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。

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-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-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-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]。

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。

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)。

hMAO-B MB-COMT-IN-1 是 MAO-B MB-COMT 的双重抑制剂，对 hMAO-B 的IC50值为 2.5 μM，对MB-COMT 的IC50值为 3.84 μM。hMAO-B MB-COMT-IN-1 能保护细胞免受氧化损伤，可用于神经退行性疾病，如帕金森病 (PD)等的研究。

HIF-1α-IN-5 是 HIF-1α的抑制剂，在 HEK293T 细胞中的 IC50值为 24 nM，也可抑制 MAO-A 的活性。 在缺氧条件下， HIF-1α-IN-5可下调 VEGF 和 PDK1 mRNA 的表达。HIF-1α-IN-5 具有用于癌症研究的潜力。

MAO-B-IN-15 是一种MAO-B 的选择性抑制剂，可与 Tyr 326 残基形成 π-π 相互作用，IC50 值为 13.5 μM。它可被用于研究帕金森病。

SSAO inhibitor-2 (Compound 1) 可用于动脉粥样硬化、糖尿病及其并发症、肥胖、中风、慢性肾病、视网膜病变、慢性阻塞性肺病 (COPD)、自身免疫性疾病、多发性硬化等的研究。SSAO inhibitor-2 是氨基脲敏感性胺氧化酶 (SSAO) 抑制剂，其对人 SSAO 和 MAO-A 的IC50分别为 <10 nM 和 10-100 μM。

MAO-B-IN-13 (compound 12a) 是一种高效、可逆和血脑屏障(BBB)渗透性的MAO-B 抑制剂 (IC50 = 10 nM)。MAO-B-IN-13 显示出神经保护和抗氧化活性， 可用于研究帕金森病。

MAO-B-IN-16 是单胺氧化酶 B (MAO-B) 的选择性抑制剂 (IC 50 = 1.55 μM)，可用于中枢神经疾病研究，例如帕金森病。

Monoamine Oxidase B inhibitor 1 是一种可逆、口服有效和选择性的单胺氧化酶 B 抑制剂 (IC50 = 0.02 nM)，可以穿过血脑屏障 (BBB)。Monoamine Oxidase B inhibitor 1 显示出抗氧化和抗神经炎症活性，可用于研究帕金森病。