COMT-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/COMT.html COMTCatechol-O-methyltransferaseCatechol O-methyltransferase (COMT) is the enzyme responsible for the O-methylation of endogenous neurotransmitters and ofxenobiotic substances and hormones incorporating catecholic structures. COMT is present in mammal

2、s as soluble (S-COMT) andmembrane-bound (MB-COMT) forms. S-COMT is the predominant form of COMT in the peripheral organs and MB-COMT is moreabundant in the Central Nervous System.Physiological substrates of COMT include L-dopa, catecholamines (dopamine, norepinephrine, and epinephrine), their hydrox

3、ylatedmetabolites, catecholestrogens, ascorbic acid, and dihydroxyindolic intermediates of melanin. Specifically, COMT plays a critical rolein the inactivation and metabolism of dopamine and other catechol compounds. The enzyme reduces a catechol molecule in orderto prevent genomic damage through DN

4、A adduct formation or via oxygen radicals produced from the redox cycling of catechols.COMT is a druggable biological target for the treatment of various central and peripheral nervous system disorders, includingParkinsons disease, depression, schizophrenia, and other dopamine deficiency-related dis

5、eases.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/COMT.html COMT HYPERLINK https:/www.MedChemE/Targets/COMT.html HYPERLINK https:/www.MedChemE/Targets/COMT.html Inhibitors HYPERLINK https:/www.MedChemE/e-entacapone-d10.html (E)-Entacapone-d10Cat. No.: HY-14280S2 HYPERLINK https:/www.MedChem

6、E/3-o-methyltolcapone.html 3-O-Methyltolcapone(Ro 40-7591) Cat. No.: HY-100642Entacapone-d10 is the deuterium labeledEntacapone. Entacapone is a potent, reversible,peripherally acting and orally activecatechol-O-methyltransferase (COMT)inhibitor.3-O-Methyltolcapone (Ro 40-7591) is a metaboliteof Tol

7、capone. Tolcapone is an orally active,reversible, selective and potent COMTinhibitor. Tolcapone crosses the blood-brainbarrier, and can be used for treatment ofParkinsons disease.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1

8、 mg, 5 mg HYPERLINK https:/www.MedChemE/3-o-methyltolcapone-d7.html 3-O-Methyltolcapone HYPERLINK https:/www.MedChemE/3-o-methyltolcapone-d7.html HYPERLINK https:/www.MedChemE/3-o-methyltolcapone-d7.html D7(Ro 40-7591 D7) Cat. No.: HY-100642S HYPERLINK https:/www.MedChemE/3-o-methyl-tolcapone-d4.htm

9、l 3-O-Methyltolcapone-d4(Ro 40-7591-d4) Cat. No.: HY-100642S13-O-Methyltolcapone D7 (Ro 40-7591 D7) is adeuterium labeled 3-O-Methyltolcapone.3-O-Methyltolcapone is a metabolite of Tolcapone.Tolcapone is an orally active, reversible,selective and potent COMT inhibitor.3-O-Methyltolcapone-d4 (Ro 40-7

10、591-d4) is thedeuterium labeled 3-O-Methyltolcapone.3-O-Methyltolcapone (Ro 40-7591) is a metaboliteof Tolcapone. Tolcapone is an orally active,reversible, selective and potent COMTinhibitor.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development Rep

11、ortedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/5-hydroxyferulic-acid.html 5-Hydroxyferulic HYPERLINK https:/www.MedChemE/5-hydroxyferulic-acid.html HYPERLINK https:/www.MedChemE/5-hydroxyferulic-acid.html acid HYPERLINK https:/www.MedChemE/5-hydroxyferulic-acid.html HYPERLINK https:/www.MedChem

12、E/entacapone.html EntacaponeCat. No.: HY-133068 Cat. No.: HY-142805-Hydroxyferulic acid is a hydroxycinnamic acidand is a metabolite of the phenylpropanoidpathway. 5-Hydroxyferulic acid is a precursor inthe biosynthesis of sinapic acid and is also aCOMT non-esterifed substrate.Entacapone is a potent

13、, reversible, peripherallyacting and orally activecatechol-O-methyltransferase (COMT)inhibitor. Entacapone inhibits COMT from ratbrain, erythrocytes and liver with IC values of5010 nM, 20 nM, and 160 nM, respectively.Purity: 99.80%Clinical Data: No Development ReportedSize: 5 mg, 10 mgPurity: 99.97%

14、Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/entacapone-sodium-salt.html Entacapone HYPERLINK https:/www.MedChemE/entacapone-sodium-salt.html HYPERLINK https:/www.MedChemE/entacapone-sodium-salt.html sodium HYPERLINK https:/www.MedChemE/entacapone-sodiu

15、m-salt.html HYPERLINK https:/www.MedChemE/entacapone-sodium-salt.html salt HYPERLINK https:/www.MedChemE/entacapone-sodium-salt.html HYPERLINK https:/www.MedChemE/entacapone-d10.html Entacapone-d10Cat. No.: HY-14280A Cat. No.: HY-14280SEntacapone sodium salt is a potent, reversible,peripherally acti

16、ng and orally activecatechol-O-methyltransferase (COMT)inhibitor.Entacapone-d10 is the deuterium labeledEntacapone. Entacapone is a potent, reversible,peripherally acting and orally activecatechol-O-methyltransferase (COMT)inhibitor.Purity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mgPurity: 98%Clinic

17、al Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Flopropione.html Flopropione HYPERLINK https:/www.MedChemE/Flopropione.html HYPERLINK https:/www.MedChemE/nebicapone.html NebicaponeCat. No.: HY-100562(BIA 3-202) Cat. No.: HY-106405Flopropione is a 5-HT receptor antagoni

18、st andalso a catechol-o-methyltransferase (COMT)inhibitor. Flopropione also as an antispasmodicagent.Nebicapone (BIA 3-202), a reversiblecatechol-O-methyltransferase (COMT)inhibitor, is mainly metabolized byglucuronidation.Purity: 98.93%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mgPurity: 98%Clini

19、cal Data: Phase 2Size: 1 mg, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/nitecapone.html Nitecapone(OR-462) Cat. No.: HY-106842 HYPERLINK https:/www.MedChemE/opicapone.html Opicapone(BIA 9-1067) Cat. No.: HY-14896Nitecapone (OR-462) is an orally activ

20、e andshort-acting catechol-O-methyltransferase(COMT) inhibitor with gastroprotective andantioxidant properties. Nitecapone (OR-462)scavenges reactive oxygen and nitric radicals andprevents lipid peroxidation.Purity: 99.32%Clinical Data: No Development ReportedSize: 5 mg, 10 mgOpicapone (BIA 9-1067)

21、is a potentthird-generation catechol-O-methyltransferase(COMT) inhibitor for the research ofParkinsons disease and motor fluctuations.Opicapone decreases the ATP content of the cellswith an IC of 98 M.50Purity: 99.64%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLIN

22、K https:/www.MedChemE/ro-41-0960.html Ro HYPERLINK https:/www.MedChemE/ro-41-0960.html HYPERLINK https:/www.MedChemE/ro-41-0960.html 41-0960Cat. No.: HY-125339 HYPERLINK https:/www.MedChemE/Rosmarinic-acid.html Rosmarinic HYPERLINK https:/www.MedChemE/Rosmarinic-acid.html HYPERLINK https:/www.MedChe

23、mE/Rosmarinic-acid.html acid(Labiatenic acid) Cat. No.: HY-N0529Ro 41-0960 is a selectivecatechol-O-methyltransferase(COMT) inhibitor.Rosmarinic acid is a widespread phenolic estercompound in the plants. Rosmarinic acid inhibitsMAO-A, MAO-B and COMT enzymes with IC s50of 50.1, 184.6 and 26.7 M, resp

24、ectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.70%Clinical Data: Phase 4Size: 10 mM 1 mL, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/tolcapone.html Tolcapone(Ro 40-7592) Cat. No.: HY-17406 HYPERLINK https:/www.MedChemE/tolcapone-d7.html Tolcapone HYPERLINK https:/www.MedChemE/tolcapone-d7.html HYPERLINK https:/www.MedChemE/tolcapone-d7.html D7(Ro 40-7592 D7) Cat. No.: HY-17406STolcapone (Ro 40-7592) is a selective, orallyactive and powerful