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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-COMT-Entacapone
Entacapone

Chemical Structure : Entacapone

CAS No.: 130929-57-6

Entacapone

货号: PC-27365Not For Human Use, Lab Use Only.

Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor with IC50 values of 10 nM, 20 nM, and 160 nM for COMT from rat brain, erythrocytes and liver respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor with IC50 values of 10 nM, 20 nM, and 160 nM for COMT from rat brain, erythrocytes and liver 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 also is an inhibitor of FTO demethylation with IC50 of 3.5 uM, directly binds to FTO and inhibits FTO activity in vitro, reduces body weight and lowered fasting blood glucose concentrations in diet-induced obese mice.
Entacapone also is a small molecule capable of targeting Myoferlin (MYOF), blocks nuclear transport of phosphorylated STAT3 and suppresses downstream signaling, significantly impedes glioma development across experimental models.

物理化学性质&存储条件

分子量 305.29
分子式 C14H15N3O5
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(E)-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethylacrylamide

参考文献

1. E Nissinen, et al. Naunyn Schmiedebergs Arch Pharmacol. 1992 Sep;346(3):262-6.

2. Zhao P, et al. Cell Death Discov. 2026 Jul 14. doi: 10.1038/s41420-026-03254-0.

3. Shiming Peng, et al. Sci Transl Med. 2019 Apr 17;11(488):eaau7116.

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