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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 |
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. |