Entacapone

製品コードS3147 バッチS314701

印刷

化学情報

Synonyms

OR-611

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₄H₁₅N₃O₅

分子量

305.29

CAS No.

130929-57-6

Solubility (25°C)*

体外

DMSO

61 mg/mL (199.81 mM)

Ethanol

2 mg/mL (6.55 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%TFA 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	3.05mg/ml (9.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 61 mg/ml clarified TFA stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Entacapone (OR-611) inhibits catechol-O-methyltransferase(COMT) with IC50 of 151 nM. Entacapone can be used for the research of Parkinson's disease. Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders.
in vitro	Entacapone inhibits catechol-O-methyltransferase(COMT) with similar IC50 in different tissues including live, duodenum, kidney and lung, but this compound is more active than tolcapone in those tissues. ^[1] This compound (< 100 μM) is a potent inhibitor of α-syn and β-amyloid (Aβ) oligomerization and fibrillogenesis, and also protects against extracellular toxicity induced by the aggregation of both proteins in PC12 cells. ^[2]
in vivo	Entacapone administration reduced body weight and lowered fasting blood glucose concentrations in diet-induced obese mice.

製品説明

Entacapone (OR-611) inhibits catechol-O-methyltransferase(COMT) with IC50 of 151 nM. Entacapone can be used for the research of Parkinson's disease. Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders.

in vitro

Entacapone inhibits catechol-O-methyltransferase(COMT) with similar IC50 in different tissues including live, duodenum, kidney and lung, but this compound is more active than tolcapone in those tissues. ^[1]

This compound (< 100 μM) is a potent inhibitor of α-syn and β-amyloid (Aβ) oligomerization and fibrillogenesis, and also protects against extracellular toxicity induced by the aggregation of both proteins in PC12 cells. ^[2]

in vivo

Entacapone administration reduced body weight and lowered fasting blood glucose concentrations in diet-induced obese mice.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	PC12 cells
	濃度	5 μM
	反応時間	72 h
	実験の流れ	Cells were treated with various concentrations of this compound for 72 h.
動物実験	動物モデル	Male C57BL/6 mice
	投薬量	600 mg/kg
	投与方法	p.o.

参考

https://pubmed.ncbi.nlm.nih.gov/9681662/
https://pubmed.ncbi.nlm.nih.gov/20150427/
https://pubmed.ncbi.nlm.nih.gov/14718680/

https://pubmed.ncbi.nlm.nih.gov/19879254/
https://pubmed.ncbi.nlm.nih.gov/30996080/

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Metabolic sensing in AgRP neurons integrates homeostatic state with dopamine signalling in the striatum [ Elife, 2022, 11e72668]	PubMed: 35018884
Glucose-sensing in AgRP neurons integrates homeostatic energy state with dopamine signalling in the striatum [ bioRxiv, 2021, 10.1101/2021.03.22.436393]	PubMed: None

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。