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RP-64477

目录号: PL14723 纯度: ≥99%

RP-64477 是胆固醇酯化酶酰基辅酶 A：胆固醇 O-酰基转移酶 (ACAT) 的有效抑制剂。

CAS No. :135239-65-5

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中文名称	RP-64477
英文名称	RP-64477
英文别名	RP-64477;K10EML8B3S;n-Butyl-3-(4-decyloxybenzamido)-4-(methylthio)benzamide;N-butyl-3-[(4-decoxybenzoyl)amino]-4-methylsulfanylbenzamide;rp64477;RP 64477;N-butyl-3-(p-decyloxybenzamido)-4-(methylthio)benzamide;N'-Butyl-4-(decyloxy)-4'-(methylthio)-N,3'-bibenzamide;N-butyl-3-(4-(decyloxy)benzamido)-4-(methylthio)benzamide;Benzamide, n-butyl-3-((4-(decyloxy)benzoyl)amino)-4-(methylthio)-
Cas No.	135239-65-5
分子式	C₂₉H₄₂N₂O₃S
分子量	498.72
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	RP-64477 是胆固醇酯化酶酰基辅酶 A：胆固醇 O-酰基转移酶 (ACAT) 的有效抑制剂。

产品详情	RP-64477 是胆固醇酯化酶酰基辅酶 A：胆固醇 O-酰基转移酶 (ACAT) 的有效抑制剂。
生物活性	RP-64477 is a potent inhibitor of the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT).
性状	Solid
IC50 & Target[1][2]	ACAT
体外研究(In Vitro)	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, IC50 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 IC50s 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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Bello AA, et al. RP 64477: a potent inhibitor of acyl-coenzyme A:cholesterol O-acyltransferase with low systemic bioavailability. Biochem Pharmacol. 1996 Feb 23;51(4):413-21.

溶解度数据	In Vitro: DMSO : 8.33 mg/mL (16.70 mM; Need ultrasonic)配制储备液

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[1]. Bello AA, et al. RP 64477: a potent inhibitor of acyl-coenzyme A:cholesterol O-acyltransferase with low systemic bioavailability. Biochem Pharmacol. 1996 Feb 23;51(4):413-21.

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

RP-64477

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