Neurociência

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.

<p>BRD0418 acts as an upregulator of TRIB1 expression by leading to reprogramming of hepatic lipoprotein metabolism from adipogenesis to clearance it.</p>

Subtype-selective nicotinic agonist

SZ1676 is a derivative of SZ1677, which is an agent of neuromuscular blocking.

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

Sulamserod hydrochloride is a 5-HT4 receptor antagonist. It is utilized in research related to gastrointestinal disorders.

<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>

Jimscaline (compound R-(-)2) is a 5-HT2A agonist and a mescaline analogue, used in neuroscience research.

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

CTW0404 is an effective positive allosteric modulator (PAM) of the 5-HT receptor, with promising implications for research into neuropsychiatric disorders.

Thiazolo[5,4-c]pyridin-4(5H)-one is a compound used for diagnostic imaging of TDP-43, in PET imaging of neurodegenerative diseases ALS、AD、FTD、LATE.

VU6016235 is a structurally unique, orally available, and highly selective tricyclic M4 muscarinic acetylcholine receptor positive allosteric modulator.

Amyloid-β-IN-2 (Compound EX.112) is a selective inhibitor of γ-secretase. In H4 cells, it demonstrates inhibitory activity on Aβ42 secretion, with an EC50 value of 226 nM. Amyloid-β-IN-2 holds potential for research in Alzheimer's disease (AD) and diseases associated with Aβ deposition.

<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>

LRRK2-IN-16 (compound 25) is an inhibitor of the LRRK2 kinase with an IC50 value of less than 5 μM. It is applicable for research in neurodegenerative and autoimmune diseases.

<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>

LP 12 hydrochloride hydrate: potent, selective 5-HT7 agonist (Ki: 0.13 nM); less affinity for D2, 5-HT1A/2A receptors.

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.

Aβ-IN-2 is a peptide inhibitor of Aβ1-42.

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

FCOB02 is a monoamine oxidase B (MAO-B) ligand. It can be labeled as [18F]FCOB02, serving as a 4-methylcoumarin-like targeting probe. [18F]FCOB02 demonstrates high affinity for MAO-B, with an IC50 of 10.68 nM. It is utilized for specific imaging and quantitative analysis of MAO-B in vivo.

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

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.

MAO-B-IN-40 (3a) is an inhibitor of MAOB, exhibiting an IC50 value of 0.493 μM against hMAOB, and demonstrates significant neuroprotective and antioxidant effects. MAO-B-IN-40 (3a) is applicable in Parkinson's disease research.

AChE-IN-83 (compound f1) is an AChE inhibitor that suppresses nematode growth and acetylcholinesterase activity in rice seeds while being safe for the seeds. It specifically targets Aphelenchoides besseyi, with an LC50 of 19.0 μg/mL over 48 hours. AChE-IN-83 impedes nematode populations and behaviors in rice seeds, damages the nematode cuticle, and induces reactive oxygen species, lipofuscin, and lipid generation within the nematodes.

Revexepride, a 5-HT4 agonist, may boost CYP3A4, used for treating GERD.

HW161023 (compound) is an orally active inhibitor of AP2 associated protein kinase 1 (AAK1), exhibiting IC50 values of 5.4 nM for AAK1 and 11.9 μM for hERG. HW161023 can suppress pain response in a rat model of chronic sciatic nerve compression injury.

LK-732 is a thrombin inhibitor with antithrombotic activity. It exhibits dose-dependent inhibition in models of hypercoagulability, with an IC50 value of 1.3 mg/kg. LK-732 is used in cardiovascular and cerebrovascular research.

Compound 6f is a potent, selective 5-HT1A receptor blocker (Ki: 35 nM), useful in CNS disorder research.

SGE516: neuroactive steroid, enhances GABAA, lowers neuronal activity, protects from seizures.

Dual AChE-MAO B-IN-1: orally active CNS-permeable, safe, stable neuroprotective agent; AChE IC50=550 nM, MAO-B IC50=8.2 nM.

(E)-CHBO4 is an MAO-B inhibitor with an IC50 value of 0.023 μM, making it a potential candidate for research into Parkinson's disease treatment.

MAO-B-IN-34 (compound 3d) is an inhibitor of monoamine oxidase B.

8 Hydroxy PIPAT oxalate is a selective 5-HT1A receptor agonist that enhances the spontaneous release of histamine by promoting the degranulation of mast cells in guinea pig and human intestinal preparations. By activating the serotonin signaling pathway, this compound demonstrates potential in regulating gastrointestinal functions and offers insight into the management and suppression of functional gastrointestinal disorders such as irritable bowel syndrome. Its effects in increasing histamine release could play a crucial role in gastrointestinal regulation.

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

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

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

MADAM demonstrates high affinity and selectivity for 5-HTT, with a Ki value of 1.6 nM. It is utilized as a PET radiotracer for visualizing serotonin transporters.

AAZ-A 154 hydrobromide is a selective, competitive, non-hallucinogenic 5-HT2AR antagonist. It promotes neuronal growth in rodents and yields enduring beneficial behavioral effects.

<p>AAZ-A 154 benzoate is a selective, competitive, and non-hallucinogenic 5-HT2AR antagonist. This compound facilitates neuronal growth in rodents and produces lasting beneficial behavioral effects.</p>

AAZ-A 154 hydrochloride is a selective, competitive, non-hallucinogenic antagonist of 5-HT2AR. It promotes neuronal growth in rodents and results in enduring beneficial behavioral effects.

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.

AAZ-A 154 is a selective, competitive, and non-hallucinogenic antagonist of the 5-HT2AR. It promotes neuronal growth in rodents and results in lasting beneficial behavioral effects.

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

EF1502 is a potent and selective GABA transporter inhibitor.

LRRK2-IN-12 (compound 1) is a potent inhibitor of LRRK2 (G20195) with an IC 50 of 0.45 nM, LRRK2 WT with an IC 50 of 1.1 nM, and LRRK2 WT ADP-Glo with an IC 50 of 0.46 nM. This compound is utilized in research related to Alzheimer's Disease [1].

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

eeAChE-IN-1 is a strong inhibitor of eeAChE (IC50: 23 nM).

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

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

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

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

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

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

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

mGlu1 receptor antagonist

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.

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

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

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.

neuronal α7 nAChR antagonist

group II metabotropic glutamate 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).

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

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

<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>

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.

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%.

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.

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).

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.

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.

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

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].

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.

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

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].

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

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

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.

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-6. 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-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 Mouse 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 Mouse IL-6. You can calculate the concentration of Mouse 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 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.