135239-65-5
中文名称 | 135239-65-5 |
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中文同义词 | 化合物RP64477;N-丁基-3-(4-(癸氧基)苯甲酰胺基)-4-(甲硫基)苯甲酰胺 |
英文名称 | RP-64477 |
英文同义词 | RP-64477;Benzamide, N-butyl-3-[[4-(decyloxy)benzoyl]amino]-4-(methylthio)-;RP-64477,Diglyceride acyltransferase,RP 64477,inhibit,mono- acylglycerol acyltransferase,Acyltransferase,Inhibitor,acyl-CoA:cholesterol acyltransferase,Diacylglycerol acyltransferase |
CAS号 | 135239-65-5 |
分子式 | C29H42N2O3S |
分子量 | 498.72 |
EINECS号 | |
相关类别 | |
Mol文件 | 135239-65-5.mol |
结构式 | ![]() |
135239-65-5 性质
储存条件 | Store at -20°C |
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溶解度 | 二甲基亚砜:8.33 mg/mL(16.70 mM) |
形态 | 固体 |
颜色 | 白色至米白色 |
Target | Value |
ACAT
(CaCo-2 cell-based assay) | 113 nM |
ACAT
(THP-1 cell-based assay) | 180 nM |
ACAT
(HepG2 cell-based assay) | 503 nM |
RP-64477 is a potent inhibitor of the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT). Inhibitory potencies of RP-64477 in vitro in tissue preparations are obtained from a range of species and in human cell cultures. For animal tissues, IC 50 values in the range 6 to 283 nM are recorded, with no obvious species/tissue differences apparent. Potent inhibitory activity of RP-64477 is also recorded in human cell lines of hepatic (HepGZ), intestinal (CaCo-2), and monocytic (THP-1) origin with IC 50 s of 503, 113, and 180 nM, respectively. No inhibitory activity is recorded against rat PCEH or LCAT at test concentrations up to 200 μM and 20 μM, respectively.
Administration of RP-64477 (0.01% and 0.03% w/w by diet) reduces significantly plasma cholesterol levels in cholesterol/cholic acid-fed rats by 29% and 61%, respectively. Food consumption is not affected by dietary incorporation of RP-64477. Animals receiving RP-64477 (10 and 30 mg/kg b.i.d.) over this period exhibit significantly lower plasma cholesterol levels on both days 4 and 7 when compare to values recorded from vehicle treated animals fed the cholesterol-containing diet. Compare to cholesterol-fed controls, after 7 days of dosing, plasma cholesterol levels are 35% and 53% lower in animals receiving 10 and 30 mg/kg b.i.d. doses of RP-64477, respectively.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-16437 | 135239-65-5 RP-64477 | 135239-65-5 | 5mg | 1800元 |
2024/08/19 | HY-16437 | 135239-65-5 RP-64477 | 135239-65-5 | 10 mg | 2880元 |