Neurociência

<p>CEase-IN-1 (A1H3), potent CEase inhibitor, IC50 0.36μM, for hypercholesterolemia study.</p>

SB 243213 hydrochloride is an orally active, selective and high-affinity antagonist of 5-hydroxytryptamine (5-HT)2C receptor(pKi of 9.37 and a pKb of 9.8).It

<p>Zanapezil is an acetylcholinesterase (AChE) inhibitor. Zanapezil increases choline acetyltransferase activity in cultured rat septal cholinergic neurons.</p>

<p>Serotonin hydrogen maleate serves as a monoaminergic neurotransmitter and an endogenous 5-HT receptor agonist within the central nervous system (CNS). It also functions as an inhibitor of catechol O-methyltransferase (COMT), exhibiting a Ki value of 44 μM.</p>

<p>SB 258741 hydrochloride is a potent antagonist of the 5-HT 7 receptor, designed specifically for studying schizophrenia [1].</p>

<p>(+)-Cevimeline HCl hemihydrate is a muscarinic agonist for dry mouth in Sjogren's with rapid absorption, differing metabolism in species.</p>

<p>DL-Thyroxine is a thyroid hormone that acts as a monoamine oxidase (monoamine oxidase) inhibitor.</p>

<p>AM9405: peripheral CB1/5-HT3 agonist, suppresses gut motility, relieves GI disorder symptoms in mice.</p>

<p>Subtype-selective nicotinic agonist</p>

<p>P2X4 antagonist-1 is a potent P2X4 receptor antagonist used in the study of neurological, cardiovascular, and immune system diseases.</p>

<p>LRRK2-IN-5 is an oral, BBB-penetrating selective inhibitor for LRRK2 with IC50s: 1.2μM (GS) and 16μM (WT); halts LRRK2 autophosphorylation.</p>

<p>PXS-5153A is an oral, fast-acting LOXL2/3 inhibitor with IC50 &lt;40 nM for LOXL2 and 63 nM for LOXL3, potentially treating fibrosis.</p>

<p>Compound 16 (hAChE/Aβ1-42-IN-1) is a potent inhibitor targeting both hAChE and Aβ1-42 aggregation, demonstrating considerable safety in hepG2 cell lines and</p>

<p>AM-6494 is a potent and orally active BACE1 inhibitor (IC50: 0.4 nM) with in vivo selectivity over BACE2 (IC50: 18.6 nM).</p>

<p>ChE/Aβ1-42-IN-1 (compound 28) is a potent aggregation inhibitor of ChE and Aβ 1-42 with excellent BBB permeability.</p>

BACE1-IN-4 is a potent and highly selective BACE1 inhibitor (IC50: 3.8 nM; Ki: 1.9 nM), more selective at BACE1 over BACE2.

<p>Tebideutorexant, an orexin-1 receptor antagonist, shows anti-panic effects in rodents and humans, providing a tool for stress response and psychiatric research.</p>

<p>AChE-IN-63 (Compound 5AD) serves as a selective inhibitor of hAChE, exhibiting an IC 50 value of 0.103 μM. Moreover, it inhibits hBChE and hBACE-1 with IC 50 values of 10 μM and 1.342 μM, respectively. AChE-IN-63 is effective in inhibiting Aβ aggregation and preventing the formation and deposition of Aβ1-42. It can effectively penetrate the blood-brain barrier and is orally bioavailable. This compound is primarily utilized in research related to Alzheimer's disease [1].</p>

<p>Compound AV-2, also known as AChE/Aβ-IN-5, is a bifunctional inhibitor that acts on AChE and auto-induced Aβ (Amyloid-β) aggregation. This compound has demonstrated significant efficacy in mitigating cognitive impairment in mice induced by scopolamine and Aβ [1].</p>

<p>AChE-IN-10 (24r) inhibits AChE (IC50=2.4 nM), reducing amyloid buildup, tau phosphorylation, and promotes neuron health.</p>

<p>K027 is a potent organophosphate (OP) inhibitor of acetylcholinesterase (AChE) reactivation. k027 can be used to study Alzheimer's disease.</p>

LY3020371 HCl: potent mGlu2/3 antagonist, antidepressant-like; Ki: 5.3/2.5 nM, IC50: 16.2 nM for cAMP inhibition.

<p>LRRK2-IN-2: selective, potent LRRK2 inhibitor, IC50 of 0.6 nM, oral, crosses blood-brain barrier, for Parkinson's research.</p>

MAO-B-IN-28 (compound 10e) is a potent hMAO-B inhibitor with an IC50 value of 1.9±0.5 nM, potentially serving as a candidate molecule for neurodegenerative disease research.

<p>Aβ aggregation-IN-1 (Compound 1b) is an inhibitor of amyloid-beta precursor protein. It suppresses the aggregation and disaggregation of amyloid-beta fibrils with IC50 values of 3.92 and 7.19 M, respectively. Additionally, Aβ aggregation-IN-1 reduces malondialdehyde formation in neuronal cells, increases intracellular levels of reduced glutathione (GSH), and inhibits caspase 3.</p>

<p>Anti-Aβ agent 1A is a potent anti-amyloid-β agent.</p>

<p>5-IAI hydrochloride is a psychoactive analog of para-iodoamphetamine. 5-IAI hydrochloride significantly reduces serotonin uptake sites and hippocampal serotonin levels in rats.</p>

<p>Ro4368554 is a selective 5-HT6 antagonist capable of crossing the blood-brain barrier. It can reverse memory deficits caused by scopolamine and tryptophan depletion. Ro4368554 is applicable for research related to memory impairments.</p>

hAChE-IN-10 (Compound ET11) is an inhibitor of human acetylcholinesterase (AChE) with an IC50 of 6.34 nM. This compound is capable of scavenging free radicals and exhibits antioxidant activity. Additionally, hAChE-IN-10 demonstrates metal-chelating properties, inhibiting Cu2+-induced Aβ1-42 aggregation, reducing amyloid plaque formation, and offering neuroprotective effects. It also ameliorates cognitive impairment in mice induced by Scopolamine.

<p>Geissoschizoline inhibits human AChE/BChE (IC50: 20.40/10.21 µM) and has anti-inflammatory properties.</p>

<p>VU6005806 is a potent M4 PAM with EC50s: 94 nM (human), 28 nM (rat), 87 nM (dog), 68 nM (cyno); studied for neuropsychiatric disorders.</p>

<p>Elzasonan hydrochloride is a serotonin 1B and serotonin 1D receptor antagonist. It is utilized in the study of depression.</p>

<p>hMAO-B-IN-10 (compound 7) is an inhibitor of MAO-A/B with IC50 values of 424.1 nM and 177.9 nM, respectively. It has demonstrated neuroprotective effects in the MPTP-induced mouse model of Parkinson's Disease (PD).</p>

<p>Desmethylflunitrazepam (Norflunitrazepam) is a benzodiazepine derivative and an active metabolite of Flunitrazepam.</p>

<p>Tiprenolol hydrochloride is a β-adrenoceptor (β-adrenoceptor) antagonist. This compound is effective in eliminating ventricular arrhythmias in dogs caused by intravenous administration of adrenaline, following inhalation of halothane.</p>

<p>Tuclazepam (KC 1956) is a derivative of the benzodiazepine class of drugs, exhibiting anti-anxiety and sedative properties.</p>

<p>SGE516: neuroactive steroid, enhances GABAA, lowers neuronal activity, protects from seizures.</p>

Designed anti-Alzheimer’s compound; potent Glutaminyl Cyclase inhibitor; IC50 at 4.5 nM; reduces brain Aβ; improves cognition.

<p>Lu 26-046 is a muscarinic receptor agonist.</p>

Remlifanserin is a potent inverse agonist of the serotonin receptor (5-HT2A).

<p>DAPM (gamma-Secretase Inhibitor XVI) is a Notch pathway inhibitor with anticancer activity and antiproliferative effects.</p>

<p>Notch inhibitor 1 blocks Notch 1/3 (IC50: 7.8/8.5 nM) and aids cancer research.</p>

<p>BChE-IN-38 (compound 13) is a potent BChE inhibitor, with Ki values of 62.05, 28.78, 14.09, and 1.15 nM for hCAI, hCAII, AChE, and BChE, respectively. BChE-IN-38 also demonstrates cytotoxic activity.</p>

<p>2,6-Dimethoxybenzylamine hydrochloride (Compound 5) exhibits reversible inhibitory activity against copper amine oxidase (CAO) and inhibits benzylamine oxidase (BAO) and monoamine oxidase B (MAO B) with IC50 values of 120 μM and 190 μM, respectively.</p>

FP0429 is an agonist of mGlu4.

<p>PF-06648671 is a γ-secretase modulator for the treatment of neurodegenerative and/or neurological disorders.</p>

<p>AChE/BChE-IN-3 (BMC-1) HCl is a dual inhibitor with IC50s: eqBChE 0.383 μM, elAChE 6.08 μM.</p>

<p>5-HT6R/MAO-B modulator 1 blocks 5-HT6R and permanently inhibits MAO-B, protects glial cells, and reverses memory loss.</p>

<p>LY367385 hydrochloride: selective mGluR1a antagonist, IC50 = 8.8 μM, neuroprotective, anticonvulsant, antiepileptic.</p>

<p>MAO-B-IN-42 (Compound 4f) is a selective and reversible monoamine oxidase-B (MAO-B) inhibitor, with an IC50 value of 0.184 μM. By blocking the oxidative deamination of monoamines catalyzed by MAO-B, it helps maintain neurotransmitter levels. MAO-B-IN-42 shows potential for research into Parkinson's disease.</p>

<p>BACE1-IN-2 is a BACE1 inhibitor (IC50: 22 nM).</p>

<p>AChE-IN-11 aids Alzheimer's research, has neuroprotection/antioxidant properties (ORAC=2.5), and acts on AChE, MAO-B, BACE1 with IC50 values of 7.9-9.9 μM.</p>

<p>DSP-1053: Benzylpiperidine-based, potent SERT inhibitor (Ki=1.02nM), partial 5-HT1A receptor agonist (Ki=5.05nM), antidepressant.</p>

<p>Compound B15, a potent α7 nAChR antagonist, IC50 = 3.3 μM, promising for research on schizophrenia, Alzheimer's, and inflammation.</p>

<p>(9R)-RO7185876 (Compound example 16) is a γ-secretase inhibitor. It reduces the secretion of Αβ42. This compound can be employed in the research of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, multi-infarct dementia, senile dementia, or Down syndrome.</p>

<p>AChE/BACE1/GSK3β-IN-1 is an orally active, blood-brain barrier-transparent, moderately bioavailable triple inhibitor of AChE/BACE1/GSK3β.</p>

<p>Compound 4c, a potent GABAA agonist with anti-depressive effects in mouse FST/TST, shows promise in depression research.</p>

<p>BChE-IN-2, a pyrimidine/pyridine derivative, potently inhibits BChE (Ki 0.099 μM) and shows promise in AD research.</p>

<p>MAO-B-IN-5: potent, selective oral MAO-B inhibitor, IC50=0.204μM, potential for Parkinson's research.</p>

<p>MAO-B-IN-10: Potent, selective MAO-B inhibitor; crosses blood-brain barrier; IC50 5.3 μM; reduces Aβ aggregation 58.2%, disaggregates 43.3%.</p>

<p>Moxetomidate is a GABAA receptor (GABAA receptor) agonist with hypnotic properties.</p>

<p>Antioxidant agent-8, an oral Aβ 1-42 inhibitor, reduces fibril aggregation &amp; promotes disaggregation; it's neuroprotective &amp; BBB permeable.</p>

<p>Rodatristat ethyl is an oral TPH1 inhibitor reducing 5-HT levels &amp; lowering PAH at low doses.</p>

<p>MAO-B-IN-6 is a selective, potent, orally active MAO-B inhibitor (IC50: 0.019 μM). MAO-B-IN-6 is superior to Safinamide both in vitro and in vivo.</p>

<p>CVN636, a potent and selective allosteric agonist for the mGluR7 receptor, exhibits oral activity and CNS permeability [1], with an EC50 of 7 nM for human</p>

<p>F 14679 is a potent 5-HT1A agonist (pKi=10.23) with a maximum Ca2t response similar to 5-HT.</p>

<p>YM-31636 (free base) is an orally active, potent, and selective agonist of the 5-HT3 receptor with a pKi value of 9.67. This compound induces contraction in isolated guinea pig distal colon and provokes tachycardia in isolated guinea pig right atrium, demonstrating a relative intrinsic activity of about 0.23. YM-31636 (free base) holds potential for research in constipation management.</p>

<p>MAO-A inhibitor3 (Compound 360) is an MAO-A inhibitor with an IC50 greater than 100 μM. It is utilized in the investigation of neurological disorders.</p>

<p>PTCA is a potent ligand for Ca2+/calmodulin-dependent protein kinase II α (CaMKIIα), with a pKi value of 7.2.</p>

<p>MMB-4 is an oxime that can reactivate cholinesterases (cholinesterases) which have been inactivated due to exposure to organophosphates such as Sarin or Soman.</p>

<p>Beloxepin is an oral dual selective inhibitor of serotonin and norepinephrine uptake.</p>

<p>Metoquizine is an anticholinergic compound. It is a muscarinic acetylcholine receptor antagonist that has been used to treat ulcers.</p>

<p>benzodiazepine receptor antagonist,competitive</p>

Azotomycin is an antagonist of L-glutamine and may be used as an immunosuppressant.

<p>Revexepride, a 5-HT4 agonist, may boost CYP3A4, used for treating GERD.</p>

<p>Poskine is an anticholinergic and central nervous system depressant. It is utilized in research related to Parkinson's disease and motion sickness.</p>

<p>5-HT2A and 2C receptor antagonist</p>

RO-1-5237, a cholinergic compound and a metabolic product of Pyridostigmine Bromide, is utilized in research for myasthenia gravis.

<p>AChE-IN-22 (10q) selectively inhibits AChE (IC50: 0.88 μM), less on BuChE (IC50: 10 μM), targets CAS and PAS, useful in Alzheimer's research.</p>

<p>LB-102 is an orally active inhibitor of dopamine D2, D3, and serotonin 5-HT7 receptors, utilized in the study of schizophrenia and other psychiatric disorders.</p>

<p>NB-360: potent, brain-penetrant BACE1/2 inhibitor; IC50s: 5-6 nM; high selectivity vs pepsin, cathepsin E/D.</p>

<p>Iclepertin (BI-425809) is a GlyT1 inhibitor.Iclepertin is used for the treatment of Alzheimer;s disease and other CNS disorders.</p>

BDZ-g: potent, selective AMPA receptor antagonist; useful for researching neurological disorders.

<p>AChE/BChE-IN-10 inhibits AChE/BChE (IC50: 0.176/0.47 μM), crosses the blood-brain barrier, and prevents Aβ-aggregation.</p>

<p>BMS 299897, a sulfonamide γ-secretase inhibitor, inhibits Aβ production with an IC50 of 7 nM in HEK293 cells overexpressing APP.</p>

<p>LY2979165 (mGlu2 agonist) is an orthosteric agonist of mGluR2 and can be used in studies about serving as an anti-depressant.</p>

<p>SB-224289 hydrochloride (SB-224289A) is a selective antagonist of 5-HT1B receptor, with anxiolytic effect.</p>

<p>AChE-IN-26 (compound 4a) is an AChE (acetylcholinesterase) inhibitor (IC50: 0.42 μM).</p>

<p>Umibecestat inhibits human and mouse BACE-1 (IC50: 11 nM &amp; 10 nM), potentially for Alzheimer's research.</p>

<p>Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol also shows potency for inhibiting the binding of the radioligand [125I-ICYP] to [5HT1B-serotonergic] receptor sites. It is an antihypertensive agent.</p>

<p>(S)-Rasagiline is rasagiline S-isomer, and is an agent of anti-Parkinson.</p>

<p>7-Desmethyl-agomelatine, a metabolite of Agomelatine, exhibits lower activity than Agomelatine, which functions as a melatonergic (MT1 and MT2) agonist and 5-HT2C antagonist.</p>

Xanthocillin X permethyl ether, a natural product extracted from fungal sources, exhibits Aβ-42 lowering activity.

(-)-Bicuculline methobromide is a potent antagonist of GABAA receptor .

group II metabotropic glutamate receptor antagonist

<p>Pumosetrag Hydrochloride is an orally available 5-HT3 partial agonist. It is developed for the treatment of irritable bowel syndrome and gastroesophageal reflux disease.</p>

<p>(Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial the 5-HT1A receptor agonist.</p>

mGlu1 receptor antagonist

Eglumegad is a highly effective and selective agonist of group II (mGlu2/3) receptor (IC50s: 5 and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively).

neuronal α7 nAChR antagonist

<p>BF 227 is a candidate for an amyloid imaging probe for PET [Ki: 4.3 nM for Aβ1-42 fibrils].</p>

SB-399885 hydrochloride is an antagonist of 5-HT6 receptor.

<p>The test principle applied in this kit is Sandwich enzyme immunoassay. The microtiter plate provided in this kit has been pre-coated with an antibody specific to Rat NT3. Standards or samples are added to the appropriate microtiter plate wells then with a biotin-conjugated antibody specific to Rat NT3. Next, Avidin conjugated to Horseradish Peroxidase (HRP) is added to each microplate well and incubated. After TMB substrate solution is added, only those wells that contain Rat NT3, biotin-conjugated antibody and enzyme-conjugated Avidin will exhibit a change in color. The enzyme-substrate reaction is terminated by the addition of sulphuric acid solution and the color change is measured spectrophotometrically at a wavelength of 450nm ± 10nm. The concentration of Rat NT3 in the samples is then determined by comparing the OD of the samples to the standard curve.</p>