2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. OSU-ERβ-12

OSU-ERβ-12 是一种选择性的口服有效且可透过血脑屏障的 ERβ 激动剂，其 EC50 为 78.3 nM，Ki 为 2.02 nM，对 ERβ 的选择性比 ERα 高出 200 倍以上。OSU-ERβ-12 能够强烈地与 ERβ 结合，减少由 TGF-β 介导的促纤维化基因的表达，从而有助于降低肝纤维化。OSU-ERβ-12 可用于研究纤维化肝病、非酒精性脂肪性肝病 (NAFLD)、神经炎症。

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OSU-ERβ-12

OSU-ERβ-12 Chemical Structure

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Customer Review

OSU-ERβ-12 相关抗体

Top Publications Citing Use of Products

查看 Estrogen Receptor/ERR 亚型特异性产品:

查看所有亚型
Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

OSU-ERβ-12 is a selective, orally active and brain-penetrant ERβ agonist with an EC50 of 78.3 nM and a Ki of 2.02 nM. OSU-ERβ-12 shows more than 200-fold selectivity for ERβ over ERα. OSU-ERβ-12 potently binds to ERβ, reducing the expression of pro-fibrotic genes mediated by TGF-β, which contributes to the reduction of liver fibrosis. OSU-ERβ-12 can be used for the study of fibrotic liver disease, non-alcoholic fatty liver disease (NAFLD), neuroinflammation[1][2][3].

IC50 & Target[1]

ERβ

78.3 nM (EC50)

ERα

>10,000 nM (EC50)

hERβ

2.0 nM (Ki)

hERα

6.6 nM (Ki)

体外研究
(In Vitro)

OSU-ERβ-12 (1 μM；18 小时；HEK-293 细胞) 对 hERβ 具有高度选择性[1]。
OSU-ERβ-12 (10 μM-30 μM；60 分钟；人肝微粒体) 在人肝微粒体中非常稳定[1]。
OSU-ERβ-12 (2 μM；6 小时；小鼠、大鼠、猴和人血浆) 在多种物种的血浆中具有高蛋白结合率[1]。
OSU-ERβ-12 (30 μM；5 分钟；表达 hERG 钾通道的中国仓鼠卵巢细胞) 不抑制 hERG 钾通道[1]。
OSU-ERβ-12 (24 小时；人肝细胞癌细胞 (HepG2) 和人肝星状细胞 (LX-2) 共培养) 降低共培养系统中 TGF-β 介导的促纤维化基因 (MCP-1，TGF-β，COL1A1) 的表达[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

OSU-ERβ-12 相关抗体:
体内研究
(In Vivo)

OSU-ERβ-12 (10 mg/kg，100 mg/kg；灌胃；每日一次；4 周) 可降低 CCl4 诱导的小鼠肝纤维化模型中的肝纤维化[1][3]。
OSU-ERβ-12 (20 mg/kg，50 mg/kg；口服灌胃；连续 6 天) 增加 67NR 小鼠非转移性乳腺肿瘤模型中血浆和大脑浓度以及子宫质量[2]。
OSU-ERβ-12 (50 mg/kg；6 天；双侧卵巢切除 (OVX) 小鼠的海马体、前额皮层和下丘脑) 在下丘脑中增加 IL-6 的表达，主要由肿瘤携带的小鼠驱动[2]。
OSU-ERβ-12 (50 mg/kg；6 天；双侧卵巢切除 (OVX) 小鼠的下丘脑、海马体和前额皮层) 在假手术小鼠的前额皮层中增加 Gper1 和 Cyp19a1 的表达，但在肿瘤携带的小鼠中则没有[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6N mice (22.2 g; 8-week-old) bearing CCl4-induced hepatic fibrosis[1]
Dosage: 10 mg/kg, 100 mg/kg
Administration: Oral gavage; once daily; 4 weeks
Result: Significantly reduced CCl4-induced liver fibrosis in mice at both non-selective (100 mg/kg). 
Animal Model: Balb/c (female, 8-9-week-old, nulliparous, ovariectomized)[2]
Dosage: 20 mg/kg, 50 mg/kg
Administration: oral gavage; 6 consecutive days
Result: Increased plasma and brain concentrations in a dose-dependent manner and increased uterine mass six hours after the final treatment.
Animal Model: Balb/c (female, 8-9-week-old, nulliparous, ovariectomized)[2]
Dosage: 50 mg/kg
Administration: oral gavage; 6 consecutive days
Result: Did not effectively reduce neuroinflammation and increased IL-6 expression in the hippocampus and frontal cortex in tumor-free mice. In tumor-bearing mice, it increased hypothalamic IL-6 expression and partially ameliorated the reduction in hypothalamic expression of Esr1, Esr2, and Gper1.
分子量

352.43

Formula

C25H20O2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

OSU-ERβ-12 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

OSU-ERβ-12Estrogen Receptor/ERRhERGoff-target interactionsagonistNASHERβestrogen receptor betaERβ agonistOSU-ER\u03b2-12Carborane-basedpharmacokineticshuman liver microsome stabilityHepaticCYPER\u03b2-selectiveFibrosisfunctional activityInhibitorinhibitorinhibit

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目录号：
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