2. Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  3. Estrogen Receptor/ERR Reactive Oxygen Species
  4. GSK5182

GSK5182 是一种高效选择性，具有口服活性的 ERRγ 反向激动剂，其 IC50 值为 79 nM。GSK5182 不与其他核受体相互作用，包括 ERRα 和 ERα。GSK5182 还能增加肝癌细胞中 reactive oxyen species (ROS) 的产生。

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GSK5182 Chemical Structure

GSK5182 Chemical Structure

CAS No. : 877387-37-6

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1430
In-stock
1 mg ￥495
In-stock
5 mg ￥1300
In-stock
10 mg ￥1900
In-stock
25 mg ￥3500
In-stock
50 mg ￥5300
In-stock
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of GSK5182:

GSK5182 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

GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM. GSK5182 does not interact with other nuclear receptors, including ERRα or ERα. GSK5182 also induces reactive oxyen species (ROS) generation in hepatocellular carcinoma (HCC)[1][2][3].

IC50 & Target[1][2]

ERRγ

79 nM (IC50)

Reactive Oxygen Species

 

体外研究
(In Vitro)

GSK5182 (0-20 μM; 0-hours; PLC/PRF/5 cells) treatment leads to a significant and dose-dependent reduction in the number of proliferating PLC/PRF/5 cells[1].
GSK5182 (0-20 μM; 24 hours; PLC/PRF/5 cells) treatment also causes a dose-dependent increase in the expression of p21 and p27 while at the same time reducing the level of phosphorylated retinoblastoma protein (p-pRb)[1].
GSK5182 (10-20 μM; PLC/PRF/5 cells) treatment induces cell cycle arrest at G1 phase, which in turn induces a corresponding dose-dependent reduction in the percentage of cells in S phase[1].

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

GSK5182 相关抗体:

Cell Proliferation Assay[1]

Cell Line: The human hepatoma cell line PLC/PRF/5
Concentration: 0 μM, 10 μM, 20 μM
Incubation Time: 0 hour, 24 hours, 48 hours, 72 hours
Result: Led to a significant and dose-dependent reduction in the number of proliferating PLC/PRF/5 cells.

Western Blot Analysis[1]

Cell Line: The human hepatoma cell line PLC/PRF/5
Concentration: 0 μM, 10 μM, 20 μM
Incubation Time: 24 hours
Result: Caused a dose-dependent increase in the expression of p21 and p27 while at the same time reducing the level of p-pRb.

Cell Cycle Analysis[1]

Cell Line: The human hepatoma cell line PLC/PRF/5
Concentration: 10 μM, 20 μM
Incubation Time:
Result: Induced cell cycle arrest.
体内研究
(In Vivo)

GSK5182 (40 mg/kg; intraperitoneal injection; every day; 25 or 30 days; db/db mice, diet-induced obesity mice) specifically inhibits the transcriptional activity of ERRγ, and suppresses hepatic glucose production through inhibition of hepatic gluconeogenesis. GSK5182 elicits anti-diabetic effects in mouse models via negative regulation of the hepatic gluconeogenesis program. GSK5182 normalizes hyperglycemia mainly through inhibition of hepatic glucose production[3].

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

Animal Model: db/db mice (male, 7-12-week-old), diet-induced obesity (DIO) mice[3]
Dosage: 40 mg/kg
Administration: Intraperitoneal injection; every day; 30 days for db/db mice, 25 days for DIO mice
Result: Inhibited the transcriptional activity of ERRγ, suppressed hepatic glucose production through inhibition of hepatic gluconeogenesis.
分子量

417.55

Formula

C27H31NO3
CAS 号
性状

固体

颜色

White to off-white

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
细胞实验： 

DMSO 中的溶解度 : 25 mg/mL (59.87 mM; 超声助溶 (<80°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3949 mL 11.9746 mL 23.9492 mL
5 mM 0.4790 mL 2.3949 mL 4.7898 mL
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 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。

  • 方案 一

    请依序添加每种溶剂： 50% PEG300    50% Saline

    Solubility: 25 mg/mL (59.87 mM); 悬浊液; 超声助溶

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.85%

COA (285 KB) HNMR (185 KB) LCMS (95 KB)

产品使用指南 (1538 KB)
参考文献

GSK5182 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3949 mL 11.9746 mL 23.9492 mL 59.8731 mL
5 mM 0.4790 mL 2.3949 mL 4.7898 mL 11.9746 mL
10 mM 0.2395 mL 1.1975 mL 2.3949 mL 5.9873 mL
15 mM 0.1597 mL 0.7983 mL 1.5966 mL 3.9915 mL
20 mM 0.1197 mL 0.5987 mL 1.1975 mL 2.9937 mL
25 mM 0.0958 mL 0.4790 mL 0.9580 mL 2.3949 mL
30 mM 0.0798 mL 0.3992 mL 0.7983 mL 1.9958 mL
40 mM 0.0599 mL 0.2994 mL 0.5987 mL 1.4968 mL
50 mM 0.0479 mL 0.2395 mL 0.4790 mL 1.1975 mL
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:

GSK5182877387-37-6GSK 5182GSK-5182Estrogen Receptor/ERRReactive Oxygen SpeciesInhibitorinhibitorinhibit

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