1438071-12-5

中文名称 N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine

英文名称 N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine

CAS 1438071-12-5

分子式 C20H18Cl2N2O2S

分子量 421.34

MOL 文件 1438071-12-5.mol

1438071-12-5 结构式

基本信息物理化学性质常见问题列表

基本信息

中文别名

化合物 T11490
化合物 GSK2945

英文别名

GSK-2945
GSK-2945 (GSK2945 )
GSK 2945 DISCONTINUED. Please see G797405
2-Thiophenemethanamine, N-[(4-chloro-2-methylphenyl)methyl]-N-[(4-chlorophenyl)methyl]-5-nitro-
N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine

物理化学性质

沸点525.0±45.0 °C(Predicted)

密度1.363±0.06 g/cm3(Predicted)

溶解度Acetonitrile (Slightly), DMSO (Slightly, Heated), Methanol (Slightly, Sonicated)

酸度系数(pKa)5.23±0.50(Predicted)

形态Solid

颜色Off-White to Light Beige

稳定性Hygroscopic

常见问题列表

生物活性

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。

体外研究

GSK2945 dose-dependently enhances the transcriptional activity of Rev-erbα and a Bmal1 (a target gene of REV-ERBs) luciferase reporter ( EC ₅₀ of 2.05 μM).
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.

RT-PCR

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

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.

Animal Model:	Male C57BL/6 mice (8-10 weeks of age)
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.