GSK5182|cas:877387-37-6|西域试剂

GSK5182,99.85%

产品编号：Bellancom-111226| CAS NO：877387-37-6| 分子式：C₂₇H₃₁NO₃| 分子量：417.54

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货号	价格	库存与货期
Bellancom-111226	￥1300.00	杭州北京（现货）
Bellancom-111226	￥1900.00	杭州北京（现货）
Bellancom-111226	￥3500.00	杭州北京（现货）
Bellancom-111226	￥5300.00	杭州北京（现货）
Bellancom-111226	￥8000.00	杭州北京（现货）

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GSK5182

产品介绍

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。

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).

体外研究

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.
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).
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.

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

Cell Proliferation Assay

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

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

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.

西域 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
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.

体内研究

西域 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
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.

体内研究

西域 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
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 25 mg/mL (59.87 mM; ultrasonic and warming and heat to 80°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3950 mL	11.9749 mL	23.9498 mL
5 mM	0.4790 mL	2.3950 mL	4.7900 mL
10 mM	0.2395 mL	1.1975 mL	2.3950 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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式