mao in 1

MAO-IN-1是一种高效的单胺氧化酶B (MAO B)抑制剂（IC50：20 nM），可用于研究神经系统相关疾病。

MAO-B-IN-1 is a monoamine oxidase B inhibitor and can be used for the research of neurological diseases.

AChE BChE MAO-B-IN-1是一种可逆的、非时间依赖且可透过血脑屏障的AChE、BChE 和MAO-B 抑制剂，对 hAChE、hBChE 和 hMAO-B 表现出抑制作用，IC50分别为 7.31、0.56 和 26.1 μM。AChE BChE MAO-B-IN-1具有神经保护作用且无明显细胞毒性。

MAO-A SERT-IN-1 是MAO-A与血清素转运体 (SERT) 的抑制剂。此化合物能有效降低SERT介导的5-HT再摄取，并在细胞模型中展现神经保护作用。MAO-A SERT-IN-1 还能改善斑马鱼和小鼠的抑郁症状。

HDAC1 MAO-B-IN-1 具有用于阿尔茨海默病研究的潜力。它是一种有效的、选择性的HDAC1 MAO-B 抑制剂，可以穿过血脑屏障。HDAC1 MAO-B-IN-1 对 HDAC1 和 MAO-B 的IC50值分别为 21.4 nM 和 99.0 nM。

MAO A HDAC-IN-1 是有效的单胺氧化酶 A (MAO A) 和HDAC 双重抑制剂，可用于胶质瘤研究。

Dual AChE-MAO B-IN-1 (compound 15) 是一种安全的、代谢稳定的神经保护剂。Dual AChE-MAO B-IN-1 是一种强效的、口服具有活力的中枢神经系统渗透的人 AChE(IC50=550 nM) 和 MAO-B (IC50=8.2 nM)抑制剂，对 AChE 和 MAO-B 的 IC50 值分别为 550 nM、8.2 nM。

AChE MAO-IN-1 是一种有效的AChE、MAO-A 和MAO-B 抑制剂，对人 AChE、MAO-B 和MAO-A 的IC50分别为 0.0248、0.0409 和 0.1108 μM。

MAO A HSP90-IN-1 (4-b) 是一种针对MAO A和HSP90的双重抑制剂，展现在恶性胶质瘤GL26细胞上的IC50为1.77 μM，针对HSP90α的IC50为0.019 μM。该化合物能够通过抑制MAO A活性和HSP90结合，以及降低HER2和phospho-Akt表达，进而抗击恶性胶质瘤（GMB）。同时，MAO A HSP90-IN-1 (4-b)可减少PD-L1的表达，从而降低T细胞活化的抑制，有望用来抑制肿瘤的免疫逃逸。该化合物适用于脑肿瘤相关疾病研究。

5-HT6R MAO-B modulator 1 是一种 5-HT6R 在 Gs 信号传导处的拮抗剂和不可逆的MAO-B 抑制剂，表现出胶质保护活性。5-HT6R MAO-B modulator 1 对东莨菪碱诱导的记忆缺陷表现出诱导作用。

MAO-B ligand-1 is a selective MAO-B inhibitor.

MAO-A inhibitor1 (compound VIII) 作为一种有效的MAO-A抑制剂，展现出了100 μM的IC50值。

MAO-B-IN-5 是一种有效的、选择性和具有口服活性的MAO-B 抑制剂，IC50值为 0.204 μM。MAO-B-IN-5 在帕金森病 (PD) 中具有研究潜力。

MAO-B-IN-8是一种高效且可逆的单胺氧化酶-B(MAO-B)抑制剂，同时也能抑制微胶质细胞产生的神经炎症介质。该化合物专为神经退行性疾病相关研究而设计[1]。

ORY-1001 is a KDM1A inhibitor (IC50 <20nM) with high selectivity against related FAD dependent aminoxidases (MAO-A B, IL4I1, KDM1B >100uM, SMOX 7uM). Treatment of THP-1 (MLL-AF9) cells with ORY-1001, results in a time dose dependent me2H3K4 accumulation a

N-Desbutyl dronedarone is an active metabolite of the antiarrhythmic agent dronedarone .1,2,3It is formed from dronedarone by cytochrome P450s (CYPs) and monoamine oxidase (MAO) in human hepatocyte preparations.4N-Desbutyl dronedarone inhibits the binding of 3,3’,5-triiodo-L-thyronine to the thyroid hormone receptors TRα1and TRβ1(IC50s = 59 and 280 μM for the chicken and human receptors, respectively).1It inhibits CYP2J2-mediated formation of 14,15-EET from arachidonic acid and soluble epoxide hydrolase-mediated formation of 14,15-DHET from 14,15-EET (IC50s = 1.59 and 2.73 μM, respectively, in cell-free assays).2N-Desbutyl dronedarone decreases intracellular ATP levels in H9c2 rat cardiomyocytes (IC50= 1.07 μM) and inhibits mitochondrial complex I, also known as NADH dehydrogenase, and mitochondrial complex II, also known as succinate dehydrogenase, activities in isolated rat heart mitochondria (IC50s = 11.94 and 24.54 μM, respectively).3 1.Van Beeren, H.C., Jong, W.M.C., Kaptein, E., et al.Dronerarone acts as a selective inhibitor of 3,5,3’-triiodothyronine binding to thyroid hormone receptor-α1: in vitro and in vivo evidenceEndocrinology144(2)552-558(2003) 2.Karkhanis, A., Tram, N.D.T., and Chan, E.C.Y.Effects of dronedarone, amiodarone and their active metabolites on sequential metabolism of arachidonic acid to epoxyeicosatrienoic and dihydroxyeicosatrienoic acidsBiochem. Pharmacol.146188-198(2017) 3.Karkhanis, A., Leow, J.W.H., Hagen, T., et al.Dronedarone-induced cardiac mitochondrial dysfunction and its mitigation by epoxyeicosatrienoic acidsToxicol. Sci.163(1)79-91(2018) 4.Klieber, S., Arabeyre-Fabre, C., Moliner, P., et al.Identification of metabolic pathways and enzyme systems involved in the in vitro human hepatic metabolism of dronedarone, a potent new oral antiarrhythmic drugPharmacol. Res. Perspec.2(3)e00044(2014)

Erythromycin 2'-propionate is a macrolide antibiotic and an esterified form of erythromycin .1It is active againstS. aureuswhen used at a concentration of 1 μg/ml. Erythromycin 2'-propionate (1 mM) inhibits protein synthesis in a cell-free assay. 1.Tardrew, P.L., Mao, J.C.H., and Kenney, D.Antibacterial activity of 2'-esters of erythromycinAppl. Microbiol.18(2)159-165(1969)

Connexin43 mimetic peptide. Reduces swelling, astrogliosis, neuroinflammation and neuronal cell death following spinal cord injury ex vivo and in vivo. Exhibits analgesic effects in models of neuropathic pain. O'Carroll et al (2008) Connexin 43 mimetic peptides reduce swelling, astrogliosis and neuronal cell death after spinal cord injury. Cell.Commun.Adhes. 15 27 PMID:18649176 |Mao et al (2017) Characterisation of Peptide5 systemic administration for treating traumatic spinal cord injured rats. Exp.Brain.Res. 235 3033 PMID:28725925 |Kim et al (2017) Characterising the mode of action of extracellular Connexin43 channel mimetic peptides in an in vitro ischemia injury model. Biochem.Biophys.Acta. 1861 68 PMID:27816754 |Tonkin et al (2017) Attenuation of mechanical pain hypersensitivity by treatment with Peptide5, a connexin-43 mimetic peptide, involves inhibition of NLRP3 inflammasome in nerve-injured mice. Exp.Neurol. 300 1 PMID:29055716

Rasagiline-13C3is intended for use as an internal standard for the quantification of rasagiline by GC- or LC-MS. Rasagiline is an inhibitor of monoamine oxidase B (MAO-B; IC50= 4.43 nM for the rat brain enzyme).1It is selective for MAO-B over MAO-A (IC50= 412 nM for the rat brain enzyme). It inhibits serum and NGF withdrawal-induced apoptosis of PC12 cells when used at concentrations ranging from 0.01 to 100 μM.2Rasagiline inhibits rat brain MAO-Bin vivo(ED50= 0.1 mg kg).1It reduces cerebral edema in a mouse model of traumatic brain injury.2Rasagiline (0.1 mg kg) reduces cortical and hippocampal levels of full-length and soluble amyloid precursor protein (APP) in rats and mice. It also reduces α-synuclein-induced substantia nigral neuron loss and improves motor dysfunction in a mouse model of Parkinson's disease.3Formulations containing rasagiline have been used in the treatment of Parkinson's disease. 1.Youdim, M.B.H., Gross, A., and Finberg, J.P.Rasagiline [N-propargyl-1R(+)-aminoindan], a selective and potent inhibitor of mitochondrial monoamine oxidase BBrit. J. Pharmacol.132(2)500-506(2001) 2.Youdim, M.B.H., and Weinstock, M.Molecular basis of neuroprotective activities of rasagiline and the anti-Alzheimer drug TV3326 [(N-propargyl-(3R) aminoindan-5-YL)-ethyl methyl carbamate]Cell. Mol. Neurobiol.21(6)555-573(2001) 3.Kang, S.S., Ahn, E.H., Zhang, Z., et al.α-Synuclein stimulation of monoamine oxidase-B and legumain protease mediates the pathology of Parkinson's diseaseEMBO J.37(12)e98878(2018)

CAY10680 is a dopamine-sparing, benzothiazinone compound that selectively inhibits both MAO-B activity (IC50 = 34.9 nM in human) and adenosine A2A receptors (Ki = 39.5 nM in human). It demonstrates significantly less potent inhibitory values for other adenosine receptor subtypes (Kis > 1 μM) and MAO-A (IC50 ≥ 10 μM). At 1-20 μM, CAY10680 has been shown to abolish cAMP accumulation in CHO cells transfected with adenosine A2A receptors. In the central nervous system adenosine A2A receptor expression is localized to dopamine-innervated areas where heteromeric complexes are formed with dopamine D2 receptors. Because inhibition of adenosine A2A receptors has been shown to enhance D2 receptor function, the blockade of adenosine A2A receptors has emerged as a potential treatment for Parkinson's disease. An additional strategy in the treatment of Parkinson's disease has been to block the activity of monoamine oxidase B (MAO-B), the enzyme involved in dopamine catabolism.

Desmethoxyyangonin (5,6-Dehydrokavain) 是一种MAO-B 可逆性抑制剂。

Pivalylbenzhydrazine (Pivhydrazine) 是一种有效的单胺氧化酶 (MAO) 抑制剂。Pivalylbenzhydrazine 会降低正常大鼠的软骨生长。Pivalylbenzhydrazine 可用于抑郁症的研究。

Safrazine 是一种不可逆的、非特异性的、具有口服活性的单胺氧化酶 (MAO) 抑制剂。Safrazine 可用于抑郁症的研究。

LSD1-IN-12 (compound 2) 是有效的 LSD1抑制剂，Ki 值分别为 1.1 μM (LSD1), 61 μM (LSD2), 2.3 μM (MAO-A), 和 3.5 μM (MAO-B)。