Entacapone 是一种有效的、可逆的、外周作用和具有口

Entacapone  (Synonyms: 恩他卡朋)

Entacapone 是一种有效的、可逆的、外周作用和具有口服活性儿茶酚-O-甲基转移酶 (COMT) 抑制剂。Entacapone 对大鼠脑、红细胞和肝脏 COMT 有抑制作用，IC₅₀ 值分别为 10 nM、20 nM和160 nM。Entacapone 对 COMT 的选择性优于其他儿茶酚胺代谢酶，包括MAO-A、MAO-B、酚磺基转移酶 M (PST-M) 和 PST-P (IC₅₀s >50 µM)。Entacapone 可用于帕金森病的研究。Entacapone 抑制 FTO 去甲基化活性，IC₅₀ 是 3.5 μM，可用于研究代谢紊乱。

美国medchemexpress（MCE)浙江省一级代理:杭州昊鑫生物科技股份有限公司
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生物活性    
Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone can be used for the research of Parkinson's disease[1]. Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders[2].

IC50 & Target    
IC50: 10 nM (rat brain COMT); 20 nM (rat erythrocyte COMT); 160 nM (rat liver COMT)[1]

体外研究(In Vitro)    
Entacapone (50 μM, 48 hours) enhances the amount of m6A on mRNA in Hep-G2 cells. It does not show any inhibitory effect on the enzymatic activity of the RNA m6A demethylase AlkB homolog 5 (ALKBH5) or the ten-eleven translocation methylcytosine dioxygenase 1 (TET1), nor does it alter the DNA methylation or histone methylation patterns in entacapone-treated Hep-G2 cells[2].

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

体内研究(In Vivo)    
Entacapone (oral administration; 600 mg/kg per day; 3-9 weeks) results in a dose-response effect dose-response effect. After 3 weeks, mouse body weight are decreased by 10.1% compared to controls, and shows similar food intake??fat mass and fat mass ratio reduced after entacapone treatment. Entacapone also increases the energy expenditure of mice: reductions in total cholesterol (17.6%), low-density lipoprotein cholesterol (31.0%), and triglycerides (10.2%) in mice[2].

分子量    
305.29

性状    
Solid

Formula    
C14H15N3O5

CAS 号    
130929-57-6

中文名称    
恩他卡朋

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    1 year
-20°C    6 months
溶解性数据    
In Vitro: 
DMSO : 33.33 mg/mL (109.17 mM; Need ultrasonic)

H2O : 2 mg/mL (6.55 mM; ultrasonic and adjust pH to 10 with NaOH)

配制储备液    
浓度溶剂体积质量    1 mg    5 mg    10 mg
1 mM    3.2756 mL    16.3779 mL    32.7557 mL
5 mM    0.6551 mL    3.2756 mL    6.5511 mL
10 mM    0.3276 mL    1.6378 mL    3.2756 mL
*
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℃, 1 years; -20℃, 6 months。-80℃ 储存时，请在 1 年内使用， -20℃ 储存时，请在 6 个月 内使用。

In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.
请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

Solubility: ≥ 2.5 mg/mL (8.19 mM); Clear solution

2.
请依序添加每种溶剂： 10% DMSO    90% corn oil

Solubility: 2.5 mg/mL (8.19 mM); Clear solution; Need warming

3.
请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (6.81 mM); Clear solution

4.
请依序添加每种溶剂： PBS

Solubility: 1 mg/mL (3.28 mM); Clear solution; Need ultrasonic and warming and heat to 60°C


 

参考文献	[1]. E Nissinen, et al. Biochemical and pharmacological properties of a peripherally acting catechol-O-methyltransferase inhibitor entacapone. Naunyn Schmiedebergs Arch Pharmacol. 1992 Sep;346(3):262-6.  [Content Brief] [2]. Shiming Peng, et al. Identification of entacapone as a chemical inhibitor of FTO mediating metabolic regulation through FOXO1. Sci Transl Med  [Content Brief]