3.7 nM。 Prinaberel 对 ERβ 的选择性是 ERα 的 200 倍以上。Prinaberel是有效的皮肤癌化学预防剂,可通过抑制 WNT/β-catenin 信号通路发挥作用。Prinaberel 诱导卵巢癌细胞凋亡 (apoptosis)。

Prinaberel(Synonyms: 普林贝瑞; ERB-041)

Prinaberel Chemical Structure

CAS No. : 524684-52-4

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Prinaberel 相关产品

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生物活性

Prinaberel (ERB-041) is a potent and selective estrogen receptor (ER) β agonist with IC50s of 5.4, 3.1 and 3.7 nM for human, rat and mouse ERβ, respectively. Prinaberel displays >200-fold selectivity for ERβ over ERα. Prinaberel is a potent skin cancer chemopreventive agent that acts by dampening the WNT/β-catenin signaling pathway. Prinaberel induces ovarian cancer apoptosis[1][2][3].

IC50 & Target

hERβ

5.4 nM (IC50)

rat ERβ

3.1 nM (IC50)

mouse ERβ

3.7 nM (IC50)

hERα

1200 nM (IC50)

mouse ERα

750 nM (IC50)

rat ERα

620 nM (IC50)

体外研究
(In Vitro)

Prinaberel (ERB-041) (0-60 µM; 24 hours) treatment of human SCC cells induces cell differentiation, cell cycle arrest and reduces colony formation[2].
Prinaberel shows a marked reduction in the expression of inflammation regulatory proteins such as p-NFκBp65, iNOS and COX-2 in A431 cells. Prinaberel diminishes phosphorylated-PI3K and -AKT, which is associated with the enhancement in E-cadherin expression and reduction in migration of A431 cells[2].
Prinaberel (0.01-10 µM) inhibits cell proliferation in a dose- and time-dependent manner[3].
Prinaberel (10 µM; 48 hours) promotes ovarian cancer (SKOV-3 cells) apoptosis[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[2]

Cell Line: A431 cells
Concentration: 0, 20, 40 and 60 µM
Incubation Time: 24 hours
Result: Reduction in the expression of G1 cyclins (D1, D2 and D3) and CDK4.

Cell Proliferation Assay[3]

Cell Line: SKOV-3, A2780CP or OVCAR-3 cells
Concentration: 0.01, 0.1 and 10 µM
Incubation Time: 24-48 hours
Result: Showed significantly inhibitory effect on cell proliferation.

体内研究
(In Vivo)

Prinaberel (2mg/mouse; topically; 30 min prior to UVB irradiation for 30 weeks) suppresses development of squamous cell carcinoma in SKH-1 hairless mice[2].
Prinaberel reduces proliferation and angiogenesis and induces apoptosis in UVB-induced skin tumors. Prinaberel suppresses pro-inflammatory signaling pathway in UVB-induced skin tumors. Prinaberel diminished tumor invasiveness via PI3K-AKT pathway and WNT signaling[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Six- to eight-weeks-old SKH-1 hairless female mice[2]
Dosage: 2 mg/mouse in 200µl ethanol
Administration: Topically; 30 min prior to UVB (180mJ/cm2) irradiation for 30 weeks
Result: Diminished UVB-induced skin tumor development in SKH-1 hairless mice.

Clinical Trial

分子量

271.24

Formula

C15H10FNO3

CAS 号

524684-52-4

中文名称

普林贝瑞

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 40 mg/mL (147.47 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.6868 mL 18.4339 mL 36.8677 mL
5 mM 0.7374 mL 3.6868 mL 7.3735 mL
10 mM 0.3687 mL 1.8434 mL 3.6868 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 5 mg/mL (18.43 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (18.43 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 5 mg/mL (18.43 mM); Suspended solution; Need ultrasonic

    此方案可获得 5 mg/mL (18.43 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 5 mg/mL (18.43 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (18.43 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Malamas MS, et al. Design and synthesis of aryl diphenolic azoles as potent and selective estrogen receptor-beta ligands. J Med Chem. 2004;47(21):5021-5040.

    [2]. Chaudhary SC, et al. Erb-041, an estrogen receptor-β agonist, inhibits skin photocarcinogenesis in SKH-1 hairless mice by downregulating the WNT signaling pathway. Cancer Prev Res (Phila). 2014;7(2):186-198.

    [3]. Chan KKL, et al. Estrogen receptor modulators genistein, daidzein and ERB-041 inhibit cell migration, invasion, proliferation and sphere formation via modulation of FAK and PI3K/AKT signaling in ovarian cancer. Cancer Cell Int. 2018;18:65. Published 2018 May 1.

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