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Monoamine oxidase (EC 1.4.3.4) is an enzyme composed of different polypeptides. Monoamine oxidation catalyzes the oxidative deamination of various biological amines in brain and peripheral tissues by producing hydrogen peroxide. Monoamine oxidase plays an important role in maintaining the regulation of synaptic transmission, emotional behavior and other brain functions .
Monoamine oxidase/Aromatase-IN-1 (compound 2q) is a highly potent monoamine oxidase (MAO) and aromatase dual inhibitor with IC50s of 39 nM and 31 nM for MAO-B and aromatase, respectively. Monoamine oxidase/Aromatase-IN-1 can be used for researching neurological disorder and breast cancer .
Monoamine Oxidase B inhibitor 1 is a potent, reversible, orally active and selective monoamine oxidase B (MAO-B) inhibitor with an IC50 of 0.02 nM. Monoamine Oxidase B inhibitor 1 has antioxidant and anti-neuroinflammatory activities. Monoamine Oxidase B inhibitor 1 can across the blood-brain barrier (BBB), and can be used for Parkinson’s disease study .
Monoamine Oxidase B inhibitor 2 is a potent, reversible, orally active and selective monoamine oxidase B (MAO-B) inhibitor with an IC50 of 1.33 nM. Monoamine Oxidase B inhibitor 2 has antioxidant and anti-neuroinflammatory activities. Monoamine Oxidase B inhibitor 2 can across the blood-brain barrier (BBB), and can be used for Parkinson’s disease study .
Lafadofensine D-(-)-Mandelic acid is the monoamines reuptake inhibitor. Lafadofensine D-(-)-Mandelic acid has sufficient effects after short-term administration .
Lafadofensine is the monoamines reuptake inhibitor. Lafadofensine has th sufficient effects after short-term administration (extracted from patent WO2006121218A1, compound 1) .
1,4-Naphthoquinone is a potential pharmacophore for inhibition of both MAO (monoamine oxidase) and DNA topoisomerase activities, this latter associated with antitumor activity .
MAO-B-IN-17 is a selective monoamine oxidase B (MAO-B) inhibitor with the IC50 value of 5.08 μM. MAO-B-IN-17 can be used in Parkinson’s disease research .
Glicoricone, a phenolic compound, is isolated from a species of licorice. Glicoricone is an inhibitor of monoamine oxidase (MAO), with an IC50 of 140 μM. Glicoricone binds to estrogen receptor (ER) and shows estrogen antagonist activity .
Moclobemide N-Oxide (Ro 12-5637) is N-oxide metabolite of Moclobemide. Moclobemide N-Oxide retains certain MAO-A (monoamine oxidase) inhibitory activity, but is generally present in low concentrations. Moclobemide N-Oxide can be detected by UV absorption at 240 nm .
Methyl citrate is a Monoamine oxidase B (MAO-B) inhibitor (IC50=0.23 mM). Methyl citrate is isolated from the fruits of Opuntia ficus-indica var. saboten Makino .
Tranylcypromine (SKF 385) hydrochloride (GMP) is Tranylcypromine (HY-17447) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Tranylcypromine hydrochloride is a potent monoamine oxidase (MAO) inhibitor .
MAO-IN-5 (Compound ZINC000016952895) is a monoamine oxidase (MAO) inhibitor. According to the prediction of Swiss ADME, MAO-IN-5 can inhibit the CYP enzyme family, has blood-brain barrier (BBB) permeability, and has a high gastrointestinal absorption rate. MAO-IN-5 can be used in the study of neurological diseases .
Melitracen hydrochloride is an orally active biphasic antidepressant and antianxiety agent. Melitracen hydrochloride can inhibit the uptake of Norepinephrine and 5-HT (serotonin) through the presynaptic membrane inducing the increase of monoamine transmitters in synaptic space .
Contezolid acefosamil sodium (MRX-4), a new and orally active oxazolidinone, is an antibiotic in study for complicated skin and soft tissue infections (cSSTI) caused by resistant Gram-positive bacteria. Contezolid acefosamil sodium (MRX-4) markedly reduces potential for myelosuppression and monoamine oxidase inhibition (MAOI) .
MAO-B-IN-16 is a selective monoamine oxidase B (MAO-B) inhibitor, with an IC50 of 1.55 µM. MAO-B-IN-16 can be used in the study of central nervous disorders, such as parkinson's disease .
Lazabemide (Ro 19-6327) is a selective, reversible inhibitor of monoamine oxidase B (MAO-B) (IC50=0.03 μM) but less active for MAO-A (IC50>100 μM). Lazabemide inhibits monoamine uptake at high concentrations, the IC50 values are 86 μM, 123 μM and >500 μM for noradrenalin, serotonin and dopamine uptake, respectively. Lazabemide can be used for the research of parkinson and alzheimer′s disease .
Lazabemide hydrochloride (Ro 19-6327 hydrochloride) is a selective, reversible inhibitor of monoamine oxidase B (MAO-B) (IC50=0.03 μM) but less active for MAO-A (IC50>100 μM). Lazabemide inhibits monoamine uptake at high concentrations, the IC50 values are 86 μM, 123 μM and >500 μM for noradrenalin, serotonin and dopamine uptake, respectively. Lazabemide can be used for the research of parkinson and alzheimer′s disease .
FFN246 is a fluorescent, dual substrate of serotonin transporter (SERT) probe and vesicular monoamine transporter 2 (VMAT2) with excitation and emission spectra 392/427 nm. FFN246 can be used for labeling serotonergic neurons in mouse brain tissue through SERT-dependent accumulation .
Obtusin, isolated from Cassia obtusifolia Linn seed, is a highly selective and competitive human monoamine oxidase-A (hMAO-A) inhibitor with an IC50 of 11.12 μM and a Ki of 6.15 μM. Obtusin plays a preventive role in neurodegenerative diseases, especially anxiety and depression .
Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A .Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
MAO-B-IN-27 (Compound 12c) is a monoamine oxidase B (MAO-B) inhibitor. MAO-B-IN-27 has potent and selective MAO-B inhibitory effect for hMAO-B with an IC50 values of 8.9 nM. MAO-B-IN-27 can be used for the research of parkinson's disease (PD) .
J147 is an exceptionally potent, orally active, neuroprotective agent for cognitive enhancement. J147 can pass the blood brain barrier (BBB). J147 can inhibit monoamine oxidase B (MAO B) and the dopamine transporter. J147 plays an impotant role in Alzheimer’s disease (AD) .
OG-L002 is a potent and highly selective LSD1 inhibitor with an IC50 of 0.02 μM. OG-L002 is a potent monoamine oxidases (MAO) inhibitor with IC50s of 1.38 μM and 0.72 μM for MAO-A and MAO-B, respectively. OG-L002 potently inhibits the expression of HSV IE genes .
1-Methyl-2-nonyl-4(1H)-quinolone, a quinolone alkaloid, is a potent and selective MAO-B (monoamine oxidase) inhibitor. 1-Methyl-2-nonyl-4(1H)-quinolone exhibites inhibitory activity on leukotriene biosynthesis, with an IC50 of 12.1 μM .
Indatraline hydrochloride (Lu 19-005) is a non-selective monoamine transporter inhibitor that blocks the reuptake of neurotransmitters (dopamine, serotonin, and norepinephrine). Indatraline hydrochloride can be used for the research of antidepressive. Indatraline hydrochloride induces autophagy while simultaneously inhibiting cell proliferation. Indatraline hydrochloride may also serve to direct the development of new agents for autophagy-related diseases such as atherosclerosis or restenosis .
Tesofensine (NS-2330) is a triple monoamine reuptake inhibitor inducing a potent inhibition of the re-uptake process in the synaptic cleft of the neurotransmitters dopamine (DA; IC50=6.5 nM), norepinephrine (NE;IC50=1.7 nM), and serotonin (5-HT;IC50=11 nM), and with potentials as an anti-obesity agent . Tesofensine is a CNS acting anti-obesity agent .
(E)-8-(3-Chlorostyryl)caffeine is a selective adenosine A2A receptor antagonist. (E)-8-(3-Chlorostyryl)caffeine inhibits monoamine oxidase B (MAO-B) with a Ki value of 70 nM by a pathway that is independent of its actions on the A2A receptor. (E)-8-(3-Chlorostyryl)caffeine has the potential for Parkinson's disease research .
FFN 206 dihydrochloride, a fluorescent probe, is used as an excellent Vesicular Monoamine Transporter 2 (VMAT2) substrate with an apparent Km of 1.16 μM. FFN 206 dihydrochloride is capable of detecting VMAT2 activity in intact cells using fluorescence microscopy, with subcellular localization to VMAT2-expressing acidic compartments without apparent labeling of other organelles .
GZ-11608 is a potent and selective vesicular monoamine transporter-2 (VMAT2) inhibitor with high affinity (Ki = 25 nM). GZ-11608 decreases methamphetamine-induced dopamine release from isolated synaptic vesicles from brain dopaminergic neurons. GZ-11608 exhibits rapid brain penetration and without neurotoxicity. GZ-11608 can be used for the research of methamphetamine use disorder .
Norharmane (Norharman), a β-carboline alkaloid, is a potent and reversible monoamine oxidase inhibitor, with IC50 values of 6.5 and 4.7 μM for MAO-A and MAO-B, respectively. Norharmane causes antidepressant responses. Norharmane is also a prospective anti-cancer photosensitizer. Norharmane alters polar auxin transport (PAT) by inhibiting PIN2, PIN3 and PIN7 transport proteins, thus causing a significant inhibitory effect on the growth of Arabidopsis thaliana seedlings .
Ladostigil (TV-3326) is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC50s of 37.1 and 31.8 μM for MAO-B and AChE, respectively. Ladostigil exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil can be used for the research of depression and Alzheimer's disease . Ladostigil is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Ladostigil (TV-3326) hydrochloride is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC50s of 37.1 and 31.8 μM for MAO-B and AChE, respectively. Ladostigil hydrochloride exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil can be used for the research of depression and Alzheimer's disease . Ladostigil (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Trimipramine N-oxide is an active metabolite of the tricyclic antidepressant trimipramine. Trimipramine N-oxide inhibits the human monoamine transporters for noradrenaline (hNAT), serotonin (hSERT), dopamine (hDAT) and the human organic cation transporters (hOCT1 and hOCT2) with IC50s of 11.7, 3.59, 9.4, 9.35 and 27.4 nM, respectively. Trimipramine N-oxide can be used for the research of depression and anxiety .
(E/Z)-J147 is an exceptionally potent, orally active, neuroprotective agent for cognitive enhancement. (E/Z)-J147 can readily pass the blood brain barrier (BBB). (E/Z)-J147 can inhibit monoamine oxidase B (MAO B) and the dopamine transporter with EC50 values of 1.88 μM and 0.649 μM, respectively. (E/Z)-J147 has potential for the treatment of Alzheimer’s disease (AD) .
PF9601N, an monoamine oxidase B (MAO-B) inhibitor, possesses neuroprotective properties in several in vitro and in vivo models of Parkinson's disease (PD). PF9601N can be used for the research of neurodegenerative diseases mediated by excitotoxicity . PF9601N is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
NW-1772 (methanesulfonate) (22b) is a potent and selective monoamine oxidase (MAO) B inhibitor. NW-1772 (methanesulfonate) is the equivalent of HY-111156 NW-1772. NW-1772 has some advantages, such as rapid blood-brain barrier penetration, short-acting and reversible inhibitory activity, slight inhibition of selected cytochrome P450s, and low in vitro toxicity. NW-1772 can be used for the research of neurodegenerative diseases .
Hydroxyisobakuchiol (Delta3,2-Hydroxylbakuchiol), an analog of Bakuchiol (HY-N0235) isolated from Psoralea corylifolia (L.), is a potent monoamine transporter inhibitor. 13-Hydroxyisobakuchiol is more selective for the dopamine transporter (DAT) (IC50=0.58 μM) and norepinephrine transporter (NET) (IC50=0.69 μM) than for the serotonin transporter (SERT) (IC50=312.02 μM). 13-Hydroxyisobakuchiol has the potential for the research of disorders such as Parkinson's disease and depression .
1-Methyl-2-undecyl-4(1H)-quinolone is a potent, irreversible and selective inhibitor of type B monoamine oxidase (MAO-B). 1-Methyl-2-undecyl-4(1H)-quinolone shows a selective inhibition of MAO-B activity with the IC50 and Ki values of 15.3 μM and 9.91 μM, respectively, but did not inhibit type A MAO (MAO-A) activity. Methyl-2-undecyl-4(1H)-quinolone, as a quinolone alkaloid, is isolated from fresh leaves and fruits of Evodia rutaecarpa HOOK. f. et THOMS .
ChEs/MAOs-IN-1 (Compound 4i) is a dual inhibitor of cholinesterases (ChEs) and monoamine oxidases (MAOs).ChEs/MAOs-IN-1 has IC50 values of 0.048 μM, 0.89 μM, 3.58 μM, and 0.095 μM for AChE, BChE, MAO-B and MAO-B respectively. ChEs/MAOs-IN-1 can be used in the study of neurodegenerative diseases .
Budipine is an anti-parkinson agent. Budipine also is a substrate of P-glycoprotein (P-gp), is mediated the uptake into the brain by P-gp. Budipine also is N-methyl-d-aspartate (NMDA) antagonist, and has indirect dopaminergic effects through an improved dopamine release, the inhibition of monoamine oxidase type B (MAO-B). Budipine can be used for the research of CNS disorders include Parkinson disease .
H3R antagonist 2 (Compound 23) is a multitarget histamine H3 receptor (H3R) antagonist with a Ki of 170 nM for hH3R . H3R antagonist 2 shows inhibitory effects with IC50 values of 180, 880 and 775 nM for acetylcholinesterase, butyrylcholinesterase and human monoamine oxidase B (hMAO B), respectively. H3R antagonist 2 shows favorable anti-neuropathic pain and memory-enhancing effects. H3R can across BBB .
Befloxatone (MD-370503) is an orally active, selective and reversible inhibitor of Monoamine Oxidase A (MAO-A) (IC50=4 nM). Befloxatone increases the tissue level of monoamine, striatal dopamine and cortical norepinephrine. Befloxatone has antidepressant potential .
WAY-620147 (compound 6) is an N-(2-morpholinoethyl)nicotinamide derivative that inhibits monoamine oxidase (Monoamine Oxidase). WAY-620147 inhibits MAO-A and MAO-B with IC50s of 26 μM and 55 μM, respectively .
MAO-B-IN-31 (Compound 30) is an effective and selective inhibitor of monoamine oxidase B (monoamine oxidase B). The IC50 value is 41 nM. MAO-B-IN-31 also inhibits α-syn and tau aggregation. MAO-B-IN-31 has neuroprotective activity .
Clorgyline hydrochloride is an irreversible and selective inhibitor of monoamine oxidase A (MAO-A) that is used in scientific research; structurally related to Pargyline.
Iproniazid phosphate is a non-selective, irreversible monoamine oxidase (MAO) inhibitor of the hydrazine class. Iproniazid phosphate has antidepressive activity .
Hydroxylamine hydrochloride is a selective monoamine oxidase (MAO) inhibitor used for inhibiting of platelet aggregation. Hydroxylamine hydrochloride is an intermediate of organic synthesis .
MAO-B-IN-9 (compound 16) is a potent, selective, BBB-penetrated, irreversible and time-dependent MAO-B (monoamine oxidase B) inhibitor, with an IC50 of 0.18 μM. MAO-B-IN-9 prevents Aβ1-42-induced neuronal cell death. MAO-B-IN-9 shows neuroprotective effects, which may be the result of its Aβ1-42 anti-aggregation effects . MAO-B-IN-9 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
2614W94 is a selective, reversible inhibitor of monoamine oxidase-A with a competitive mechanism of inhibition and IC50 of 5 nM and Ki of 1.6 nM with serotonin as substrate.
(+)-Tetrabenazine-d6 is the deuterium labeled (+)-Tetrabenazine. (+)-Tetrabenazine is a reversible inhibitor of vesicular monoamine transporter 2 (VMAT-2).
Pivalylbenzhydrazine (Pivhydrazine) is a potent monoamine oxidase (MAO) inhibitor. Pivalylbenzhydrazine decreases cartilage growth in normal rats. Pivalylbenzhydrazine can be used in research of depression .
NBI-98782 is a high affinity and selectivity vesicular monoamine transporter 2 (VMAT2) inhibitor with a Ki of 3 nM. NBI-98782 has antipsychotic activity .
Amitraz is a non-systemic acaricide and insecticide, with alpha-adrenergic agonist activity, interaction with octopamine receptors of the central nervous system and inhibition of monoamine oxidases and prostaglandin synthesis.
Rubrofusarin triglucoside is a glycoside compound isolated from Cassia obtusifolia Linn seeds. Rubrofusarin triglucoside inhibits human monoamine oxidase A (hMAO-A) with an IC50 of 85.5 μM .
Cimoxatone (MD 780515) is a reversible, selectively and orally active type A monoamine oxidase (MAO-A) inhibitor. Cimoxatone enhances the anorectic action of Serotonin (HY-B1473A) .
MAO-B-IN-14 (Compound 9) is a potent and selective monoamine oxidase-B (MAO-B) inhibitor with an IC50 of 0.95 μM and a Ki of 0.55 μM against human MAO-B.
Diclofensine hydrochloride (Ro-8-4650 hydrochloride) is a potent inhibitor of monoamine reuptake, blocking the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3, and 3.7 nM, respectively.
Diclofensine(Ro-8-4650) is a potent inhibitor of monoamine reuptake, blocking the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3, and 3.7 nM, respectively.
Hydroxylamine-d3 (hydrochloride) is the deuterium labeled Hydroxyamine hydrochloride[1]. Hydroxyamine hydrochloride is a selective monoamine oxidase (MAO) inhibitor used for inhibiting of platelet aggregation. Hydroxyamine hydrochloride is an intermediate of organic synthesis[2].
Pimprinine is a potent monoamine oxidase inhibitor, could be isolated from fermented broths. Pimprinine has antioxidative activity and anticonvulsant activity. Pimprinine inhibits tremorine-induced tremors and analgesia in mice .
FFN200 dihydrochloride, a fluorescent substrate of VMAT2, selectively trace monoamine exocytosis in both neuronal cell culture and brain tissue. The fluorescence excitation and emission maxima of FFN200 are determined to be 352 and 451 nm, respectively .
PSB-1491 is a selective and competitive monoamine oxidase B (MAO-B) inhibitor with an IC50 of 0.386 nM for hMAO-B. PSB-1491 shows >25000-fold selective versus MAO-A .
Tetrabenazine (Ro 1-9569) is a reversible inhibitor of the vesicular monoamine transporter VMAT2 with the Kd value of 1.34 nM. Tetrabenazine can be used for research on diseases related to hyperactive movement disorders such as Huntington's disease .
Amitraz-d3 is the deuterium labeled Amitraz. Amitraz is a non-systemic acaricide and insecticide, with alpha-adrenergic agonist activity, interaction with octopamine receptors of the central nervous system and inhibition of monoamine oxidases and prostaglandin synthesis.
Tetrabenazine (Ro 1-9569) mesylate is a reversible inhibitor of the vesicular monoamine transporter VMAT2 with the Kd value of 1.34 nM. Tetrabenazine mesylate can be used for research on diseases related to hyperactive movement disorders such as Huntington's disease .
Tetrindole mesylate is a selective inhibitor of monoamine oxidase A (MAO A). Tetrindole mesylate inhibits rat brain mitochondrial MAO A in a competitive manner with a Ki value of 0.4 μM and inhibits MAO B with a Ki of 110 μM. Tetrindole mesylate has antidepressant activity .
Trans (2,3)-Dihydrotetrabenazine ((2R,3R,11bR)-rel-Dihydrotetrabenazine), a metabolite of Tetrabenazine, shows remarkable inhibition activity on vesicular monoamine transporter (VMAT2) .
C175-0062 is a monoamine oxidase B (MAO-B) inhibitor. C175-0062 can be used for the research of neurodegenerative disorders, including Parkinson's disease (PD), Alzheimer’s disease (AD), and amyotrophic lateral sclerosis (ALS) .
Contezolid (MRX-I), a new and orally active oxazolidinone, is an antibiotic in study for complicated skin and soft tissue infections (cSSTI) caused by resistant Gram-positive bacteria. Contezolid (MRX-I) markedly reduces potential for myelosuppression and monoamine oxidase inhibition (MAOI) .
Cassiaside B2 is a protein tyrosine phosphatase 1B (PTP1B) and human monoamine oxidase A (hMAO-A) inhibitor. Cassiaside B2 possesses antiallergic and is a 5-HT2C receptor agonist . ..
SL-25.1188 is a potent monoamine oxidase B (MAO-B) inhibitor with Ki values of 2.9 and 8.5 nM for human MAO-B and rat MAO-B, respectively. SL-25.1188 can be used for positron emission tomography .
MAO-IN-4 (Compound 2l) is a monoamine oxidase (MAO) inhibitor, with IC50 values of 0.07 and 0.75 μM for MAO-A and MAO-B Enzymes, respectively. MAO-IN-4 can be used for the research of depression and Parkinson’s disease (PD) .
Methylpiperic acid is a piperine alkaloid with significant MAO inhibitory activity (IC503.6 μM). Methylpiperic acid is less effective against MAO-B (IC 501.6 μM) than MAO-A (IC5027.1 μM) has a bidirectional inhibitory effect. Methylphenidate is used to treat mental disorders .
Tetrabenazine Metabolite is an active metabolite of Tetrabenazine. Tetrabenazine Metabolite is a vesicular monoamine transporter 2 (VMAT2) inhibitor with a high affinity (Ki=13.4 nM) . Tetrabenazine Metabolite is be developed for the treatment of chorea associated with Huntington’s disease and other hyperkinetic disorders .
Melitracen-d6 (hydrochloride) is the deuterium labeled Melitracen hydrochloride. Melitracen hydrochloride is an orally active biphasic antidepressant and antianxiety agent. Melitracen hydrochloride can inhibit the uptake of Norepinephrine and 5-HT (serotonin) through the presynaptic membrane inducing the increase of monoamine transmitters in synaptic space[1][2].
Moclobemide-d4 is deuterium labeled Moclobemide. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A[1].Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
1,4-Naphthoquinone-d6 is the deuterium labeled 1,4-Naphthoquinone[1]. 1,4-Naphthoquinone is a potential pharmacophore for inhibition of both MAO (monoamine oxidase) and DNA topoisomerase activities, this latter associated with antitumor activity[2].
AChE-IN-60 (compound 6k) is a potant acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitor with IC50s of 27 nM and 43 nM, respectively. AChE-IN-60 also inhibits monoamine oxidase (MAO)-A and MAO-B with IC50s of 353 nM and 716 nM, respectively .
Ro 41-1049 hydrochloride is a reversible and selective inhibitor of monoamine oxidase-A (MAO-A). An homogeneous population of high affinity binding sites for [ 3H]Ro 41-1049 is found in membrane preparations from human frontal cortex and placenta (Kd values of 16.5 and 64.4 nM, respectively) .
FFN270 hydrochloride, a fluorescent tracer of norepinephrine, is a fluorescent substrate of the norepinephrine and vesicular monoamine transporters. FFN270 hydrochloride exhibits two resolved absorption/excitation maxima depending on solvent pH (FFN270 ex: 320 nm or 365 nm, em: 475 nm) and can function as ratiometric fluorescent pH-sensors .
DOV-216,303 (Free Base) is a potent triple serotonin, norepinephrine, and dopamine reuptake inhibitor, with IC50 values of 14 nM, 20 nM and 78 nM for hSERT, hNET and hDAT, respectively . Has antidepressant-like effects and increases monoamine release in the prefrontal cortex of olfactory bulbectomized (OBX) rats .
hMAO-B-IN-5(B15) is a potent, selective and reversible inhibitor of human monoamine oxidase hMAO-B with IC50 of 0.12 μM. hMAO-B-IN-5 can pass through the blood-brain barrier and can be used in the research of neurodegenerative diseases .
Tranylcypromine (SKF 385) hemisulfate is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression. Tranylcypromine hemisulfate is also a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis. Tranylcypromine has antidepressant effects .
FTEAA is a 4-styrylpiperidine inhibitor. FTEAA exhibits potent inhibitory effect towards both monoamine oxidase with IC50s of 0.52 μM (MAO-A), 1.02 μM (MAO-B), respectively. MAO inhibitors can be used for cardiovascular, neurological and oncological disorders research .
Tranylcypromine-d5 (hydrochloride) is a deuterium labeled (rel)-Tranylcypromine hydrochloride. Tranylcypromine hydrochloride is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression. Tranylcypromine hydrochloride is also a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis[1][2].
Bifemelane hydrochloride (MCI-2016) is a potent, selective and competitive inhibitor of monoamine oxidase A (MAO-A), with a Ki of 4.20 μM. Bifemelane hydrochloride also inhibits MAO-B noncompetitively with a Ki of 46.0 μM. Bifemelane hydrochloride has a potent antidepressant activity and can be used for the research of cognitive and emotional disturbances related to cerebrovascular disease .
Homopterocarpin is an isoflavonoid that can be isolated from Pterocarpus erinaceus. Homopterocarpin has hepatoprotective and antioxidant properties. Homopterocarpin is a competitive reversible inhibitor of human monoamineoxidase-B with an IC50 and a Ki of 0.72 and 0.21 μM for hMAO-B, respectively. Homopterocarpin can be used for the research of liver injury and oxidative stress .
(+)-Tetrabenazine ((+)-TBZ; (3R,11bR)-TBZ; (3R,11bR)-Tetrabenazine) is a reversible inhibitor of vesicular monoamine transporter 2 (VMAT-2), inhibits transport by VMAT2 with 10-fold greater potency than transport by VMAT1.
4-Hydroxyderricin, the major active ingredients of Angelica keiskei Koidzumi, is a potent selective MAO-B (Monoamine oxidase inhibitors) inhibitor with an IC50 of 3.43 μM. 4-Hydroxyderricin also mildly inhibits DBH (dopamine β-hydroxylase) activity. 4-Hydroxyderricin has antidepressant activity .
Osthenol (Ostenol), a prenylated coumarin isolated from the dried roots of Angelica pubescens, is selective, reversible, and competitive human monoamine oxidase-A (hMAO-A) inhibitor (Ki=0.26 µM). Osthenol potently inhibits recombinant hMAO-A with an IC50 of 0.74 µM and shows a high selectivity index for hMAO-A versus hMAO-B .
Pargyline hydrochloride is an irreversible monoamine oxidase (MAO) inhibitor with Kis of 13 μM and 0.5 μM for MAO-A and MAO-B, respectively. Pargyline hydrochloride has antihypertensive and anticancer activities . Pargyline (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Pargyline is an irreversible monoamine oxidase (MAO) inhibitor with Kis of 13 μM and 0.5 μM for MAO-A and MAO-B, respectively. Pargyline has antihypertensive and anticancer activities . Pargyline is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
GZ-793A is an orally active and selective vesicular monoamine transporter-2 (VMAT2) inhibitor, with an Ki of 0.029 µM. GZ-793A inhibits the neurochemical effects of methamphetamine (METH)-induced dopamine release. GZ-793A can be used for research of METH addiction .
hMAO-B-IN-7 (compound 11n) is a potent and blood–brain barrier (BBB) penetrable inhibitor of human monoamine oxidase-B (hMAO-B), with the IC50 value of 0.79±0.05 μM. hMAO-B-IN-7 can be used for Alzheimer’s disease (AD) and Parkinson’s disease (PD) research .
MAO-A inhibitor 2 (compound HT4) is a monoamine oxidase A (MAO-A) inhibitor with an IC50 of 14.3 µM. MAO-A inhibitor 2 shows a less effect on MAO-B (IC50 of 106 µM) and shows almost ineffective on xanthine oxidase (XO). MAO-A inhibitor 2 can be used for the neurodegenerative disorders and oxidative stress research .
CA/MAO-B-IN-1 (Compound 78) is a dual inhibitor for human brain carbonic anhydrases (CA) and Monoamine Oxidase-B (MAO-B), with IC50s of 8.8 and 7.0 nM, respectively. CA/MAO-B-IN-1 reveals a human oral absorption of 71.9% through in silico prediction .
MAO A/HDAC-IN-1 is a dual?inhibitor?of monoamine oxidase A (MAO A) and HDAC. MAO A/HDAC-IN-1 can be used for glioma research . MAO A/HDAC-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Tranylcypromine hydrochloride (SKF 385 hydrochloride) is an irreversible inhibitor of lysine-specific demethylase 1 (LSD1/BHC110) and monoamine oxidase (MAO). Tranylcypromine hydrochloride inhibits LSD1, MAO A and MAO B with IC50s of 20.7, 2.3 and 0.95 μM, respectively. Tranylcypromine hydrochloride can be used for the research of depression .
DOV-216,303 is an antidepressant compound. DOV-216,303 inhibits the reuptake of norepinephrine (NE), serotonin (5‐HT), and dopamine (DA), with IC50 values of 14 nM, 20 nM and 78 nM for hSERT, hNET and hDAT, respectively. DOV-216,303 increases monoamine release in the prefrontal cortex of olfactory bulbectomized (OBX) rats .
Isatin (Indoline-2,3-dione) is a potent inhibitor of monoamine oxidase (MAO) with an IC50 of 3 μM. Also binds to central benzodiazepine receptors (IC50 against clonazepam, 123 μM) . Also acts as an antagonist of both atrial natriuretic peptide stimulated and nitric oxide-stimulated guanylate cyclase activity . Shows effect on the serotonergic system .
(-)-Dizocilpine maleate ((-)-MK-801 maleate) is a less active (-)-enantiomer of Dizocilpine. (-)-Dizocilpine maleate is a selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist with a Ki of 211.7 nM. (-)-Dizocilpine maleate has antidepressant effects .
Rasagiline (R-AGN1135) mesylate is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC50s of 4.43?nM and 412?nM for rat brain MAO B and A activity, respectively . Rasagiline (mesylate) is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Rasagiline (R-AGN1135) is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC50s of 4.43?nM and 412?nM for rat brain MAO B and A activity, respectively . Rasagiline is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Azure B is a cationic dye and the major metabolite of Methylene blue. Azure B is used in making Azure eosin stains for blood smear staining. Azure B is a high-potency, selective and reversible inhibitor of monoamine oxidases (MAO)-A, with IC50s of 11 and 968 nM for recombinant human MAO-A and MAO-B, respectively. Azure B possesses significant antidepressant-like effects .
MAO-B-IN-10 (compound 4f) is a potent, selective, BBB-penetrated MAO-B (monoamine oxidase-B) inhibitor, with IC50 of 5.3 μM. MAO-B-IN-10 can inhibit (58.2%) and disaggregate (43.3%) self-mediated Aβ (amyloid β) aggregation. MAO-B-IN-10 can be use for Alzheimer’s disease research .
Octopamine ((±)-p-Octopamine) hydrochloride, a biogenic monoamine structurally related to noradrenaline, acts as a neurohormone, a neuromodulator and a neurotransmitter in invertebrates. Octopamine hydrochloride can stimulate alpha2-adrenoceptors (ARs) in Chinese hamster ovary cells transfected with human alpha2-ARs. Octopamine hydrochloride increased glycogenolysis, glycolysis, oxygen uptake, gluconeogenesis and the portal perfusion pressure .
Rasagiline- 13C3 (mesylate racemic) is a 13C-labeled Rasagiline mesylate racemic. Rasagiline mesylate racemic is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor[1]. Rasagiline-13C3 (mesylate racemic) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
FFN511 is a potent fluorescent false neurotransmitters (FFNs) that targets neuronal vesicular monoamine transporter 2 (VMA T2). FFN511 inhibits serotonin binding to VMA T2-containing membranes with an IC50 of 1 µM. FFN511 directly images the dynamics of release during exocytosis, can be used to label dopamine terminals in live cortical-striatalacute slices .
Methylene blue trihydrate (C.I. Basic Blue 9 trihydrate) is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue trihydrate is a vasopressor and is often used as a dye in several medical procedures. Methylene blue trihydrate has antinociception, antimalarial, antidepressant and anxiolytic activity effects. Methylene Blue trihydrate has the potential for methemoglobinemias, neurodegenerative disorders and ifosfamide-induced encephalopathytreatment .
Rasagiline- 13C3 ((R)-AGN1135- 13C3; TVP1012- 13C3) mesylateis the deuterium labeledRasagiline (mesylate)(HY-14605) . Rasagiline (R-AGN1135) mesylate is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC50s of 4.43?nM and 412?nM for rat brain MAO B and A activity, respectively .
AChE/BChE/MAO-B-IN-1 (Compound 10) is a reversible and non-time-dependent AChE, BChE and MAO-B inhibitor with IC50 values of 7.31, 0.56 and 26.1 μM for hAChE, hBChE and hMAO-B, respectively. AChE/BChE/MAO-B-IN-1 can cross the BBB and shows neuroprotective effects without cytotoxicity .
Myristicine is an orally bioavailable serotonin receptor antagonist and weak monoamine oxidase (MAO) inhibitor. Myristicine also exerts anti-cancer effects on gastric cancer cells by inhibiting the EGFR/ERK signaling pathway. Myristicine is the main component of nutmeg essential oil and has anti-cancer, anti-proliferative, antibacterial, anti-inflammatory and apoptosis-inducing effects. Myristicine abuse can produce hallucinogenic effects, organ damage, etc .
Octopamine-d4 (hydrochloride) is the deuterium labeled Octopamine hydrochloride. Octopamine ((±)-p-Octopamine) hydrochloride, a biogenic monoamine structurally related to noradrenaline, acts as a neurohormone, a neuromodulator and a neurotransmitter in invertebrates. Octopamine hydrochloride can stimulate alpha2-adrenoceptors (ARs) in Chinese hamster ovary cells transfected with human alpha2-ARs. Octopamine hydrochloride increased glycogenolysis, glycolysis, oxygen uptake, gluconeogenesis and the portal perfusion pressure[1][2][3].
hMAO-B-IN-4 (compound B10) is a selective, reversible and blood–brain barrier (BBB) penetrable human monoamine oxidase-B (hMAO-B) inhibitor with an IC50 value and a Ki value of 0.067 and 0.03 μM, respectively. hMAO-B-IN-4 inhibits hMAO-A with an IC50 value of 33.82 μM. hMAO-B-IN-4 can be used for Alzheimer’s disease (AD) and Parkinson’s disease (PD) research .
(1S,2R)-Tranylcypromine-d5 (hydrochloride) is the deuterium labeled Tranylcypromine hydrochloride[1]. Tranylcypromine hydrochloride (SKF 385 hydrochloride) is an irreversible inhibitor of lysine-specific demethylase 1 (LSD1/BHC110) and monoamine oxidase (MAO). Tranylcypromine hydrochloride inhibits LSD1, MAO A and MAO B with IC50s of 20.7, 2.3 and 0.95 μM, respectively. Tranylcypromine hydrochloride can be used for the research of depression[2][3][4].
Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM) . Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al .
Methylene blue (Basic Blue 9) is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue is a vasopressor and is often used as a dye in several medical procedures. Methylene blue through the nitric oxide syntase/guanylate cyclase signalling pathway to reduce prepulse inhibition. Methylene blue is a REDOX cycling compound and able to cross the blood-brain barrier. Methylene blue is a Tau aggregation inhibitor. Methylene blue reduces cerebral edema, attenuated microglial activation and reduced neuroinflammation .
Ladostigil (TV-3326) hemitartrate is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC50s of 37.1 and 31.8 μM for MAO-B and AChE, respectively. Ladostigil hemitartrate exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil hemitartrate can be used for the research of depression and Alzheimer's disease . Ladostigil (hemitartrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Methylene blue (Basic Blue 9) hydrate is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue is a vasopressor and is often used as a dye in several medical procedures. Methylene blue hydrate through the nitric oxide syntase/guanylate cyclase signalling pathway to reduce prepulse inhibition. Methylene blue hydrate is a REDOX cycling compound and able to cross the blood-brain barrier. Methylene blue hydrate is a Tau aggregation inhibitor. Methylene blue hydrate reduces cerebral edema, attenuated microglial activation and reduced neuroinflammation .
MAO A/HSP90-IN-1 (4-b) is a MAO A/HSP90 dual inhibitor with IC50 value of 1.77 μM and 0.019 μM in Glioblastoma (GBM) GL26 cells and HSP90α, respectively. MAO A/HSP90-IN-1 (4-b) can inhibit MAO A activity, HSP90 binding and the expression of HER2 and phospho-Akt to inhibit the growth of GBM, they also reduce PD-L1 expression, which inhibits T cell activation. MAO A/HSP90-IN-1 (4-b) have potential to inhibit tumor immune escape. MAO A/HSP90-IN-1 (4-b) can be used for brain tumor-related diseases research .
Safinamide (FCE 26743; EMD 1195686) mesylate is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 nM) . Safinamide mesylate also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide mesylate has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke et.al .
Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively). Harmane exhibits comutagenic effect .
Harmane-d is the deuterium labeled Harmane. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively)[1][2][3][4].
Harmane-d2 is the deuterium labeled Harmane. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively)[1][2][3][4].
Safinamide-d4-1 is deuterium labeled Safinamide. Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM)[1]. Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al[2][3].
AChE/BuChE/MAO-B-IN-1 (compound 19) is an inhibitor of human acetyl- (hAChE), butyrylcholinesterase (hBuChE) and monoamine oxidase-B (hMAO-B) with IC50s of 4.8 μM, 13.7 μM, and 1.11 μM, respectively. AChE/BuChE/MAO-B-IN-1 also exhibits high affinity to both the σ1 and σ2 receptors with Ki values of 42.8 nM (human σ1 receptor) and 191 nM (rat σ2 receptor), respectively. AChE/BuChE/MAO-B-IN-1 can be used for Alzheimer’s disease research .
hMAO-B/MB-COMT-IN-1 is a dual MAO-B/MB-COMT inhibitor (IC50s: 2.5 μΜ for hMAO-B, 3.84 μΜ for MB-COMT). hMAO-B/MB-COMT-IN-1 protects cells against oxidative damage. hMAO-B/MB-COMT-IN-1 can be used in the research of neurodegeneration disease, such as Parkinson’s Disease (PD) .
hMAO-B/MB-COMT-IN-2 is a dual MAO-B/MB-COMT inhibitor (IC50s: 4.27 μΜ for hMAO-B, 2.69 μΜ for MB-COMT). hMAO-B/MB-COMT-IN-2 protects cells against oxidative damage. hMAO-B/MB-COMT-IN-2 can be used in the research of neurodegeneration disease, such as Parkinson’s Disease (PD) .
Harmane (Standard) is the analytical standard of Harmane. This product is intended for research and analytical applications. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively). Harmane exhibits comutagenic effect .
Adenosine receptor inhibitor 2 (compound 14b) is a potent AR (adenosine receptor) inhibitor. Adenosine receptor inhibitor 2 shows dual affinity toward A1/A2A ARs with higher affinity for the A1- than the A2AAR. Adenosine receptor inhibitor 2 has Ki values of 52.2 nM for the A1AR and 167 nM for the A2AAR .
MAO-B-IN-28 (compound 10e) is a potent hMAO-B inhibitor with an IC50 of 1.9±0.5 nM. MAO-B-IN-28 can be used as a candidate for neurodegenerative diseases research .
BChE-IN-7 (compound 13) is a potent, selective, BBB-penetrated and reversible AChE and BChE inhibitor, with an IC50 of 0.06 μM (BChE). BChE-IN-7 can protect neuronal-like cells from toxic Aβ-species .
LSD1-IN-15 (compound 1b) is a potent LSD1 inhibitor. LSD1-IN-15 can inhibit LSD1-CoREST, MAO-A and MAO-B, with IC50 values of 0.149, 0.028, and 0.327 μM, respectively. LSD1-IN-15 displays cell growth arrest in prostate cancer LNCaP cells, with an IC50 of 9.9 μM .
LSD1-IN-16 (compound 4b) is a potent LSD1 inhibitor. LSD1-IN-16 can inhibit LSD1-CoREST, MAO-A and MAO-B, with IC50 values of 0.015, 0.024, and 0.366 μM, respectively. LSD1-IN-16 displays cell growth arrest in prostate cancer LNCaP cells, with an IC50 of 15.2 μM .
LSD1-IN-17 (compound 5b) is a potent LSD1 inhibitor. LSD1-IN-17 can inhibit LSD1-CoREST, MAO-A and MAO-B, with IC50 values of 0.005, 0.028, and 0.820 μM, respectively. LSD1-IN-17 displays cell growth arrest in prostate cancer LNCaP cells, with an IC50 of 17.2 μM .
Parkinson’s disease (PD), the second most common age-associated neurodegenerative disorder, is characterized by the loss of dopaminergic (DA) neurons and the presence of α-synuclein-containing aggregates in the substantia nigra pars compacta (SNpc). Motor features such as tremor, rigidity, bradykinesia and postural instability are common traits of PD. To date, there is no treatment to stop or at least slow down the progression of the disease. The etiology and pathogenesis of PD is still elusive, however, a large body of evidence suggests a prominent role of oxidative stress, inflammation, apoptosis, mitochondrial dysfunction and proteasome dysfunction in the pathogenesis of PD.
MCE offers a unique collection of 1339 compounds with anti- Parkinson’s Disease activities or targeting the unique targets of PD. MCE Anti- Parkinson's Disease Compound Library is a useful tool for exploring the mechanism of PD and discovering new drugs for PD.
Neurodegenerative diseases are incurable and life-threatening conditions that result in progressive degeneration and/or death of nerve cells. Some common neurodegenerative diseases include Alzheimer’s Disease (AD), Parkinson’s Disease (PD), Motor Neuron Disease (MND), Huntington’s Disease (HD), Spino-Cerebellar Ataxia (SCA), Spinal Muscular Atrophy (SMA), and Amyotrophic Lateral Sclerosis (ALS). Because the pathophysiology of neurodegenerative disorders is generally poorly understood, it is difficult to identify promising molecular targets and validate them. At the same time, about 85% of the drugs fail in clinical trials. Therefore, validating new targets and discovering new drugs to mitigate neurodegenerative disorders is need of the hour.
MCE offers a unique collection of 2228 compounds with anti-Neurodegenerative Diseases activities or targeting the unique targets of neurodegenerative diseases. MCE Neurodegenerative Disease-related Compound Library is a useful tool for exploring the mechanism of neurodegenerative diseases and discovering new drugs for neurodegenerative diseases.
Azure B is a cationic dye and the major metabolite of Methylene blue. Azure B is used in making Azure eosin stains for blood smear staining. Azure B is a high-potency, selective and reversible inhibitor of monoamine oxidases (MAO)-A, with IC50s of 11 and 968 nM for recombinant human MAO-A and MAO-B, respectively. Azure B possesses significant antidepressant-like effects .
Methylene blue (Basic Blue 9) is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue is a vasopressor and is often used as a dye in several medical procedures. Methylene blue through the nitric oxide syntase/guanylate cyclase signalling pathway to reduce prepulse inhibition. Methylene blue is a REDOX cycling compound and able to cross the blood-brain barrier. Methylene blue is a Tau aggregation inhibitor. Methylene blue reduces cerebral edema, attenuated microglial activation and reduced neuroinflammation .
Tranylcypromine (SKF 385) hydrochloride (GMP) is Tranylcypromine (HY-17447) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Tranylcypromine hydrochloride is a potent monoamine oxidase (MAO) inhibitor .
Tranylcypromine (SKF 385) hydrochloride (GMP) is Tranylcypromine (HY-17447) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Tranylcypromine hydrochloride is a potent monoamine oxidase (MAO) inhibitor .
Glicoricone, a phenolic compound, is isolated from a species of licorice. Glicoricone is an inhibitor of monoamine oxidase (MAO), with an IC50 of 140 μM. Glicoricone binds to estrogen receptor (ER) and shows estrogen antagonist activity .
Methyl citrate is a Monoamine oxidase B (MAO-B) inhibitor (IC50=0.23 mM). Methyl citrate is isolated from the fruits of Opuntia ficus-indica var. saboten Makino .
Obtusin, isolated from Cassia obtusifolia Linn seed, is a highly selective and competitive human monoamine oxidase-A (hMAO-A) inhibitor with an IC50 of 11.12 μM and a Ki of 6.15 μM. Obtusin plays a preventive role in neurodegenerative diseases, especially anxiety and depression .
Norharmane (Norharman), a β-carboline alkaloid, is a potent and reversible monoamine oxidase inhibitor, with IC50 values of 6.5 and 4.7 μM for MAO-A and MAO-B, respectively. Norharmane causes antidepressant responses. Norharmane is also a prospective anti-cancer photosensitizer. Norharmane alters polar auxin transport (PAT) by inhibiting PIN2, PIN3 and PIN7 transport proteins, thus causing a significant inhibitory effect on the growth of Arabidopsis thaliana seedlings .
1-Methyl-2-nonyl-4(1H)-quinolone, a quinolone alkaloid, is a potent and selective MAO-B (monoamine oxidase) inhibitor. 1-Methyl-2-nonyl-4(1H)-quinolone exhibites inhibitory activity on leukotriene biosynthesis, with an IC50 of 12.1 μM .
Hydroxyisobakuchiol (Delta3,2-Hydroxylbakuchiol), an analog of Bakuchiol (HY-N0235) isolated from Psoralea corylifolia (L.), is a potent monoamine transporter inhibitor. 13-Hydroxyisobakuchiol is more selective for the dopamine transporter (DAT) (IC50=0.58 μM) and norepinephrine transporter (NET) (IC50=0.69 μM) than for the serotonin transporter (SERT) (IC50=312.02 μM). 13-Hydroxyisobakuchiol has the potential for the research of disorders such as Parkinson's disease and depression .
1-Methyl-2-undecyl-4(1H)-quinolone is a potent, irreversible and selective inhibitor of type B monoamine oxidase (MAO-B). 1-Methyl-2-undecyl-4(1H)-quinolone shows a selective inhibition of MAO-B activity with the IC50 and Ki values of 15.3 μM and 9.91 μM, respectively, but did not inhibit type A MAO (MAO-A) activity. Methyl-2-undecyl-4(1H)-quinolone, as a quinolone alkaloid, is isolated from fresh leaves and fruits of Evodia rutaecarpa HOOK. f. et THOMS .
Rubrofusarin triglucoside is a glycoside compound isolated from Cassia obtusifolia Linn seeds. Rubrofusarin triglucoside inhibits human monoamine oxidase A (hMAO-A) with an IC50 of 85.5 μM .
Cassiaside B2 is a protein tyrosine phosphatase 1B (PTP1B) and human monoamine oxidase A (hMAO-A) inhibitor. Cassiaside B2 possesses antiallergic and is a 5-HT2C receptor agonist . ..
Methylpiperic acid is a piperine alkaloid with significant MAO inhibitory activity (IC503.6 μM). Methylpiperic acid is less effective against MAO-B (IC 501.6 μM) than MAO-A (IC5027.1 μM) has a bidirectional inhibitory effect. Methylphenidate is used to treat mental disorders .
Homopterocarpin is an isoflavonoid that can be isolated from Pterocarpus erinaceus. Homopterocarpin has hepatoprotective and antioxidant properties. Homopterocarpin is a competitive reversible inhibitor of human monoamineoxidase-B with an IC50 and a Ki of 0.72 and 0.21 μM for hMAO-B, respectively. Homopterocarpin can be used for the research of liver injury and oxidative stress .
4-Hydroxyderricin, the major active ingredients of Angelica keiskei Koidzumi, is a potent selective MAO-B (Monoamine oxidase inhibitors) inhibitor with an IC50 of 3.43 μM. 4-Hydroxyderricin also mildly inhibits DBH (dopamine β-hydroxylase) activity. 4-Hydroxyderricin has antidepressant activity .
Osthenol (Ostenol), a prenylated coumarin isolated from the dried roots of Angelica pubescens, is selective, reversible, and competitive human monoamine oxidase-A (hMAO-A) inhibitor (Ki=0.26 µM). Osthenol potently inhibits recombinant hMAO-A with an IC50 of 0.74 µM and shows a high selectivity index for hMAO-A versus hMAO-B .
Isatin (Indoline-2,3-dione) is a potent inhibitor of monoamine oxidase (MAO) with an IC50 of 3 μM. Also binds to central benzodiazepine receptors (IC50 against clonazepam, 123 μM) . Also acts as an antagonist of both atrial natriuretic peptide stimulated and nitric oxide-stimulated guanylate cyclase activity . Shows effect on the serotonergic system .
Octopamine ((±)-p-Octopamine) hydrochloride, a biogenic monoamine structurally related to noradrenaline, acts as a neurohormone, a neuromodulator and a neurotransmitter in invertebrates. Octopamine hydrochloride can stimulate alpha2-adrenoceptors (ARs) in Chinese hamster ovary cells transfected with human alpha2-ARs. Octopamine hydrochloride increased glycogenolysis, glycolysis, oxygen uptake, gluconeogenesis and the portal perfusion pressure .
Myristicine is an orally bioavailable serotonin receptor antagonist and weak monoamine oxidase (MAO) inhibitor. Myristicine also exerts anti-cancer effects on gastric cancer cells by inhibiting the EGFR/ERK signaling pathway. Myristicine is the main component of nutmeg essential oil and has anti-cancer, anti-proliferative, antibacterial, anti-inflammatory and apoptosis-inducing effects. Myristicine abuse can produce hallucinogenic effects, organ damage, etc .
Harmane (Standard) is the analytical standard of Harmane. This product is intended for research and analytical applications. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively). Harmane exhibits comutagenic effect .
SULT1A3 protein, a sulfotransferase utilizing PAPS, catalyzes the sulfate conjugation of phenolic monoamines, including neurotransmitters (dopamine, norepinephrine, serotonin) and drugs. This activity contributes significantly to inactivation and elimination, emphasizing SULT1A3's crucial role in regulating neurotransmitter and drug levels, maintaining homeostasis, and ensuring proper biological system functioning. SULT1A3 Protein, Human (His) is the recombinant human-derived SULT1A3 protein, expressed by E. coli , with N-6*His labeled tag. The total length of SULT1A3 Protein, Human (His) is 295 a.a., with molecular weight of ~35.0 kDa.
The Rnls protein catalyzes the oxidation of the less abundant 1,2-dihydro-β-NAD(P) and 1,6-dihydro-β-NAD(P) to form β-NAD(P)(+). Mainly secreted by the kidneys, this enzyme circulates in the blood and plays a vital role in regulating heart function and systemic blood pressure. Rnls Protein, Mouse (His-SUMO) is the recombinant mouse-derived Rnls protein, expressed by E. coli , with N-His, N-SUMO labeled tag. The total length of Rnls Protein, Mouse (His-SUMO) is 325 a.a., with molecular weight of ~52.0 kDa.
(+)-Tetrabenazine-d6 is the deuterium labeled (+)-Tetrabenazine. (+)-Tetrabenazine is a reversible inhibitor of vesicular monoamine transporter 2 (VMAT-2).
Hydroxylamine-d3 (hydrochloride) is the deuterium labeled Hydroxyamine hydrochloride[1]. Hydroxyamine hydrochloride is a selective monoamine oxidase (MAO) inhibitor used for inhibiting of platelet aggregation. Hydroxyamine hydrochloride is an intermediate of organic synthesis[2].
Amitraz-d3 is the deuterium labeled Amitraz. Amitraz is a non-systemic acaricide and insecticide, with alpha-adrenergic agonist activity, interaction with octopamine receptors of the central nervous system and inhibition of monoamine oxidases and prostaglandin synthesis.
Melitracen-d6 (hydrochloride) is the deuterium labeled Melitracen hydrochloride. Melitracen hydrochloride is an orally active biphasic antidepressant and antianxiety agent. Melitracen hydrochloride can inhibit the uptake of Norepinephrine and 5-HT (serotonin) through the presynaptic membrane inducing the increase of monoamine transmitters in synaptic space[1][2].
Moclobemide-d4 is deuterium labeled Moclobemide. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A[1].Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
1,4-Naphthoquinone-d6 is the deuterium labeled 1,4-Naphthoquinone[1]. 1,4-Naphthoquinone is a potential pharmacophore for inhibition of both MAO (monoamine oxidase) and DNA topoisomerase activities, this latter associated with antitumor activity[2].
Tranylcypromine-d5 (hydrochloride) is a deuterium labeled (rel)-Tranylcypromine hydrochloride. Tranylcypromine hydrochloride is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression. Tranylcypromine hydrochloride is also a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis[1][2].
Rasagiline- 13C3 (mesylate racemic) is a 13C-labeled Rasagiline mesylate racemic. Rasagiline mesylate racemic is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor[1]. Rasagiline-13C3 (mesylate racemic) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Rasagiline- 13C3 ((R)-AGN1135- 13C3; TVP1012- 13C3) mesylateis the deuterium labeledRasagiline (mesylate)(HY-14605) . Rasagiline (R-AGN1135) mesylate is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC50s of 4.43?nM and 412?nM for rat brain MAO B and A activity, respectively .
Octopamine-d4 (hydrochloride) is the deuterium labeled Octopamine hydrochloride. Octopamine ((±)-p-Octopamine) hydrochloride, a biogenic monoamine structurally related to noradrenaline, acts as a neurohormone, a neuromodulator and a neurotransmitter in invertebrates. Octopamine hydrochloride can stimulate alpha2-adrenoceptors (ARs) in Chinese hamster ovary cells transfected with human alpha2-ARs. Octopamine hydrochloride increased glycogenolysis, glycolysis, oxygen uptake, gluconeogenesis and the portal perfusion pressure[1][2][3].
(1S,2R)-Tranylcypromine-d5 (hydrochloride) is the deuterium labeled Tranylcypromine hydrochloride[1]. Tranylcypromine hydrochloride (SKF 385 hydrochloride) is an irreversible inhibitor of lysine-specific demethylase 1 (LSD1/BHC110) and monoamine oxidase (MAO). Tranylcypromine hydrochloride inhibits LSD1, MAO A and MAO B with IC50s of 20.7, 2.3 and 0.95 μM, respectively. Tranylcypromine hydrochloride can be used for the research of depression[2][3][4].
Harmane-d is the deuterium labeled Harmane. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively)[1][2][3][4].
Harmane-d2 is the deuterium labeled Harmane. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively)[1][2][3][4].
Safinamide-d4-1 is deuterium labeled Safinamide. Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM)[1]. Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al[2][3].
Ladostigil (TV-3326) hydrochloride is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC50s of 37.1 and 31.8 μM for MAO-B and AChE, respectively. Ladostigil hydrochloride exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil can be used for the research of depression and Alzheimer's disease . Ladostigil (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
PF9601N, an monoamine oxidase B (MAO-B) inhibitor, possesses neuroprotective properties in several in vitro and in vivo models of Parkinson's disease (PD). PF9601N can be used for the research of neurodegenerative diseases mediated by excitotoxicity . PF9601N is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Pargyline hydrochloride is an irreversible monoamine oxidase (MAO) inhibitor with Kis of 13 μM and 0.5 μM for MAO-A and MAO-B, respectively. Pargyline hydrochloride has antihypertensive and anticancer activities . Pargyline (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Ladostigil (TV-3326) is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC50s of 37.1 and 31.8 μM for MAO-B and AChE, respectively. Ladostigil exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil can be used for the research of depression and Alzheimer's disease . Ladostigil is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
MAO-B-IN-9 (compound 16) is a potent, selective, BBB-penetrated, irreversible and time-dependent MAO-B (monoamine oxidase B) inhibitor, with an IC50 of 0.18 μM. MAO-B-IN-9 prevents Aβ1-42-induced neuronal cell death. MAO-B-IN-9 shows neuroprotective effects, which may be the result of its Aβ1-42 anti-aggregation effects . MAO-B-IN-9 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Pargyline is an irreversible monoamine oxidase (MAO) inhibitor with Kis of 13 μM and 0.5 μM for MAO-A and MAO-B, respectively. Pargyline has antihypertensive and anticancer activities . Pargyline is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
MAO A/HDAC-IN-1 is a dual?inhibitor?of monoamine oxidase A (MAO A) and HDAC. MAO A/HDAC-IN-1 can be used for glioma research . MAO A/HDAC-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Rasagiline (R-AGN1135) mesylate is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC50s of 4.43?nM and 412?nM for rat brain MAO B and A activity, respectively . Rasagiline (mesylate) is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Rasagiline (R-AGN1135) is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC50s of 4.43?nM and 412?nM for rat brain MAO B and A activity, respectively . Rasagiline is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Rasagiline- 13C3 (mesylate racemic) is a 13C-labeled Rasagiline mesylate racemic. Rasagiline mesylate racemic is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor[1]. Rasagiline-13C3 (mesylate racemic) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Ladostigil (TV-3326) hemitartrate is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC50s of 37.1 and 31.8 μM for MAO-B and AChE, respectively. Ladostigil hemitartrate exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil hemitartrate can be used for the research of depression and Alzheimer's disease . Ladostigil (hemitartrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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