1438071-12-5
中文名称
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
结构式
基本信息
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
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) |
| 酸度系数(pKa) | 5.23±0.50(Predicted) |
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. |
供应商信息 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 GSK2945
英文名称：GSK2945
CAS：1438071-12-5
包装信息：25mg/RMB 10600;100mg/RMB 17500;50mg/RMB 13800
銳迪國際科技有限公司
联系电话：
18024082417
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
常州优瑞医药科技有限公司
联系电话：
18168818882
产品介绍：
英文名称：N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine
CAS：1438071-12-5
纯度：98%
包装信息：100mg;1g;10g;50g;100g;500g;1kg;10kg
备注：100%自产自研，非经销，医药级，可定制