Neurociência

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

Potent 5-HT6/5-HT2A receptors dual antagonist with K i of 11 nM & 39 nM.

U92016A hydrochloride: potent, orally active 5-HT1A agonist, metabolically stable, high intrinsic activity, Ki=0.2 nM.

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

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].

AAK1-IN-2 TFA (compound (S)-31) is a selective and potent AAK1 inhibitor (IC50: 5.8 nM) that can cross the blood-brain barrier.

(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.

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

NY0116 is an agonist of the neuromedin U receptor 2 (NMUR2), exhibiting EC50 values of 27.76 μM for hNMUR1 and 13.61 μM for hNMUR2. In NMUR2 stably expressing HEK293 cells, NY0116 reduces cAMP levels while enhancing calcium signaling [1].

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

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

5-HT2/5-HT7 receptor antagonist

Terguride: treats hyperprolactinemia, blocks 5-HT2A/B, activates dopamine receptors, studied for PAH.

CGS-9895 is a GABA antagonist that operates by interacting with the benzodiazepine binding site on GABA receptors containing the γ subunit (ag).

Dihydro-β-erythroidine, a competitive nicotinic receptor antagonist, effectively blocks the discriminative stimulus properties and inhibits the anxiolytic

5-HT2A/5-HT2C inverse agonist 1 serves as a dual and potent inverse agonist for the 5-HT2A and 5-HT2C receptors, with hERG inhibition properties that mitigate cardiovascular risks. Demonstrating significant antipsychotic efficacy in the MK-801-induced mouse model, this compound holds potential for psychosis research.

<p>(S)-YNT-3708 is the S-isomer of YNT-3708, demonstrating relatively low activity against OX1R and OX2R receptors, with EC50 values of 3595 nM and 1661 nM, respectively.</p>

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.

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

5-HT2 receptor antagonist

COX-2-IN-47 (compound 6c) is a selective inhibitor of COX-2, exhibiting an IC50 of 0.03 μM. This compound also displays antiedema activity.

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

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

Thiomuscimol hydrobromide is an agonist of GABAA receptor.

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

VA012 (compound 11) acts as a positive allosteric modulator (PAM) of the serotonin 5-HT2C receptor. It has been shown to reduce food intake and prevent weight gain during subchronic administration without causing central nervous system-related discomfort. VA012 is applicable in obesity research.

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

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

AAK1-IN-3 TFA, an AAK1 inhibitor with IC50 of 11 nM, crosses the blood-brain barrier, is a quinoline analogue, and may aid neuropathic pain research.

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

PF470 (PF-06297470) is a negative allosteric modulator of the metabotropic glutamate receptor 5 (mGluR5), which demonstrated significant therapeutic effects in Parkinson's disease models. However, its clinical development was halted due to potential issues identified in toxicological studies.

LRRK2-IN-3: potent, selective oral LRRK2 blocker, BBB-penetrant, IC50 of 0.6 nM in hPBMCs, for Parkinson's research.

5-HT1A modulator 4 (Compound 1) is a ligand for the 5-HT receptor, with Ki values of 2.18 μM for 5-HT1A and 19.7 μM for 5-HT2A.

(+)-sparteine (sulfate pentahydrate) is a ganglion blocker that competitively blocks nicotinic acetylcholine receptors in neurons.

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

<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>

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

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.

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

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

AChE-IN-25: selective, potent AChE inhibitor, non-competitive, IC50 = 2.95 μM, for Alzheimer's research.

β-Secretase Inhibitor III is a highly selective inhibitor of BACE1 with a Ki value of 0.13 nM.

2002-G12 (compound 5a) is an Aβ42 inhibitor that can reduce Aβ42 toxicity by 76%. It is applicable in Alzheimer's research.

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

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.

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.

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

Refisolone is an antagonist of the GABAA receptor.

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>

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

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>

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

<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.

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

mGlu1 receptor antagonist

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.

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

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).

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.

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

group II metabotropic glutamate receptor antagonist

neuronal α7 nAChR 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.

(-)-Bicuculline methobromide is a potent antagonist of GABAA 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>

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].

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.

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

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).

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.

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].

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.

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.

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

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%.

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).

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 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.