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. |
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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. |
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| 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 | 1 mM | 2.3734 mL | 11.8669 mL | 23.7338 mL | | 5 mM | 0.4747 mL | 2.3734 mL | 4.7468 mL | | 10 mM | 0.2373 mL | 1.1867 mL | 2.3734 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。 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。
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