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GSK2945
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GSK2945图片
CAS NO:1438071-12-5
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
GSK2945 是一类叔胺,是一种高度特异性的Rev-erbα/REV-ERBα(小鼠/人反向成红细胞病病毒α) 拮抗剂, 其EC50值分别为 21.5 μM 和 20.8 μM。GSK2945 可增强胆固醇 7α-羟化酶 (CYP7A1) 水平和胆固醇代谢。
生物活性

GSK2945 is a class of tertiary amine, and is a highly specificRev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α)antagonist withEC50s of 21.5 μM and 20.8 μM, respectively. GSK2945 enhancescholesterol7α-hydroxylase (CYP7A1)level andcholesterolmetabolism[1].

体外研究
(In Vitro)

GSK2945 dose-dependently enhances the transcriptional activity of Rev-erbα and a Bmal1 (a target gene of REV-ERBs) luciferase reporter (EC50of 2.05 μM)[1].
GSK2945 (20 μM; 12 hours and 24 hours; mouse and human primary hepatocytes) treatment increases levels of Cyp7a1/CYP7A1 in mouse and human primary hepatocytes. GSK2945 (20 μM) treatment also increases Lrh-1/LRH-1 (a known hepatic activator of Cyp7a1/CYP7A1) mRNA and protein[1].

RT-PCR[1]

Cell Line:Mouse (male, CD1) and human (male, Caucasian) primary hepatocytes
Concentration:20 μM
Incubation Time:12 hours and 24 hours
Result:Led to significant increases in mRNA and protein (at 24-h) expression of Cyp7a1. mRNA and protein (at 24-h) levels of CYP7A1 were increased in human primary hepatocyte. Lrh-1/LRH-1 was upregulated.
体内研究
(In Vivo)

GSK2945 (0-10 mg/kg; intraperitoneal injection; twice every day; for 7 days; male C57BL/6 mice) treatment increases hepatic mouse cholesterol 7α-hydroxylase (Cyp7a1) level and lowers plasma cholesterol in wild-type mice[1].

Animal Model:Male C57BL/6 mice (8-10 weeks of age)[1]
Dosage:0 mg/kg or 10 mg/kg
Administration:Intraperitoneal injection; twice every day; for 7 days
Result:Increased hepatic mouse cholesterol 7α-hydroxylase (Cyp7a1) level and lowered plasma cholesterol in wild-type mice.
分子量

421.34

Formula

C20H18Cl2N2O2S

CAS 号

1438071-12-5

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.

溶解性数据
In Vitro: 

DMSO : 83.33 mg/mL(197.77 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.3734 mL11.8669 mL23.7338 mL
5 mM0.4747 mL2.3734 mL4.7468 mL
10 mM0.2373 mL1.1867 mL2.3734 mL
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: ≥ 2.08 mg/mL (4.94 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.94 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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%corn oil

    Solubility: ≥ 2.08 mg/mL (4.94 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.94 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 20.8 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本网站选购。