2. Metabolic Enzyme/Protease
  3. Acyltransferase
  4. RP-64477

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。

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RP-64477 Chemical Structure

RP-64477 Chemical Structure

CAS No. : 135239-65-5

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规格 价格 是否有货 数量
5 mg ￥1800
In-stock
10 mg ￥2880
In-stock
25 mg ￥5180
In-stock
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Customer Review

RP-64477 相关抗体

Top Publications Citing Use of Products

查看 Acyltransferase 亚型特异性产品:

查看所有亚型
ACAT1 ACAT2 MGAT2 ACAT

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

IC50 & Target

ACAT[1]
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

RP-64477 相关抗体:
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

498.72

Formula

C29H42N2O3S
CAS 号
性状

固体

颜色

White to off-white

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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 8.33 mg/mL (16.70 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0051 mL 10.0257 mL 20.0513 mL
5 mM 0.4010 mL 2.0051 mL 4.0103 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献
Cell Assay
[1]

ACAT activity is determined in CaCo-2 cells. Cells cultured in 6-well plates are preincubated for 2 hr in 2 mL of Medium 199 supplemented with 10 mM Hepes, pH 7.4, and cholesterol-rich micelles in the presence or absence of RP-64477 that has been initially prepared in neat DMSO. The final concentration of DMSO in the culture medium is 0.2% v/v. Preincubation medium is then replaced with the same medium containing 50 μM [14C] oleic acid complexed with 17 μM bovine serum albumin (fatty acid-free) and cells incubated for a further 2 hr. RP-64477 or vehicle is present during both incubations[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Hypocholesterolaemic activity of RP-64477 is investigated by administering RP-64477 (0.00l% to 0.03% w/w by diet) to rats maintained for 3 days on powdered laboratory diet supplemented with cholesterol/cholic acid. Animals are then killed by asphyxiation in carbon dioxide, and terminal blood samples taken by cardiac puncture into a heparinised syringe for preparation of plasma. Plasma cholesterol concentrations are determined enzymatically using standard assay kits. Hypocholesterolaemic activity of RP-64477 in rabbits is investigated by administering RP-64477 at doses of 1, 3, 10, and 30 mg/kg b.i.d. for 7 days to animals receiving standard laboratory diet supplemented with cholesterol. Blood samples are obtained from the central ear artery on days 0 (predosing), 4, and 7 of the study[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

RP-64477 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0051 mL 10.0257 mL 20.0513 mL 50.1283 mL
5 mM 0.4010 mL 2.0051 mL 4.0103 mL 10.0257 mL
10 mM 0.2005 mL 1.0026 mL 2.0051 mL 5.0128 mL
15 mM 0.1337 mL 0.6684 mL 1.3368 mL 3.3419 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RP-64477135239-65-5RP64477RP 64477AcyltransferaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-16437
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