Neurociência

ChEs/MAOs-IN-2 (compound a11) serves as an inhibitor for both cholinesterases and monoamine oxidases, exhibiting IC 50 values of 0.10 µM for MAO-A, 0.20 µM for MAO-B, 0.30 µM for AChE, and 0.40 µM for BChE. This compound shows promise for Alzheimer's disease research [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].

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

THRX-194556 is an agonist of the 5-HT4 receptor. It is applicable in the study of gastrointestinal functional disorders and Alzheimer's disease.

<p>AChE/BChE-IN-1: dual AChE/BChE inhibitor, IC50 of 1.06 nM/7.3 nM, crosses blood-brain barrier, with antioxidant properties for Alzheimer's research.</p>

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.

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

(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.

BChE-IN-3: Selective, pseudo-irreversible BChE inhibitor (IC50: 56.9 nM); borderline reversible AChE inhibitor.

SB 224289: selective 5-HT1B antagonist, pKi 8.2, 60x selectivity, effective orally.

Aβ42 agonist-1 is a small molecule compound with anti-cancer activity and NF-κB inhibitory properties, inducing Aβ42 aggregation.

LRRK2-IN-4: Potent, selective LRRK2 inhibitor, oral, BBB-penetrating, IC50=2.6 nM, potential for Parkinson's.

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

PF-06751979 is an inhibitor of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) (IC50 of 7.3 nM in BACE1 binding assay).

Gabaculine, an irreversible GABA-T inhibitor (Ki: 2.9 μM), impacts plastid development and affects DPOR/GluTR levels.

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.

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

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

ASP-2205, a 5-HT2C receptor agonist (human 5-HT2C receptor, EC50=0.85 nM; rat 5-HT2C receptor, EC50=2.5 nM), enhances the urethral closure reflex mediated by the genital nerve, thereby preventing urinary incontinence.

<p>Befiradol HCl (NLX-112) is a selective 5-HT1A receptor agonist with anxiolytic effects and prevents ATXN3 aggregation.</p>

QP5020 is a QPCTL inhibitor with an IC50 value of 15 nM, demonstrating antitumor efficacy.

EF1502 is a potent and selective GABA transporter inhibitor.

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.

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.

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

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.

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.

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

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.

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

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

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.

FP0429 is an agonist of mGlu4.

Rodatristat ethyl is an oral TPH1 inhibitor reducing 5-HT levels & lowering PAH at low doses.

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

Etoperidone is an antidepressant that acts as an orally active reuptake inhibitor for serotonin (serotonin) and noradrenaline (nor-adrenaline). It demonstrates specific binding affinities (Kd) for several receptors: 36 nM at the 5-HT2 receptor, 38 nM at the α1-adrenergic receptor (α1-adrenergic receptor), 85 nM at the 5-HT1A receptor, and 570 nM at the α2-adrenergic receptor (α2-adrenergic receptor).

AChE-IN-8 (Compound 19), potent acetylcholinesterase blocker; IC50 = 1.95 μM; potential Alzheimer's treatment.

<p>AChE/BuChE-IN-3 inhibits AChE (IC50: 0.65 μM), BuChE (IC50: 5.77 μM), crosses BBB, and hinders Aβ1-42 aggregation for Alzheimer's research.</p>

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).

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-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).

5-HT2A and 2C receptor antagonist

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

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

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.

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

YNT-3708 is an orexin receptor (OXR) agonist, exhibiting EC50 values of 14.6 nM for OX1R and 277 nM for OX2R.

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.

Refisolone is an antagonist of the GABAA receptor.

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

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

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

<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>

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>

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

neuronal α7 nAChR antagonist

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

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

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

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.

mGlu1 receptor 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).

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

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

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>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>

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

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.

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.

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

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.

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).

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.

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].

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].

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%.

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).

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

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 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 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 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.