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

RP-64477 是膽固醇酯化酶酰基輔酶 A：膽固醇 O-?；D(zhuǎn)移酶 (ACAT) 的有效抑制劑。

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RP-64477 Chemical Structure

RP-64477 Chemical Structure

CAS No. : 135239-65-5

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規(guī)格 價格 是否有貨 數(shù)量
1 mg ￥741
In-stock
5 mg ￥1800
In-stock
10 mg ￥2880
In-stock
25 mg ￥5180
In-stock
50 mg 現(xiàn)貨 詢價
100 mg 現(xiàn)貨 詢價
200 mg   詢價  
500 mg   詢價  

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Customer Review

查看 Acyltransferase 亞型特異性產(chǎn)品:

  • 生物活性

  • 實驗參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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]
體外研究
(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.
體內(nèi)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 號
性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實驗： 

DMSO 中的溶解度 : 8.33 mg/mL (16.70 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)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
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.62%

參考文獻(xiàn)
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.
參考文獻(xiàn)

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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.

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Inquiry Information

產(chǎn)品名稱：
RP-64477
目錄號：
HY-16437
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