N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine
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- CAS號(hào):
- 1438071-12-5
- 英文名:
- N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine
- 英文別名:
- 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
- 中文別名:
- 化合物 T11490;化合物 GSK2945
- CBNumber:
- CB63464337
- 分子式:
- C20H18Cl2N2O2S
- 分子量:
- 421.34
- MOL File:
- 1438071-12-5.mol
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N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine化學(xué)性質(zhì)
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沸點(diǎn):
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525.0±45.0 °C(Predicted)
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密度:
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1.363±0.06 g/cm3(Predicted)
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溶解度:
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Acetonitrile (Slightly), DMSO (Slightly, Heated), Methanol (Slightly, Sonicated)
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酸度系數(shù)(pKa):
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5.23±0.50(Predicted)
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形態(tài):
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Solid
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顏色:
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Off-White to Light Beige
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穩(wěn)定性:
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Hygroscopic
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N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine性質(zhì)、用途與生產(chǎn)工藝
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。
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
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Cell Line:
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Mouse (male, CD1) and human (male, Caucasian) primary hepatocytes
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Concentration:
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20 μM
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Incubation Time:
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12 hours and 24 hours
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Result:
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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.
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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.
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Animal Model:
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Male C57BL/6 mice (8-10 weeks of age)
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Dosage:
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0 mg/kg or 10 mg/kg
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Administration:
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Intraperitoneal injection; twice every day; for 7 days
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Result:
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Increased hepatic mouse cholesterol 7α-hydroxylase (Cyp7a1) level and lowered plasma cholesterol in wild-type mice.
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N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine
上下游產(chǎn)品信息
上游原料
下游產(chǎn)品
N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine
生產(chǎn)廠家
1438071-12-5, N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine 相關(guān)搜索:
- 抑制劑
- 化合物 GSK2945
- 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