Neurociência

<p>AChE-IN-84 (compound 21) is an inhibitor of AChE.</p>

benzodiazepine receptor antagonist,competitive

25B-NBOH hydrochloride is a phenethylamine that exhibits high affinity for serotonin (5-HT) receptors 5-HT2A and 5-HT2C, with pKi values of 8.3 and 9.4, respectively.

D3/5-HT receptor modulator-1 (compound 5i) is a selective antagonist of the dopamine D3 and 5-HT2A receptors, and a partial agonist at the 5-HT1A receptor. It exhibits Ki values of 4.5 nM, 11.9 nM, and 15.3 nM for the dopamine D3, 5-HT2A, and 5-HT1A receptors respectively. The compound shows lower affinity for the dopamine D2 receptor, 5-HT2C receptor, and hERG channel. D3/5-HT receptor modulator-1 possesses atypical antipsychotic properties.

LY593093 is a selective partial orthosteric agonist of M1 muscarinic acetylcholine receptor.

LY2794193, a potent and selective mGlu3 receptor agonist, reduces akathisia seizures and increases GAT1, GLAST and GLT-1 protein levels in rats.

LRRK2-IN-20 (EX. 4.64) is a selective inhibitor of LRRK2 with a potency of pIC50 at 0.7921 nM. This compound is applicable in research studies focused on Parkinson's Disease (PD).

5-HT1A antagonist; Ki=8nM, Kb=0.04nM. PDE4B IC50=80.4μM; PDE7A IC50=151.3μM. Good biofilm penetration, stable, anticognitive, antidepressant.

YM-202074: Selective mGlu1 antagonist, binds allosteric site (Ki=4.8 nM), inhibits mGlu1 (IC50=8.6 nM).

OX2R agonist 1 is an OX2R activator with an EC50 of less than 100 nM. It is utilized in research related to narcolepsy and cataplexy.

Thiomuscimol hydrobromide is an agonist of GABAA receptor.

EF1502 is a potent and selective GABA transporter inhibitor.

SRI-31255 is an orally active LRRK2 inhibitor, with IC50 values of 520 nM for human wild-type (WT) and 427 nM for the G2019S mutant. It inhibits kinase activity by binding to the ATP-binding pocket of LRRK2, providing neuroprotective effects. SRI-31255 serves as a lead compound for developing LRRK2-targeted therapies for Parkinson’s disease research.

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

Pareptide monohydrochloride is a metabolically stable analog of melatonin inhibitor (MIF).

Refisolone is an antagonist of the GABAA receptor.

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

LY367385 hydrochloride: selective mGluR1a antagonist, IC50 = 8.8 μM, neuroprotective, anticonvulsant, antiepileptic.

Norneostigmine is a potent inhibitor of AChE capable of crossing the blood-brain barrier. When administered to mice, it achieves a 50% inhibition rate of brain AChE activity within 10 minutes, comparable to the effect of Tetrahydroaminoacridine (57% inhibition in 10 minutes). Norneostigmine is applicable in research on Alzheimer's disease and other memory-related disorders.

Anti-Aβ agent 1A is a potent anti-amyloid-β agent.

Beloxepin is an oral dual selective inhibitor of serotonin and norepinephrine uptake.

MAO-B-IN-44 (Compound 4n) is a selective inhibitor of monoamine oxidase B (MAO-B) with an IC50 of 1.01 μM, demonstrating weak inhibition of MAO-A (IC50=14.4 μM). It reduces the degradation of neurotransmitters like dopamine and holds potential for research into neurodegenerative diseases such as Parkinson's disease, which are associated with MAO-B abnormalities.

LRRK2-IN-13 (Compound 13), with an IC50 value of 0.57 nM, serves as an inhibitor of LRRK2 and exhibits properties that allow it to penetrate the brain [1].

LRRK2-IN-14 (Compound 8), an orally active inhibitor of LRRK2, exhibits an IC 50 of 6.3 nM against LRRK2(G2019S) cell activity and demonstrates inhibitory effects on hERG with an IC 50 of 22 μM. Additionally, LRRK2-IN-14 is permeable to the blood-brain barrier [1].

(R,R)-LRRK2-IN-7 is an isomer of LRRK2-IN-7, a potent and selective LRRK2 kinase inhibitor with CNS penetrance. It exhibits an IC50 of 0.9 nM and demonstrates over 1000-fold selectivity compared to other kinases, ion channels, and CYP enzymes.

<p>(R)-Norfluoxetine is the (R)-enantiomer of Norfluoxetine. It functions as a potent serotonin reuptake inhibitor, with a Ki value of 13 nM. This compound is utilized in the research of depression.</p>

metabotropic glutamate receptor type 1 (mGlu1) antagonist

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

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

Aβ42-IN-1, compound 1v, is a novel, potent and orally active γ-secretase modulator (GSM).

5-HT2A receptor agonist-8 (compound 8) is a potent 5-HT2A receptor agonist with an EC50 of 0.6784 nM. It is suitable for research related to depression and bipolar disorder.

AChE/BChE-IN-19 (compound 12) is a nicotinic hydrazine derivative that acts as an inhibitor of AChE (IC50=21.45 nM) and BChE (IC50=18.42 nM), and it is applicable in Alzheimer's disease research.

p-F-HHSiD (p-Fluorohexahydrosiladifenidol) hydrochloride is a selective M3mAChR antagonist. It is capable of inhibiting acetylcholine-mediated vasodilation in human umbilical vein endothelial cells (HUVEC).

CaMKK2-IN-1 is a selective and potent inhibitor of CaMKK2, exhibiting an IC50 of 7 nM.

Aprindine, an arrhythmia inhibitor, stabilizes the cell membranes of heart muscle cells to prevent abnormal electrical impulses and irregular heartbeats. In hematological toxicity studies, aprindine demonstrated potential inhibitory effects on the replicative capacity of mouse and human blood cells at specific concentrations [1].

<p>AChE-IN-47 (compound g17) is an acetylcholinesterase (AChE) inhibitor with an IC50 of 0.24 μM. It prevents the self-aggregation of β-amyloid peptides and exhibits neuroprotective properties by effectively reducing the accumulation of intracellular reactive oxygen species (ROS).</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>

BF-168 is a candidate probe for PET and specifically recognizes both neuritic and diffuse plaques (Ki: 6.4 nM for Aβ1-42).

5-HT2A receptor agonist-7 (517) functions as a modulator of the 5-HT2A receptor, with an EC50 value of less than 100 nM.

HDAC6-IN-9 is a γ-secretase modulator that can significantly reduce the level of Aβ42 in mouse brain and can be used to study neurological diseases.

GABA-IN-4 (Compound 17) is a derivative of N-(indol-3-ylglyoxylyl)benzylamine. It exhibits high affinity for the benzodiazepine receptor (BzR), the binding site within the GABAA receptor complex, with a Ki value of 67 nM. Benzodiazepines are widely used as anxiolytic, sedative-hypnotic, and anticonvulsant agents.

β-CCM is a benzodiazepine receptor inverse agonist with anxiogenic and convulsant effects. It enhances emotional reactivity and reduces interference sensitivity in spatial working memory tasks. β-CCM is applicable in research related to anxiety disorders.

<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.

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.

Avitriptan is a 5-HT1B/1D receptor agonist with pKi values of 7.44 for 5-HT1Brat, 7.68 for 5-HT1Bhuman, and 8.36 for 5-HT1Dhuman. It can induce contraction in isolated coronary arteries and is used for the treatment of migraines.

LOX-IN-5 tosylate (compound 22) is a selective oral inhibitor of lysyl oxidase-like 2 (LOXL2) with an IC50 of less than 300 nM, and it exhibits anti-fibrotic properties.

MAO-A Inhibitor 1 (compound VIII) acts as a MAO-A inhibitor and exhibits an IC50 value of 100 μM [1].

SNRI-IN-1 (Compound 7a) acts as a dual inhibitor of serotonin and noradrenaline monoamine reuptake, with a P-glycoprotein Efflux Ratio of 20 [1].

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

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

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

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

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

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

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

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).

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

neuronal α7 nAChR antagonist

mGlu1 receptor antagonist

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

group II metabotropic glutamate receptor antagonist

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

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.

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

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>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>

Alfadolone acetate is a gamma-aminobutyric acid (GABA) receptor agonist.

Sarizotan (EMD 128130) is an orally active compound that acts as an agonist for serotonin 5-HT 1A receptors and dopamine receptors, with IC50 values of 6.5 nM for rat 5-HT 1A, 0.1 nM for human 5-HT 1A, 15.1 nM for rat D 2, 17 nM for human D 2, 6.8 nM for human D 3, and 2.4 nM for human D 4.2.

Calmodulin antagonist-1 (W-7) is a calmodulin (CaM) antagonist that effectively inhibits calmodulin-activated Ca 2+ -phosphodiesterase (PDE) with an IC 50 of 28 μM. This compound also competitively inhibits trypsin-treated Ca 2+ -PDE with respect to cyclic GMP, exhibiting an IC 50 of 375 μM and a K i value of 300 μM.

VU0080241 is a positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4).

Desmethyl cariprazine is a Cariprazine active metabolite. Cariprazine, an antipsychotic drug candidate, shows a high affinity for the D3 (Ki: 0.085 nM) and D2 (Ki: 0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (2.6 nM).

Eglumegad (LY354740) hydrochloride is a potent, selective agonist for group II (mGlu2/3) receptors, showing IC50 values of 5 nM for mGlu2 and 24 nM for mGlu3 receptors in transfected human cells. This compound provides neuroprotection against NMDA-induced toxicity and exhibits anxiolytic- and antipsychotic-like properties [1].

Acridine-9-carboxylic acid is a useful organic compound for research related to life sciences. The catalog number is T65511 and the CAS number is 5336-90-3.

VU6000918 is a positive allosteric modulator that targets the muscarinic acetylcholine receptor subtype M4. It exhibits a half maximal effective concentration (EC50) of 19 nM for the human M4 receptor.

BRL 15572 is a useful organic compound for research related to life sciences. The catalog number is T64501 and the CAS number is 734517-40-9.

Physostigmine is a potent and reversible inhibitor of cholinesterase. It is also reported to form a slowly degrading carbamylated enzyme complex with acetylcholinesterase (AChE).

Ebeiedinone, a steroidal alkaloid derived from Fritillaria species, effectively inhibits the activity of human whole blood cholinesterase (ChE) at a concentration of 0.1 mM, resulting in a significant inhibitory effect of 69.0%.

2-AEMP TFA is a potent and rapidly acting antagonist of GABA(A)-ρ1 receptors. 2-AEMP is an analog of GABA.

3-Methylglutaconic acid, a primary metabolite accumulating in 3-Methylglutaconic aciduria (MGTA), induces lipid and protein oxidation, while diminishing non-enzymatic antioxidant defenses in cerebral cortex supernatants, thereby promoting oxidative stress in the cerebral cortex. This compound is utilized in research concerning brain damage diseases [1].

This ELISA kit uses the Sandwich-ELISA principle. The micro ELISA plate provided in this kit has been pre-coated with an antibody specific to Human IFN-α. Samples (or Standards) are added to the micro ELISA plate wells and combined with the specific antibody and biotinylated detection antibody specific for Human IFN-α. Then Avidin-Horseradish Peroxidase (HRP) conjugate are added successively to each micro plate well and incubated. Free components are washed away. The substrate solution is added to each well. Only those wells that contain Human IFN-α, biotinylated detection antibody and Avidin-HRP conjugate will appear blue in color. The enzyme-substrate reaction is terminated by the addition of stop solution and the color turns yellow. The optical density (OD) is measured spectrophotometrically at a wavelength of 450 nm. The OD value is proportional to the concentration of Human IFN-α. You can calculate the concentration of Human IFN-α in the samples by comparing the OD of the samples to the standard curve.

This ELISA kit uses the Sandwich-ELISA principle. The micro ELISA plate provided in this kit has been pre-coated with an antibody specific to Mouse IFN-γ. Samples (or Standards) are added to the micro ELISA plate wells and combined with the specific antibody and biotinylated detection antibody specific for Mouse IFN-γ. Then Avidin-Horseradish Peroxidase (HRP) conjugate are added successively to each micro plate well and incubated. Free components are washed away. The substrate solution is added to each well. Only those wells that contain Mouse IFN-γ, biotinylated detection antibody and Avidin-HRP conjugate will appear blue in color. The enzyme-substrate reaction is terminated by the addition of stop solution and the color turns yellow. The optical density (OD) is measured spectrophotometrically at a wavelength of 450 nm. The OD value is proportional to the concentration of Mouse IFN-γ. You can calculate the concentration of Mouse IFN-γ in the samples by comparing the OD of the samples to the standard curve.

This ELISA kit uses the Sandwich-ELISA principle. The micro ELISA plate provided in this kit has been pre-coated with an antibody specific to Mouse IL-9. Samples (or Standards) are added to the micro ELISA plate wells and combined with the specific antibody and biotinylated detection antibody specific for Mouse IL-9. Then Avidin-Horseradish Peroxidase (HRP) conjugate are added successively to each micro plate well and incubated. Free components are washed away. The substrate solution is added to each well. Only those wells that contain Mouse IL-9, biotinylated detection antibody and Avidin-HRP conjugate will appear blue in color. The enzyme-substrate reaction is terminated by the addition of stop solution and the color turns yellow. The optical density (OD) is measured spectrophotometrically at a wavelength of 450 nm. The OD value is proportional to the concentration of Mouse IL-9. You can calculate the concentration of Mouse IL-9 in the samples by comparing the OD of the samples to the standard curve.

This ELISA kit uses the Sandwich-ELISA principle. The micro ELISA plate provided in this kit has been pre-coated with an antibody specific to Mouse GROα/CXCL1. Samples (or Standards) are added to the micro ELISA plate wells and combined with the specific antibody and biotinylated detection antibody specific for Mouse GROα/CXCL1. Then Avidin-Horseradish Peroxidase (HRP) conjugate are added successively to each micro plate well and incubated. Free components are washed away. The substrate solution is added to each well. Only those wells that contain Mouse GROα/CXCL1, biotinylated detection antibody and Avidin-HRP conjugate will appear blue in color. The enzyme-substrate reaction is terminated by the addition of stop solution and the color turns yellow. The optical density (OD) is measured spectrophotometrically at a wavelength of 450 nm. The OD value is proportional to the concentration of Mouse GROα/CXCL1. You can calculate the concentration of Mouse GROα/CXCL1 in the samples by comparing the OD of the samples to the standard curve.

This ELISA kit uses the Sandwich-ELISA principle. The micro ELISA plate provided in this kit has been pre-coated with an antibody specific to Human IL-6. Samples (or Standards) are added to the micro ELISA plate wells and combined with the specific antibody and biotinylated detection antibody specific for Human IL-6. Then Avidin-Horseradish Peroxidase (HRP) conjugate are added successively to each micro plate well and incubated. Free components are washed away. The substrate solution is added to each well. Only those wells that contain Human IL-6, biotinylated detection antibody and Avidin-HRP conjugate will appear blue in color. The enzyme-substrate reaction is terminated by the addition of stop solution and the color turns yellow. The optical density (OD) is measured spectrophotometrically at a wavelength of 450 nm. The OD value is proportional to the concentration of Human IL-6. You can calculate the concentration of Human IL-6 in the samples by comparing the OD of the samples to the standard curve.

This ELISA kit uses the Sandwich-ELISA principle. The micro ELISA plate provided in this kit has been pre-coated with an antibody specific to Mouse IL-17A. Samples (or Standards) are added to the micro ELISA plate wells and combined with the specific antibody and biotinylated detection antibody specific for Mouse IL-17A. Then Avidin-Horseradish Peroxidase (HRP) conjugate are added successively to each micro plate well and incubated. Free components are washed away. The substrate solution is added to each well. Only those wells that contain Mouse IL-17A, biotinylated detection antibody and Avidin-HRP conjugate will appear blue in color. The enzyme-substrate reaction is terminated by the addition of stop solution and the color turns yellow. The optical density (OD) is measured spectrophotometrically at a wavelength of 450 nm. The OD value is proportional to the concentration of Mouse IL-17A. You can calculate the concentration of Mouse IL-17A in the samples by comparing the OD of the samples to the standard curve.

This ELISA kit uses the Sandwich-ELISA principle. The micro ELISA plate provided in this kit has been pre-coated with an antibody specific to Mouse TNF-α. Samples (or Standards) are added to the micro ELISA plate wells and combined with the specific antibody and biotinylated detection antibody specific for Mouse TNF-α. Then Avidin-Horseradish Peroxidase (HRP) conjugate are added successively to each micro plate well and incubated. Free components are washed away. The substrate solution is added to each well. Only those wells that contain Mouse TNF-α, biotinylated detection antibody and Avidin-HRP conjugate will appear blue in color. The enzyme-substrate reaction is terminated by the addition of stop solution and the color turns yellow. The optical density (OD) is measured spectrophotometrically at a wavelength of 450 nm. The OD value is proportional to the concentration of Mouse TNF-α. You can calculate the concentration of Mouse TNF-α in the samples by comparing the OD of the samples to the standard curve.