2,2-二甲基-N-(2,4,6-三甲氧基苯基)月桂酰胺

用途

PD 128042(CI 976)是ACAT(酰基辅酶a：胆固醇酰基转移酶)的有效、口服活性和选择性抑制剂,IC50s为73 nM。PD 128042也是一种有效的LPAT(溶血磷脂酰基转移酶)抑制剂。PD 128042抑制高尔基体相关LPAT活性(IC50=15μM)。PD 128042抑制多种膜运输步骤,包括在内吞和分泌途径中发现的步骤[1][2][3]。

名称

[ CAS 号 ]:
114289-47-3

[ 中文名 ]:
2,2-二甲基-N-(2,4,6-三甲氧基苯基)月桂酰胺

[ 英文名 ]:
PD 128042

[英文别名 ]:

CI 976
C23H39NO4

生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 代谢疾病

[体内研究]

PD 128042(CI 976)(10-30 mg/kg；在慢性胆固醇喂养的大鼠模型中,灌胃)可降低非高密度脂蛋白(HDL)-胆固醇,并增加血脂异常大鼠的HDL胆固醇[4]。

[参考文献]

[1]. Chambers K, et al. A unique lysophospholipid acyltransferase (LPAT) antagonist, CI-976, affects secretory and endocytic membrane trafficking pathways. J Cell Sci. 2005;118(Pt 14):3061-3071.

[2]. O'Brien PM, et al. Inhibitors of acyl-CoA:cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 8. Incorporation of amide or amine functionalities into a series of disubstituted ureas and carbamates. Effects on ACAT inhibition in vitro and efficacy in vivo. J Med Chem. 1994;37(12):1810-1822.

[3]. Drecktrah D, et al. Inhibition of a Golgi complex lysophospholipid acyltransferase induces membrane tubule formation and retrograde trafficking. Mol Biol Cell. 2003;14(8):3459-3469.

[4]. Krause BR, et al. In vivo evidence that the lipid-regulating activity of the ACAT inhibitor CI-976 in rats is due to inhibition of both intestinal and liver ACAT. J Lipid Res. 1993;34(2):279-294.

物理化学性质

[ 密度 ]:
1.002g/cm3

[ 沸点 ]:
504.7ºC at 760mmHg

[ 分子式 ]:
C₂₃H₃₉NO₄

[ 分子量 ]:
393.56000

[ 闪点 ]:
259ºC

[ 精确质量 ]:
393.28800

[ PSA ]:
56.79000

[ LogP ]:
6.28090

[ 蒸汽压 ]:
2.59E-10mmHg at 25°C

[ 折射率 ]:
1.503

[ 储存条件 ]:
2-8°C，干燥，密封

MSDS

详细MSDS(安全技术说明书)

毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: JR2052000

CHEMICAL NAME :: Dodecanamide, 2,2-dimethyl-N-(2,4,6-trimethoxyphenyl)-

CAS REGISTRY NUMBER :: 114289-47-3

LAST UPDATED :: 199612

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C23-H39-N-O4

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 157 gm/kg/56W-C

TOXIC EFFECTS :: Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: TOXID9 Toxicologist. (Soc. of Toxicology, Inc., 475 Wolf Ledge Parkway, Akron, OH 44311) V.1- 1981- Volume(issue)/page/year: 13,317,1993

安全信息

[ 危害声明 ]:
H413

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xi

[ 危险品运输编码 ]:
NONH for all modes of transport

[ 海关编码 ]:
2924299090

海关

[ 海关编码 ]: 2924299090

[ 中文概述 ]:
2924299090. 其他环酰胺（包括环氨基甲酸酯）（包括其衍生物以及他们的盐）. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 包装

[ Summary ]:
2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

文献

cPLA2α and EHD1 interact and regulate the vesiculation of cholesterol-rich, GPI-anchored, protein-containing endosomes.

Mol. Biol. Cell 23(10) , 1874-88, (2012)

The lipid modifier phospholipase A2 catalyzes the hydrolysis of phospholipids to inverted-cone-shaped lysophospholipids that contribute to membrane curvature and/or tubulation. Conflicting findings ex...

Use of acyltransferase inhibitors to block vesicular traffic between the ER and Golgi complex.

Meth. Enzymol. 404 , 115-25, (2005)

This article describes the use of acyltransferase inhibitors as probes for studying the potential role of lysophospholipid acyltransferases (LPAT) in intracellular membrane trafficking in the secretor...

A unique lysophospholipid acyltransferase (LPAT) antagonist, CI-976, affects secretory and endocytic membrane trafficking pathways.

J. Cell Sci. 118(Pt 14) , 3061-71, (2005)

Previous studies have shown that inhibition of a Golgi-complex-associated lysophospholipid acyltransferase (LPAT) activity by the drug CI-976 stimulates Golgi tubule formation and subsequent redistrib...

更多文献