135239-65-5
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- CAS号:
- 135239-65-5
- 英文名:
- RP-64477
- 英文别名:
- 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
- 中文名:
- 135239-65-5
- 中文别名:
- 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
- CBNumber:
- CB42667296
- 分子式:
- C29H42N2O3S
- 分子量:
- 498.72
- MOL File:
- 135239-65-5.mol
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135239-65-5化学性质
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储存条件:
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Store at -20°C
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溶解度:
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DMSO: 8.33 mg/mL (16.70 mM)
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形态:
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Solid
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颜色:
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White to off-white
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135239-65-5性质、用途与生产工艺
RP-64477 是一种胆固醇酯化酶 Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT) 的有效抑制剂。RP-64477 可抑制ACAT活性,在人肠道(CaCo-2)、肝(HepG2)和单核细胞(THP-1)细胞试验中对应的IC50值分别为113 nM、503 nM和180 nM。
Target | Value |
ACAT
(CaCo-2 cell-based assay)
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113 nM
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ACAT
(THP-1 cell-based assay)
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180 nM
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ACAT
(HepG2 cell-based assay)
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503 nM
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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.
135239-65-5
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下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/04/30 | HY-16437 | 135239-65-5 RP-64477 | 135239-65-5 | 5mg | 2210元 |
2024/04/30 | S0820 | 135239-65-5 RP-64477 | 135239-65-5 | 5mg | 2449.54元 |
135239-65-5, 135239-65-5 相关搜索:
- 药靶配体
- N-丁基-3-(4-(癸氧基)苯甲酰胺基)-4-(甲硫基)苯甲酰胺
- 化合物RP64477
- 135239-65-5
- RP-64477,Diglyceride acyltransferase,RP 64477,inhibit,mono- acylglycerol acyltransferase,Acyltransferase,Inhibitor,acyl-CoA:cholesterol acyltransferase,Diacylglycerol acyltransferase
- Benzamide, N-butyl-3-[[4-(decyloxy)benzoyl]amino]-4-(methylthio)-
- RP-64477