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20

抑制剂 & 化合物

7

天然产物

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Cat. No. Product Name Target Signaling Pathways
T16398 Opicapone

BIA 9-1067

Transferase Metabolism
Opicapone (BIA 9-1067) 是第三代儿茶酚-O-甲基转移酶 (COMT)抑制剂,能够降低细胞 ATP 含量,IC50=98 μM。它有用于帕金森病和运动波动的研究潜力。
T60658 hMAO-B/MB-COMT-IN-2

hMAO-B/MB-COMT-IN-2 是MAO-B/MB-COMT 的双重抑制剂,对hMAO-B 和MB-COMT 的IC50值分别为 4.27 μM 和 2.69 μM。hMAO-B/MB-COMT-IN-2 保护细胞免受氧化损伤,可用于神经退行性疾病,如帕金森病 (PD) 等的研究。
T7831 Nitecapone

Others; Transferase Metabolism; Others
Nitecapone 是一个具有口服活性的、短效的儿茶酚-O-甲基转移酶(COMT)的抑制剂。它具有胃肠道保护和抗氧化活性,能够清除活性氧和一氧化氮,防止脂质过氧化。
T60489 hMAO-B/MB-COMT-IN-1

hMAO-B/MB-COMT-IN-1 是 MAO-B/MB-COMT 的双重抑制剂,对 hMAO-B 的IC50值为 2.5 μM,对MB-COMT 的IC50值为 3.84 μM。hMAO-B/MB-COMT-IN-1 能保护细胞免受氧化损伤,可用于神经退行性疾病,如帕金森病 (PD)等的研究。
T2216 Entacapone

OR-611,恩他卡朋

Transferase Metabolism
Entacapone (OR-611) 是可逆的、具有口服活性的、外周作用的儿茶酚-O-甲基转移酶抑制剂。它对大鼠脑、红细胞和肝脏 COMT 有抑制作用。它对 COMT 的选择性优于其他儿茶酚胺代谢酶。它抑制 FTO 去甲基化活性,可用于研究代谢紊乱。它可用于研究帕金森病。
T6708 Tolcapone

Tasmar,Ro 40-7592,托卡朋

Apoptosis; Beta Amyloid; Transferase Apoptosis; Metabolism; Neuroscience
Tolcapone (Ro 40-7592) 是一种选择性,具有口服活性的外周和中枢COMT 抑制剂,在肝脏中对 COMT 的IC50为 773 nM。它还是一种 α-syn 和 Aβ42 寡聚和原纤维形成的有效抑制剂,可诱导氧化应激导致神经母细胞瘤细胞凋亡和抑制肿瘤生长。
T4983 Isoetharine mesylate salt

Isoetarine mesilate,异丙肾上腺素甲磺酸盐

Others; Adrenergic Receptor GPCR/G Protein; Neuroscience; Others
Isoetharine mesylate salt (Isoetarine mesilate) 是一种 β-肾上腺素能受体激动剂。它还是能够上调 CYP450 表达的孕烷 X 受体(PXR) 激活剂。
T23109 3,5-Dinitrocatechol

Transferase Metabolism
3,5-Dinitrocatechol 是儿茶酚-O-甲基转移酶的有效抑制剂,IC50为 12 nM。它可用于制备钼 (VI)- 3,5-Dinitrocatechol 配合物。
T24030 Entacapone acid

AG1290,AG 1290,AG-1290,恩他卡朋酸

Transferase Metabolism
Entacapone acid (AG 1290) 是一种选择性和可逆的儿茶酚-O-甲基转移酶 (COMT) 抑制剂。
T11207 Entacapone sodium salt

Others Others
Entacapone sodium salt inhibits catechol-O-methyltransferase(COMT) with similar IC50 in different tissues including live, duodenum, kidney and lung, but entacapone is more active than tolcapone in those tissues. Entacapone (< 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.Entacapone sodium salt is a specific, potent, peripherally acting catech...
T75389 Catechol O-methyltransferase

Catechol O-methyltransferase (COMT) 在镁的作用下,通过将 S-腺苷甲硫氨酸的甲基转移至多巴胺的羟基,生成3-甲氧基酪胺,从而参与调节大脑中肾上腺素、去甲肾上腺素和多巴胺的水平。存在于组织中的Catechol O-methyltransferase有两种形态:可溶性形式(S-COMT)和膜结合形式(MB-COMT)。
T26106 Ro 41-0960

Ro-41-0960,Ro41-0960

Ro 41-0960 is used as a reversible and orally-active COMT-inhibitor.
T27162 DHMPA

DHMPA is an inhibitor of catechol-O-methyltransferase (COMT), it also reduces tissue norepinephrine and blood pressure.
T13181 Tolcapone D7

Ro 40-7592 D7

Transferase Metabolism
Tolcapone D7 is a deuterium-labeled Tolcapone. Tolcapone is a selective and orally active inhibitor of COMT.
T16279 Nebicapone

BIA 3-202

Others Others
Nebicapone is a reversible catechol-O-methyltransferase (COMT) inhibitor and is mainly metabolized by glucuronidation. Nebicapone is mainly peripherally acting inhibitor that decreases the biotransformation of L-DOPA to 3-O-methyl-DOPA by inhibition of CO
T10119 3-O-Methyltolcapone

Ro 40-7591

Transferase Metabolism
3-O-Methyltolcapone (Ro 40-7591) is a metabolite of Tolcapone which is a potent COMT inhibitor. Tolcapone crosses the blood-brain barrier and can be used for treatment of Parkinson's disease.
T36207 Methylspinazarin

Methylspinazarin is a naphthoquinone bacterial metabolite that has been found in Streptomyces and is an inhibitor of catechol O-methyltransferase (COMT; IC50 = 0.8 μg/ml).1 It is selective for COMT over tyrosine hydroxylase, DOPA decarboxylase, and dopamine-β-hydroxylase at 100 μg/ml. Methylspinazarin decreases blood pressure in spontaneously hypertensive rats when administered at a dose of 50 mg/kg. |1. Chimura, H., Sawa, T., Takita, T., et al. Methylspinazarin and dihydromethylspinazarin, gate...
T70608 cis-Entacapone

cis-Entacapone is a metabolite of the catechol-O-methyltransferase (COMT) inhibitor entacapone. It is also a potential impurity found in commercial preparations of entacapone and a degradant of entacapone formed by UV light exposure.
T29029 U-0521

U-0521, an inhibitor of catechol-O-methyltransferase (COMT), enhances the availability and utilization of levodopa in the brain.
T10118 3-O-Methyltolcapone D7

Ro 40-7591 D7

Transferase Metabolism
3-O-Methyltolcapone D7 (Ro 40-7591 D7) is a deuterium labeled 3-O-Methyltolcapone. 3-O-Methyltolcapone (Ro 40-7591) is a metabolite of Tolcapone which is a potent COMT inhibitor. Tolcapone crosses the blood-brain barrier and can be used for treatment of P

化合物

Opicapone
Cat.No: T16398
Synonym: BIA 9-1067
Target: Transferase
hMAO-B/MB-COMT-IN-2
Cat.No: T60658
Synonym:
Target:
Nitecapone
Cat.No: T7831
Synonym:
Target: Others, Transferase
hMAO-B/MB-COMT-IN-1
Cat.No: T60489
Synonym:
Target:
Entacapone
Cat.No: T2216
Synonym: OR-611,恩他卡朋
Target: Transferase
Tolcapone
Cat.No: T6708
Synonym: Tasmar,Ro 40-7592,托卡朋
Target: Apoptosis, Beta Amyloid, Transferase
Isoetharine mesylate salt
Cat.No: T4983
Synonym: Isoetarine mesilate,异丙肾上腺素甲磺酸盐
Target: Others, Adrenergic Receptor
3,5-Dinitrocatechol
Cat.No: T23109
Synonym:
Target: Transferase
Entacapone acid
Cat.No: T24030
Synonym: AG1290,AG 1290,AG-1290,恩他卡朋酸
Target: Transferase
Entacapone sodium salt
Cat.No: T11207
Synonym:
Target: Others
Catechol O-methyltransferase
Cat.No: T75389
Synonym:
Target:
Ro 41-0960
Cat.No: T26106
Synonym: Ro-41-0960,Ro41-0960
Target:
DHMPA
Cat.No: T27162
Synonym:
Target:
Tolcapone D7
Cat.No: T13181
Synonym: Ro 40-7592 D7
Target: Transferase
Nebicapone
Cat.No: T16279
Synonym: BIA 3-202
Target: Others
3-O-Methyltolcapone
Cat.No: T10119
Synonym: Ro 40-7591
Target: Transferase
Methylspinazarin
Cat.No: T36207
Synonym:
Target:
cis-Entacapone
Cat.No: T70608
Synonym:
Target:
U-0521
Cat.No: T29029
Synonym:
Target:
3-O-Methyltolcapone D7
Cat.No: T10118
Synonym: Ro 40-7591 D7
Target: Transferase
Cat. No. Product Name Target Signaling Pathways
T0525 Flopropione

夫洛丙酮,Phloropropiophenone

5-HT Receptor; Transferase GPCR/G Protein; Metabolism; Neuroscience
Flopropione (Phloropropiophenone) 是一种解痉剂,用作 5-HT1A 受体拮抗剂,也是儿茶酚-O-甲基转移酶抑制剂。
T2765 Rosmarinic acid

Labiatenic acid,迷迭香酸,Rosemary acid

Apoptosis; IκB/IKK; MAO; Endogenous Metabolite; Transferase; Monoamine Oxidase Apoptosis; Metabolism; Neuroscience; NF-κB
Rosmarinic acid (Labiatenic acid) 广泛存在植物中,具有抗氧化、抗炎和抗菌活性。它抑制 MAO-A,MAO-B 和 COMT,IC50分别为 50.1,184.6 和 26.7 μM。
TN2437 Serotonin

5-羟基色胺,5-hydroxytryptamine,血清素,五羟色胺,5-HT

Others; 5-HT Receptor; Endogenous Metabolite; Transferase GPCR/G Protein; Metabolism; Neuroscience; Others
Serotonin (5-hydroxytryptamine) 是 CNS 中的单胺神经递质和内源性5-HT 受体激动剂。它也是儿茶酚 O-甲基转移酶(COMT) 的抑制剂,Ki 值为 44 μM。
T2209 Serotonin hydrochloride

5-HT hydrochloride,5-羟基色胺盐酸盐,5-HT HCl,Serotonin HCl,5-Hydroxytryptamine hydrochloride

5-HT Receptor; Endogenous Metabolite; Transferase GPCR/G Protein; Metabolism; Neuroscience
Serotonin hydrochloride (Serotonin HCl) 是一种内源性 5-HT 受体激动剂、CNS 中的单胺神经递质和儿茶酚 O-甲基转移酶 (COMT) 抑制剂,Ki 值为 44 μM。
TN7057 rosmarinate acid

(R)-rosmarinic acid,rosmarinic acid,迷迭香素,Rosemary acid

MAO; Endogenous Metabolite; Transferase Metabolism; Neuroscience
Rosmarinate acid(Rosemary acid) 抑制 MAO-A、MAO-B 和 COMT 酶,IC50 分别为 50.1、184.6 和 26.7 μM。
T9455 4-hydroxyestrone-4-methyl ether

4-Methoxy Estrone,4-甲氧基雌酮

Estrogen Receptor/ERR; Endogenous Metabolite Endocrinology/Hormones; Metabolism
4-hydroxyestrone-4-methyl ether (4-Methoxy Estrone) 是由COMT 催化的4-OHE1的甲基化反应。
T39198 5-Hydroxyferulic acid

5-Hydroxyferulic acid is an important hydroxycinnamic acid compound and a metabolite in the phenylpropanoid pathway. It acts as a precursor for the biosynthesis of sinapic acid and functions as a non-esterified substrate for COMT.

天然产物

Flopropione
Cat.No: T0525
Synonym: 夫洛丙酮,Phloropropiophenone
Target: 5-HT Receptor, Transferase
Rosmarinic acid
Cat.No: T2765
Synonym: Labiatenic acid,迷迭香酸,Rosemary acid
Target: Apoptosis, IκB/IKK, MAO, Endogenous Metabolite, Transferase, Monoamine Oxidase
Serotonin
Cat.No: TN2437
Synonym: 5-羟基色胺,5-hydroxytryptamine,血清素,五羟色胺,5-HT
Target: Others, 5-HT Receptor, Endogenous Metabolite, Transferase
Serotonin hydrochloride
Cat.No: T2209
Synonym: 5-HT hydrochloride,5-羟基色胺盐酸盐,5-HT HCl,Serotonin HCl,5-Hydroxytryptamine hydrochloride
Target: 5-HT Receptor, Endogenous Metabolite, Transferase
rosmarinate acid
Cat.No: TN7057
Synonym: (R)-rosmarinic acid,rosmarinic acid,迷迭香素,Rosemary acid
Target: MAO, Endogenous Metabolite, Transferase
4-hydroxyestrone-4-methyl ether
Cat.No: T9455
Synonym: 4-Methoxy Estrone,4-甲氧基雌酮
Target: Estrogen Receptor/ERR, Endogenous Metabolite
5-Hydroxyferulic acid
Cat.No: T39198
Synonym:
Target:
TargetMol Loading
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