Entacapone is a potent, reversible, peripherally acting and orally activecatechol-O-methyltransferase (COMT)inhibitor. Entacapone inhibitsCOMTfrom rat brain, erythrocytes and liver withIC₅₀values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective forCOMTover other catecholamine metabolizing enzymes, includingMAO-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 ofFTO demethylationwith anIC₅₀of 3.5 μM, can be used for the research of metabolic disorders^[2].

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

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].

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].

305.29

Solid

C₁₄H₁₅N₃O₅

130929-57-6

恩他卡朋

Room temperature in continental US; may vary elsewhere.

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)

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

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

  此方案可获得 ≥ 2.5 mg/mL (8.19 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 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

  此方案可获得 2.5 mg/mL (8.19 mM) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• 3.

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

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

  此方案可获得 ≥ 2.08 mg/mL (6.81 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 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℃