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

生物活性体外研究体内研究

CAS号:: 1438071-12-5

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

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

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

中文别名:: 化合物 T11490

CBNumber:: CB63464337

分子式:: C20H18Cl2N2O2S

分子量:: 421.34

MOL File:: 1438071-12-5.mol

化学性质安全信息用途供应商 7

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

安全信息

N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine性质、用途与生产工艺

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。

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.

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

4-氯-2-甲基苯甲醛对氯苄胺

下游产品

N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine 生产厂家

全球有 7家供应商 N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine国内生产厂家

供应商	联系电话	电子邮件	国家	产品数	优势度
上海摩纹医药科技有限公司	13681854265	info@moenpharm.com	中国	511	55
TargetMol Chemicals Inc.	+1-781-999-5354 +1-00000000000	marketing@targetmol.com	美国	19892	58
安耐吉化学&3A（安徽泽升科技有限公司）	021-58432009 400-005-6266	marketing@energy-chemical.com	中国	44941	58
天津普西唐生物医药科技有限公司	010-60605840	psaitong@jm-bio.com	中国	29778	58
TargetMol中国（陶术生物）	4008200310	marketing@tsbiochem.com	中国	24017	58
銳迪國際科技有限公司	18024082417	market@ubiochem.com	中国	9180	58

1438071-12-5, N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine 相关搜索:

化合物 T11490
1438071-12-5
GSK 2945 DISCONTINUED. Please see G797405
2-Thiophenemethanamine, N-[(4-chloro-2-methylphenyl)methyl]-N-[(4-chlorophenyl)methyl]-5-nitro-
GSK-2945 (GSK2945 )
GSK-2945
N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine