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RP-64477 {[allProObj[0].p_purity_real_show]}

货号:A542357 Ambeed 开学季,买赠积分,赢豪礼

RP-64477 is a potent inhibitor of the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT).

RP-64477 化学结构 CAS号:135239-65-5
RP-64477 化学结构
CAS号:135239-65-5
RP-64477 3D分子结构
CAS号:135239-65-5
RP-64477 化学结构 CAS号:135239-65-5
RP-64477 3D分子结构 CAS号:135239-65-5
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RP-64477 纯度/质量文件 产品仅供科研

货号:A542357 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

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产品名称 Transferase 其他靶点 纯度
Tipifarnib +++

FTase, IC50: 0.6 nM

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Tolcapone +

COMT, Ki: 30 nM

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Lonafarnib +++

K-ras-4B, IC50: 2.8 nM

H-ras, IC50: 1.9 nM

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(E)-Daporinad ++++

NMPRTase, Ki: 0.4 nM

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FTI-277 HCl ++++

FTase, IC50: 500 pM

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A 922500 ++

human DGAT-1, IC50: 7 nM

mouse DGAT-1, IC50: 24 nM

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Lomeguatrib ++

O6-alkylguanine-DNA-alkyltransferas, IC50: 5 nM

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PF-04620110 +

DGAT1, IC50: 19 nM

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LB42708 +++

FTase (K-Ras), IC50: 0.8 nM

FTase (N-ras), IC50: 1.2 nM

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GGTI298 Trifluoroacetate {[allProObj[0].p_purity_real_show]}
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

RP-64477 生物活性

描述 RP-64477 is identified as a powerful inhibitor of Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT), an enzyme essential for cholesterol esterification. It demonstrates inhibitory effects across a variety of species and tissues, with IC50 values ranging from 6 to 283 nM, indicating a broad spectrum of activity without noticeable differences between species or tissues. Additionally, RP-64477 shows significant inhibition in human cell lines derived from hepatic (HepGZ), intestinal (CaCo-2), and monocytic (THP-1) origins, with IC50s of 503, 113, and 180 nM, respectively. It does not inhibit rat PCEH or LCAT up to concentrations of 200 μM and 20 μM, respectively[1].
体内研究

Dietary incorporation of RP-64477 at 0.01% and 0.03% w/w significantly lowers plasma cholesterol levels in cholesterol/cholic acid-fed rats by 29% and 61%, respectively, without affecting food intake. This reduction in plasma cholesterol levels is also observed with RP-64477 doses of 10 and 30 mg/kg b.i.d., showing a 35% and 53% decrease, respectively, after 7 days compared to cholesterol-fed controls[1].

体外研究

RP-64477 is identified as a powerful inhibitor of Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT), an enzyme essential for cholesterol esterification. It demonstrates inhibitory effects across a variety of species and tissues, with IC50 values ranging from 6 to 283 nM, indicating a broad spectrum of activity without noticeable differences between species or tissues. Additionally, RP-64477 shows significant inhibition in human cell lines derived from hepatic (HepGZ), intestinal (CaCo-2), and monocytic (THP-1) origins, with IC50s of 503, 113, and 180 nM, respectively. It does not inhibit rat PCEH or LCAT up to concentrations of 200 μM and 20 μM, respectively[1].

RP-64477 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.

RP-64477 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.01mL

0.40mL

0.20mL

10.03mL

2.01mL

1.00mL

20.05mL

4.01mL

2.01mL

RP-64477 技术信息

CAS号135239-65-5
分子式C29H42N2O3S
分子量 498.72
别名
运输蓝冰
存储条件

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 7 mg/mL(14.04 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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