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Monoamine Oxidase MAO

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Monoamine Oxidase MAO Monoamine oxidases (MAO) are a family of enzymes that catalyze the oxidation of monoamines. They are found bound to the outer membrane of mitochondria in most cell types in the body. They belong to the protein family of flavin-containing amine oxidoreductases. Monoamine oxidases catalyze the oxidative deamination of monoamines. Oxygen is used to remove an amine group from a molecule, resulting in the corresponding aldehyde and ammonia. Monoamine oxidases contain the covalently bound cofactor FAD and are, thus, classified as flavoproteins. Because of the vital role that MAOs play in the inactivation of neurotransmitters, MAO dysfunction is thought to be responsible for a number of psychiatric and neurological disorders. MAO-A inhibitors act as antidepressant and antianxiety agents, whereas MAO-B inhibitors are used alone or in combination to treat Alzheimer’sand Parkinson’s diseases. www.MedChemExpress.com 1 Monoamine Oxidase Inhibitors & Modulators (S)-Rasagiline (S)-Rasagiline mesylate (TVP1022; S-PAI) Cat. No.: HY-14200 (TVP1022 (mesylate); S-PAI mesylate) Cat. No.: HY-14200A Bioactivity: (S)-Rasagiline (TVP1022) is the S-isomer of rasagiline, which Bioactivity: (S)-Rasagiline (TVP1022) mesylate is the S-isomer of is an anti-Parkinson drug, appears to have the same rasagiline, which is an anti-Parkinson drug, appears to have neuroprotective activity as the R-isomer, but is 1000-fold the same neuroprotective activity as the R-isomer, but is less active as an MAO-B inhibitor. 1000-fold less active as an MAO-B inhibitor. Purity: 99.60% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 25 mg 5 mg, 10 mg, 25 mg 2614W94 7-Hydroxy-3,4-dihydro-2(1H)-quinolinone Cat. No.: HY-101578 (3,4-Dihydro-7-hydroxy-2(1H)-quinolinone) Cat. No.: HY-W010130 Bioactivity: 2614W94 is a selective, reversible inhibitor of monoamine Bioactivity: 7-​Hydroxy-​3,​4-​dihydro-​2(1H)​-​quinolinone is a weak MAO-A inhibitor, with an IC of 183 μM, and has no effect oxidase-A with a competitive mechanism of inhibition and IC50 50 [1] of 5 nM and Ki of 1.6 nM with serotonin as substrate. on MAO-B . Purity: >98% Purity: 99.37% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 100 mg Amitraz Brofaromine (BTS-27419) Cat. No.: HY-B1111 (CGP 11305A) Cat. No.: HY-13339 Bioactivity: Amitraz is a non-systemic acaricide and insecticide, with Bioactivity: Brofaromine (CGP 11305A) is a monoamine oxidase ( MAO) alpha-adrenergic agonist activity, interaction with octopamine inhibitor with IC50 of 0.2μM for MAO-A. receptors of the central nervous system and inhibition of monoamine oxidases and prostaglandin synthesis. Purity: 98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 100 mg Clorgyline hydrochloride CX-157 Cat. No.: HY-14197A Cat. No.: HY-100178 Bioactivity: Clorgyline hydrochloride is an irreversible and selective Bioactivity: CX-157 is a reversible inhibitor of monoamine oxidase-A ( inhibitor of monoamine oxidase A (MAO-A) that is used in MAO-A) with an EC50 of 19.3ng/mL. scientific research; structurally related to Pargyline. Purity: 99.53% Purity: >98% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 10 mg, 50 mg, 100 mg Desmethoxyyangonin Eprobemide (Demethoxyyangonin; 5,6-Dehydrokavain) Cat. No.: HY-N0918 (LIS 630) Cat. No.: HY-B1413 Bioactivity: Desmethoxyyangonin is one of the six major kavalactones found Bioactivity: Eprobemide is a non-competitive reversible inhibitor of in the Piper methysticum (kava) plant; reversible inhibitor of monoamine oxidase A. MAO-B. Purity: 98.0% Purity: 99.63% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 5 mg, 10 mg, 25 mg, 50 mg 2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] GSK-LSD1 Dihydrochloride Iproniazid phosphate Cat. No.: HY-100546A Cat. No.: HY-B0886 Bioactivity: GSK-LSD1 Dihydrochloride is a potent, selective and Bioactivity: Iproniazid is a non-selective, irreversible monoamine oxidase irreversible lysine specific demethylase 1 ( LSD1) inhibitor inhibitor (MAOI) of the hydrazine class. with an IC50 of 16 nM. Purity: 98.0% Purity: 99.92% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 5 mg, 10 mg, 25 mg, 50 mg 100 mg Isatin Isocarboxazid (Indoline-2,3-dione) Cat. No.: HY-Y0265 Cat. No.: HY-13929 Bioactivity: Isatin (Indoline-2,3-dione) is a potent inhibitor of Bioactivity: Isocarboxazid is a non-selective and irreversible inhibitor of monoamine oxidase (MAO) with an IC50 of 3 μM. Also binds monoamine oxidase, with an IC50 of 4.8 μM for rat brain [1] to central benzodiazepine receptors (IC 50 against monoamine oxidase in vitro . clonazepam, 123 μM) [1]. Also acts as an antagonist of b… Purity: 97.0% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 5 mg 100 mg Lazabemide MAO-B-IN-1 (Ro 19-6327) Cat. No.: HY-14201 Cat. No.: HY-U00343 Bioactivity: Lazabemide(Ro 19-6327) is selective, reversible monoamine Bioactivity: MAO-B-IN-1 is an inhibitor of monoamine oxidase B, used oxidase B (MAO-B) inhibitor (IC50 values are 0.03 and > 100 for the research of neurological diseases. μM for MAO-B and MAO-A respectively). Purity: 99.71% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 10 mg, 50 mg MAO-IN-1 Minaprine Cat. No.: HY-U00015 Cat. No.: HY-B0884 Bioactivity: MAO-IN-1 is a monoamine oxidase B ( MAO B) inhibitor with Bioactivity: Minaprine is a reversible inhibitor of MAO-A; weakly inhibit acetylcholinesterase; an antidepressant for treatment of an IC50 of 20 nM. depression. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 100 mg Minaprine dihydrochloride Moclobemide Cat. No.: HY-B0884A (Ro111163) Cat. No.: HY-B0534 Bioactivity: Minaprine 2Hcl is a reversible inhibitor of MAO-A; weakly Bioactivity: Moclobemide(Ro111163) is a reversible monoamine oxidase inhibit acetylcholinesterase; an antidepressant for treatment inhibitor (MAOI) selective for isoform A (RIMA) used to treat of depression. major depressive disorder. Purity: 99.82% Purity: 99.45% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 50 mg, 100 mg www.MedChemExpress.com 3 Mofegiline hydrochloride Nialamide (MDL72974A) Cat. No.: HY-16677A Cat. No.: HY-B1199 Bioactivity: Mofegiline Hcl (MDL72974A) is a potent and selective Bioactivity: Nialamide is a non-selective, irreversible monoamine oxidase enzyme-activated irreversible inhibitor of MAO-B; shows marked inhibitor (MAOI) of the hydrazine class that was used as an selectivity for the B form (IC50 = 680 and 3.6 nM for MAO-A antidepressant. and MAO-B, respectively. Purity: 97.19% Purity: 95.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 100 mg Paeonol Pargyline Cat. No.: HY-N0159 Cat. No.: HY-A0091A Bioactivity: Paeonol is an active extraction from the root of Paeonia Bioactivity: Pargyline is an irreversible non-selective monoamine oxidase suffruticosa, Paeonol inhibits MAO-A and MAO-B with IC50 (MAO) inhibitor drug (IC50 for MAO-A is 11.52 nM and for MAO-B of 54.6 μM and 42.5 μM, respectively. is 8.2 nM) . Purity: 99.98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 500 mg 250 mg, 1 g Pargyline hydrochloride Phenelzine Cat. No.: HY-A0091 Cat. No.: HY-B1018 Bioactivity: Pargyline hydrochloride is an irreversible inhibitor of Bioactivity: Phenelzine is a non-selective and irreversible monoamine monoamine oxidase (MAO) that is used clinically to treat oxidase inhibitor (MAOI), used as an antidepressant and moderate hypertension. anxiolytic. Purity: 99.91% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 100 mg, 500 mg 500 mg Phenelzine sulfate Rasagiline Cat. No.: HY-B1018A (AGN1135; TVP1012) Cat. No.: HY-14605A Bioactivity: Phenelzine sulfate is a non-selective and irreversible Bioactivity: Rasagiline(AGN1135;TVP1012) is a new MAO-B inhibitor for the monoamine oxidase inhibitor (MAOI), used as an antidepressant treatment of idiopathic Parkinson's disease. Target: Monoamine and anxiolytic. Oxidase (MAO)-B Rasagiline (N-propargyl-1-(R)-aminoindan) is a novel, highly potent irreversible monoamine oxidase (MAO)-B inhibitor, anti-Parkinsonian drug. Rasagiline is effective as… Purity: 98.70% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 50 mg, 100 mg 100 mg, 500 mg, 1 g, 2 g Rasagiline 13C3 mesylate racemic Rasagiline mesylate (AGN1135 13C3 racemic; TVP1012 13C3 racemic) Cat. No.: HY-14605BS (AGN1135 (mesylate); TVP1012 (mesylate)) Cat. No.: HY-14605 Bioactivity: Rasagiline 13C3 mesylate racemic is the deuterium labeled Bioactivity: Rasagiline Mesylate is a new MAO-B inhibitor for the treatment Rasagiline, which is an irreversible inhibitor of monoamine of idiopathic Parkinson's disease. Target: Monoamine Oxidase oxidase. (MAO)-B Rasagiline (N-propargyl-1-(R)-aminoindan) is a novel, highly potent irreversible monoamine oxidase (MAO)-B inhibitor, anti-Parkinsonian drug.
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    US 2015 0011643A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2015/0011643 A1 DiLisa et al. (43) Pub. Date: Jan. 8, 2015 (54) TREATMENT OF HEART FAILURE AND (60) Provisional application No. 61/038,230, filed on Mar. ASSOCATED CONDITIONS BY 20, 2008, provisional application No. 61/155,704, ADMINISTRATION OF MONOAMINE filed on Feb. 26, 2009. OXIDASE INHIBITORS (71) Applicants:Nazareno Paolocci, Baltimore, MD Publication Classification (US); Univeristy of Padua, Padova (IT) (51) Int. Cl. (72) Inventors: Fabio DiLisa, Padova (IT): Ning Feng, A63L/38 (2006.01) Baltimore, MD (US); Nina Kaludercic, (52) U.S. Cl. Baltimore, MD (US); Nazareno CPC ..... ... A61 K31/138 (2013.01) Paolocci, Baltimore, MD (US) USPC .......................................................... S14/651 (21) Appl. No.: 14/332,234 (22) Filed: Jul. 15, 2014 (57) ABSTRACT Related U.S. Application Data Administration of monoamine oxidase inhibitors is useful in (63) Continuation of application No. 12/407,739, filed on the prevention and treatment of heart failure and incipient Mar. 19, 2009, now abandoned. heart failure. Patent Application Publication Jan. 8, 2015 Sheet 1 of 2 US 201S/0011643 A1 Figure 1 Sial 8. Sws-L) Cleaved Š Caspase-3 ) Figure . Prevention of caspase-3 productief) fron cardiomyocytes Lapoi) reatment with clorgyi Be. Patent Application Publication Jan. 8, 2015 Sheet 2 of 2 US 201S/0011643 A1 Figure 2 8:38:8 ::::::::8: US 2015/0011643 A1 Jan. 8, 2015 TREATMENT OF HEART FAILURE AND in the art is a variety of MAO inhibitors and their pharmaceu ASSOCATED CONDITIONS BY tically acceptable compositions for administration, in accor ADMINISTRATION OF MONOAMINE dance with the present invention, to mammals including, but OXIDASE INHIBITORS not limited to, humans.
  • Pharmaceutical Appendix to the Tariff Schedule 2

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    Harmonized Tariff Schedule of the United States (2007) (Rev. 2) Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE HARMONIZED TARIFF SCHEDULE Harmonized Tariff Schedule of the United States (2007) (Rev. 2) Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE TARIFF SCHEDULE 2 Table 1. This table enumerates products described by International Non-proprietary Names (INN) which shall be entered free of duty under general note 13 to the tariff schedule. The Chemical Abstracts Service (CAS) registry numbers also set forth in this table are included to assist in the identification of the products concerned. For purposes of the tariff schedule, any references to a product enumerated in this table includes such product by whatever name known. ABACAVIR 136470-78-5 ACIDUM LIDADRONICUM 63132-38-7 ABAFUNGIN 129639-79-8 ACIDUM SALCAPROZICUM 183990-46-7 ABAMECTIN 65195-55-3 ACIDUM SALCLOBUZICUM 387825-03-8 ABANOQUIL 90402-40-7 ACIFRAN 72420-38-3 ABAPERIDONUM 183849-43-6 ACIPIMOX 51037-30-0 ABARELIX 183552-38-7 ACITAZANOLAST 114607-46-4 ABATACEPTUM 332348-12-6 ACITEMATE 101197-99-3 ABCIXIMAB 143653-53-6 ACITRETIN 55079-83-9 ABECARNIL 111841-85-1 ACIVICIN 42228-92-2 ABETIMUSUM 167362-48-3 ACLANTATE 39633-62-0 ABIRATERONE 154229-19-3 ACLARUBICIN 57576-44-0 ABITESARTAN 137882-98-5 ACLATONIUM NAPADISILATE 55077-30-0 ABLUKAST 96566-25-5 ACODAZOLE 79152-85-5 ABRINEURINUM 178535-93-8 ACOLBIFENUM 182167-02-8 ABUNIDAZOLE 91017-58-2 ACONIAZIDE 13410-86-1 ACADESINE 2627-69-2 ACOTIAMIDUM 185106-16-5 ACAMPROSATE 77337-76-9