MAO-B Inhibitor

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.

Selegiline (Deprenyl) hydrochloride is a potent, selective and irreversible inhibitor of MAO-B, with an IC₅₀ of 51 nM. Selegiline hydrochloride exhibits 450-flod selectivity for MAO-B over MAO-A (IC₅₀=23 μM). Selegiline hydrochloride can be used for the research of Parkinson's disease, Alzheimer's disease and major depressive 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.

Pargyline is an irreversible monoamine oxidase (MAO) inhibitor with K_is 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.

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.

Ethaverine hydrochloride is a Papaverine derivative and vasodilator. Ethaverine hydrochloride inhibits Phosphodiesterase, Tyrosine hydroxylase, and MAO-B. Ethaverine hydrochloride blocks L-type Ca²⁺ channels, reduces intracellular Ca²⁺ levels, inhibits platelet adhesion and aggregation, regulates cardiac conduction and heart rate, and increases peripheral and cerebral blood flow. Ethaverine hydrochloride alters cochlear microcirculation, intracochlear Po₂, CM potential, and EP in guinea pigs, and induces transient hypotension. Ethaverine hydrochloride is used in the research of peripheral vascular diseases.

MAO-B-IN-55 (Compound 5c) is a reversible competitive MAO-B inhibitor with an IC₅₀ of 2.9 nM, and it exhibits approximately 2750-fold higher selectivity for MAO-B over MAO-A. MAO-B-IN-55 can be used for the research of Parkinson's disease.

Ethaverine hydrochloride (Standard) is the analytical standard of Ethaverine hydrochloride (HY-B1440). This product is intended for research and analytical applications. Ethaverine hydrochloride is a Papaverine derivative and vasodilator. Ethaverine hydrochloride inhibits Phosphodiesterase, Tyrosine hydroxylase, and MAO-B. Ethaverine hydrochloride blocks L-type Ca²⁺ channels, reduces intracellular Ca²⁺ levels, inhibits platelet adhesion and aggregation, regulates cardiac conduction and heart rate, and increases peripheral and cerebral blood flow. Ethaverine hydrochloride alters cochlear microcirculation, intracochlear Po₂, CM potential, and EP in guinea pigs, and induces transient hypotension. Ethaverine hydrochloride is used in the research of peripheral vascular diseases.

Pargyline hydrochloride is an irreversible monoamine oxidase (MAO) inhibitor with K_is 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.

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, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Harmane is a benzodiazepine receptor inhibitor (IC₅₀=7 μM), with IC₅₀ values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC₅₀ = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF).

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, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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.

1,4-Naphthoquinone is an inhibitor with broad-spectrum inhibitory activity targeting DNA polymerase, NF-κB and monoamine oxidase (MAO-A/B), with antibacterial and anti-biofilm efficacy. 1,4-Naphthoquinone is a competitive inhibitor of MAO-B (Ki=1.4 μM) and a non-competitive inhibitor of MAO-A (Ki=7.7 μM). 1,4-Naphthoquinone inhibits DNA polymerase pol α, β, γ, δ, ε, λ with IC₅₀ ranging from 5.57-128 μM. 1,4-Naphthoquinone inhibits tumor cell proliferation, induces apoptosis and necrosis, and has anti-angiogenic and anti-inflammatory activities by inducing oxidative stress, depleting glutathione (GSH), inhibiting DNA polymerase-mediated DNA synthesis and blocking NF-κB nuclear translocation. 1,4-Naphthoquinone can be used in anti-bacterial , anti-tumor and anti-inflammatory studies, including inhibition of melanoma and colon cancer cell growth and endothelial cell function, as well as LPS-induced inflammation models.

Maackiain (DL-Maackiain) is an orally active multi-target inhibitor with anti-tumor activity and neuroprotective effects. Maackiain activates the AMPK, NLRP3 and Nrf2/HO-1 pathways, and inhibits key targets such as NF-κB, mTOR, MAO-B, NFATc1 and PKCδ, thereby precisely regulating processes including apoptosis, autophagy and pyroptosis. Maackiain also effectively inhibits microglial activation, osteoclast formation, and proliferation and invasion of tumor cells, and protects dopaminergic neurons from damage. Maackiain is applicable to the research of various diseases such as Alzheimer's disease, osteoporosis, sepsis and dengue fever。

Tedizolid phosphate (TR-701FA) is a MAO-A and MAO-B inhibitor with activity against Gram-positive bacteria.

(E)-8-(3-Chlorostyryl)caffeine is a selective adenosine A_2A receptor antagonist. (E)-8-(3-Chlorostyryl)caffeine inhibits monoamine oxidase B (MAO-B) with a K_i value of 70 nM by a pathway that is independent of its actions on the A_2A receptor. (E)-8-(3-Chlorostyryl)caffeine has the potential for Parkinson's disease research.

2'-Acetylacteoside (2'-AA) is a natural compound with oral activity and blood-brain barrier permeability. 2'-Acetylacteosideexhibits MAO‑B inhibitory activity (IC₅₀ = 17.71 μM, K_i = 13.81 μM). 2'-Acetylacteoside downregulates the expression of RANK, TRAF6, NF‑κB, NFATc1 and IKKβ, disrupts the RANKL/RANK interaction, blocks downstream signaling pathways, and increases the level of phosphorylated Akt. 2'-Acetylacteoside possesses potent anti-osteoclastogenic, anti-bone resorptive, pro-neurogenic, neuroprotective and antioxidant activities. 2'-Acetylacteoside can be used in the research of osteoporosis, ischemic stroke and Parkinson's disease.

Tisolagiline (KDS2010) is the selective, reversible and orally active inhibitor for MAO-B with an IC₅₀ of 8 nM. Tisolagiline exhibits neuroprotective and anti-neuroinflammatory activities.

LSD1/HDAC6-IN-2 (JBI-802) is an orally active LSD1/HDAC6/MAO-A inhibitor, with IC₅₀ values of 5 nM, 11 nM, and 5 nM, respectively. LSD1/HDAC6-IN-2 can inhibit the growth of multiple myeloma cells MM.1S, MM.1R, and RPMI-8226. LSD1/HDAC6-IN-2 can be used for research on diseases such as acute myeloid leukemia and lymphoma.