1438071-12-5
中文名稱
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 結(jié)構(gòu)式
基本信息
英文別名
GSK-2945GSK-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
物理化學(xué)性質(zhì)
沸點(diǎn)525.0±45.0 °C(Predicted)
密度1.363±0.06 g/cm3(Predicted)
酸度系數(shù)(pKa)5.23±0.50(Predicted)
常見問題列表
生物活性
GSK2945 是一類叔胺，是一種高度特異性的 Rev-erbα/REV-ERBα (小鼠/人反向成紅細(xì)胞病病毒α) 拮抗劑， 其 EC50 值分別為 21.5 μM 和 20.8 μM。GSK2945 可增強(qiáng)膽固醇 7α-羥化酶 (CYP7A1) 水平和膽固醇代謝。體外研究
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. |
體內(nèi)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. |