N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine
N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine
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号:1438071-12-5
分子式:C20H18Cl2N2O2S
分子量:421.34
EINECS号:
Mol文件:1438071-12-5.mol
![N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine 结构式](https://img.chemicalbook.com/CAS/20180601/GIF/1438071-12-5.gif)
N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine 性质
| 沸点 | 525.0±45.0 °C(Predicted) |
|---|---|
| 密度 | 1.363±0.06 g/cm3(Predicted) |
| 溶解度 | 可溶于乙腈（轻微）、DMSO（轻微、加热）、甲醇（轻微、超声处理） |
| 酸度系数(pKa) | 5.23±0.50(Predicted) |
| 形态 | 固体 |
| 颜色 | 灰白色至浅米色 |
| 稳定性 | 吸湿性 |
N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine 用途与合成方法
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。
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. |
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. |
N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine 上下游产品信息
上游原料
N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine供应商 更多
上海摩纹医药科技有限公司
联系电话： 13681854265
产品介绍：
英文名称：N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine
纯度：0.97
包装信息：10g;100g;1kg
天津普西唐生物医药科技有限公司
联系电话：010-60605840 15801484223
产品介绍：
英文名称：GSK2945
CAS：1438071-12-5
包装信息：5mg;25mg
备注： 试剂级
TargetMol中国（陶术生物）
联系电话： 4008200310
产品介绍：
中文名称：化合物 T11490
英文名称：GSK2945;GSK2945,GSK-2945
CAS：1438071-12-5
纯度：98%
包装信息：5 mg
銳迪國際科技有限公司
联系电话： 18988968278
产品介绍：
英文名称：GSK2945
CAS：1438071-12-5
纯度：5mg;10mg;50mg;100mg;250mg;500mg;1g
包装信息：5mg;10mg;50mg;100mg;250mg;500mg;1g
