Catalog No.
Product Name
Application
Product Information
Citations
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ChA Inhibitor
α-NETA is a potent noncompetitive inhibitor of choline acetyltransferase (ChA), exhibiting an IC50 value of 9 μM. Additionally, it displays strong antagonistic activity against aldehyde dehydrogenase 1A1 (ALDH1A1) with an IC50 of 0.04 µM and also targets chemokine-like receptor-1 (CMKLR1). While it shows some inhibitory effects on cholinesterase (ChE) and acetylcholinesterase (AChE) with higher IC50 values, α-NETA is notable for its anti-cancer properties, making it a valuable tool for research in cancer biology and neuropharmacology. -
COX-1 Inhibitor
Ibuprofen sodium is a selective inhibitor of cyclooxygenase-1 (COX-1), exhibiting an IC50 value of 13 μM. This compound demonstrates significant biological activities, including inhibition of cell proliferation, angiogenesis, and induction of apoptosis. As a nonsteroidal anti-inflammatory agent and nitric oxide (NO) donor, ibuprofen sodium is valuable in research areas such as pain, inflammation, infection, immunology, and oncology. -
γ-secretase Inhibitor
Nirogacestat dihydrobromide is a selective, noncompetitive inhibitor of γ-secretase, with a reported IC50 of 6.2 nM. This compound effectively inhibits Notch signaling, making it a valuable tool for studying Notch receptor-dependent cancers while minimizing gastrointestinal toxicity. It is particularly useful in research focused on the role of γ-secretase in cancer biology and therapeutic development. -
GABAA Receptor Agonist
Cipepofol is a positive allosteric modulator and direct agonist of the GABAA receptor. This compound demonstrates significant central nervous system inhibition and promotes sleep, offering potential applications in anesthesia and sleep research. Additionally, Cipepofol activates the Sirtuin1 (Sirt1)/Nrf2 pathway, providing cardioprotective effects against isoproterenol-induced myocardial infarction by reducing oxidative stress, inflammatory responses, and cardiomyocyte apoptosis. -
GCS Inhibitor
PDMP hydrochloride is a potent inhibitor of glucosylceramide synthase (GCS). This compound has been shown to induce apoptosis in K562/A02 cells, making it a valuable tool for studying cancer biology, particularly in leukemia research. PDMP hydrochloride's ability to disrupt glycosphingolipid metabolism provides insights into therapeutic strategies targeting GCS in cancer treatment. -
COX-2 Specific Inhibitor
SC-236 is a selective inhibitor of cyclooxygenase-2 (COX-2) with an IC50 of 10 nM and also acts as a PPARγ agonist. It effectively suppresses activator protein-1 (AP-1) through the inhibition of c-Jun NH2-terminal kinase, demonstrating significant anti-inflammatory effects. SC-236 has been shown to reduce ERK phosphorylation in murine models, highlighting its potential for investigating inflammatory pathways and therapeutic interventions. -
COX-2 Inhibitor
Humulone, a prenylated phloroglucinol derivative, is a selective inhibitor of cyclooxygenase-2 (COX-2). It demonstrates significant anti-inflammatory properties and serves as a positive modulator of GABAA receptors at low micromolar concentrations. Additionally, Humulone is known to inhibit bone resorption and exhibits antioxidant, anti-angiogenic, and pro-apoptotic activities, making it valuable for various research applications in inflammation and cancer studies. -
COX-2 Inhibitor
DuP-697 is a potent, irreversible, and selective inhibitor of cyclooxygenase-2 (COX-2), exhibiting an IC50 of 10 nM for human COX-2 and 800 nM for COX-1. This compound demonstrates significant antiproliferative effects on HT29 colorectal cancer cells with an IC50 of 42.8 nM, as well as antiangiogenic and pro-apoptotic activities. By inhibiting prostaglandin synthesis, DuP-697 offers potential applications in studies related to inflammation, cancer, and fever reduction. -
Insecticide
Dimethoate is an organophosphate insecticide and acaricide that functions primarily as an acetylcholinesterase inhibitor. It exhibits significant biological activity by inducing reactive oxygen species (ROS) production, leading to DNA damage and apoptosis in vivo. Additionally, Dimethoate impacts the immune system in murine models, highlighting its relevance in toxicological and environmental research applications. -
GABA Receptor Modulator
α-Thujone is a monoterpene that acts as a reversible modulator of the GABA type A receptor, with an IC50 of 21 μM for inhibiting GABA-induced currents. This compound demonstrates significant anti-tumor activity by inducing reactive oxygen species (ROS) accumulation, as well as promoting cell apoptosis and autophagy. Additionally, α-Thujone exhibits antinociceptive, insecticidal, and anthelmintic properties, while being capable of crossing the blood-brain barrier, making it valuable for various biological research applications. -
COX Inhibitor
Metamizole sodium is a potent cyclooxygenase (COX) inhibitor that exhibits significant anti-inflammatory, analgesic, and antipyretic properties. This compound not only inhibits cell proliferation but also promotes apoptosis in various cell types. Additionally, Metamizole sodium serves as a spasmolytic agent, making it a valuable tool for research applications aimed at pain relief and the study of inflammatory processes. Its multifunctional activities contribute to its utility in diverse areas of biomedical research. -
Cholinesterase (ChE) Inhibitor
β-NETA is a potent noncompetitive inhibitor of cholinesterase (ChE) and choline acetyltransferase (ChA), with IC50 values of 40 μM and 76 μM, respectively. Additionally, it exhibits weak inhibitory effects on acetylcholinesterase (AChE), with an IC50 value of 1 mM. This compound is relevant for research in neurobiology and studies focused on cholinergic signaling pathways and associated disorders. -
BChE Inhibitor
Gypsogenin is a selective mixed-type inhibitor of butyrylcholinesterase (BChE) with a Ki of 19.99 μM. It demonstrates significant cytotoxicity against multiple human cancer cell lines by inducing cell cycle arrest and initiating apoptosis. Additionally, Gypsogenin exhibits antibacterial properties against species such as Bacillus subtilis and Bacillus thuringiensis, positioning it as a crucial scaffold for developing novel anticancer agents. This compound is extensively utilized in research focusing on Alzheimer's disease and various cancers, including colon cancer, melanoma, and leukemia. -
α7 nAchR/JAK2/STAT3 Agonist
α7 nAchR-JAK2-STAT3 agonist 1 is a selective agonist targeting the α7 nicotinic acetylcholine receptor, modulating the JAK2-STAT3 signaling pathway. It demonstrates significant anti-inflammatory activity by inhibiting the expression of inducible nitric oxide synthase (iNOS), interleukin-1 beta (IL-1β), and interleukin-6 (IL-6) in murine RAW264.7 macrophages, with an IC50 of 0.32 μM for nitric oxide production. Additionally, it effectively suppresses lipopolysaccharide (LPS)-induced nitric oxide release, NF-κB activation, and related cytokine production. This compound is valuable for studying sepsis and inflammatory responses. -
Multitargeted Depressant
FMF-06-098-1 is a multitargeted kinase PROTAC degrader designed to promote the degradation of various kinases, including AAK1, ABL2, AURKA, and WEE1, among others. This compound exhibits broad biological activity by modulating kinase levels, which can influence cellular signaling pathways and impact cancer progression. FMF-06-098-1 is valuable in research applications focused on understanding kinase function and developing therapeutic strategies targeting multiple kinases in various diseases. -
COX-2 Inhibitor
COX-2-IN-43 is a selective COX-2 inhibitor with an IC50 of 0.247 μM for COX-2 and 0.983 μM for COX-1. This compound demonstrates significant biological activity by inhibiting cancer cell proliferation and colonization while inducing apoptosis. It is valuable for research applications targeting inflammatory diseases and cancer therapeutics. -
Stable Isotope
Galanthamine-O-methyl-d3 is a deuterium-labeled derivative of Galanthamine, a potent inhibitor of acetylcholinesterase (AChE) with an IC50 value of 500 nM. This stable isotope-labeled compound is primarily utilized in pharmacokinetic and metabolic studies. It serves as a valuable tool for investigating the pharmacological dynamics and biochemical pathways associated with cholinergic activity. -
Drug Metabolite
3-O-Methyltolcapone-d4 is a deuterium-labeled metabolite of Tolcapone, which serves as a selective and potent inhibitor of catechol-O-methyltransferase (COMT) with an IC50 of 773 nM. This compound is utilized in research focused on cancer and neurological disorders, including Parkinson's disease and neuroblastoma, due to its ability to inhibit α-synuclein and Aβ42 oligomerization, promote oxidative stress, and induce apoptosis in cancer cells. 3-O-Methyltolcapone-d4 provides a valuable tool for studying the metabolic pathways of Tolcapone and its therapeutic implications. -
Stable Isotope
Carbaryl-d7 is a deuterium-labeled derivative of Carbaryl, which functions as an acetylcholinesterase inhibitor. By suppressing the breakdown of acetylcholine in the synaptic cleft, Carbaryl-d7 leads to an accumulation of acetylcholine, potentially resulting in neurotoxic effects. This stable isotope is primarily utilized in chemical research to study the enzymatic action and biological effects of Carbaryl and its derivatives. -
COX Inhibitor
Metamizole hemimagnesium is a cyclooxygenase (COX) inhibitor with anti-inflammatory and antioxidant properties. This compound effectively reduces body temperature and has been shown to decrease levels of C-reactive protein (CRP) and interleukin 6 (IL-6). Metamizole hemimagnesium also inhibits cell proliferation and promotes apoptosis. It is utilized in research applications focused on inflammation and fever modulation. -
Drug Metabolite
Tolcapone 3-β-D-glucuronide is a drug metabolite derived from Tolcapone, which serves as a selective and potent inhibitor of catechol-O-methyltransferase (COMT). While Tolcapone exhibits notable pharmacological activity, Tolcapone 3-β-D-glucuronide itself is pharmacologically inactive. Research indicates that Tolcapone plays a role in inhibiting α-synuclein and Aβ42 oligomerization, contributing to oxidative stress, cancer cell apoptosis, and reactive oxygen species (ROS) production. This metabolite is valuable for investigations into cancer mechanisms and neurological disorders, including Parkinson's disease and neuroblastoma. -
Stable Isotope
Galanthamine-d3 hydrochloride is a deuterium-labeled derivative of Galanthamine, primarily used as a stable isotope. This compound serves as a useful tool in pharmacokinetic studies and metabolic research, enabling the investigation of drug metabolism and distribution. Galanthamine-d3 hydrochloride plays a significant role in understanding the mechanisms of action of acetylcholinesterase inhibitors and their effects on neurological processes. -
COX Inhibitor
Ketorolac hydrochloride is a non-steroidal anti-inflammatory drug (NSAID) that acts as a nonselective inhibitor of cyclooxygenase (COX), with IC50 values of 20 nM for COX-1 and 120 nM for COX-2. It is utilized in the study of various ophthalmic conditions, including allergic conjunctivitis, cystoid macular edema, intraoperative miosis, and postoperative ocular inflammation and pain. Additionally, Ketorolac hydrochloride functions as a DDX3 inhibitor, making it relevant for cancer research applications. -
Anticancer Agent
Lanuginosine is an alkaloid with demonstrated anticancer activity. It induces apoptosis and inhibits acetylcholinesterase (AChE) with an IC50 of 10.9 μM, in addition to preventing amyloid-beta (Aβ) aggregation. This compound exhibits potent anticancer effects against various malignancies, including hepatocellular carcinoma, human promyelocytic leukemia, chronic myeloid leukemia, melanoma, and brain tumors. Lanuginosine is also valuable for research related to Alzheimer's disease and its therapeutic strategies. -
PKC/CaMKII Activator
Junicedric acid is a diterpenoid compound that functions as an activator of Protein Kinase C (PKC) and calcium/calmodulin-dependent protein kinase II (CaMKII). This compound exhibits neuroprotective properties by elevating intracellular calcium levels in hippocampal neurons, thereby mitigating amyloid-β oligomer-induced synaptic protein loss, apoptosis, and inhibition of long-term potentiation (LTP). Junicedric acid serves as a valuable tool for investigating the pathological mechanisms underlying neurodegenerative diseases, including Alzheimer’s disease. -
Stable Isotope
Carbaryl-d3 is a deuterium-labeled variant of Carbaryl, characterized as an acetylcholinesterase inhibitor. This compound prevents the breakdown of acetylcholine in the synaptic cleft, resulting in its accumulation and subsequent neurotoxic effects. Carbaryl-d3 is employed in research related to neurotoxicity mechanisms and may serve as a tool for studying the pharmacokinetics and metabolic pathways of Carbaryl. Its stable isotope labeling enhances analytical precision in experimental applications. -
COX Inhibitor
Meloxicam sodium is a selective cyclooxygenase (COX) inhibitor, primarily targeting COX-2 with an IC50 of 0.49 μM while exhibiting a higher IC50 of 36.6 μM for COX-1. This non-steroidal anti-inflammatory agent is capable of crossing the blood-brain barrier, making it suitable for research applications involving central nervous system inflammation and pain management. Meloxicam sodium is widely utilized in studies assessing the efficacy of anti-inflammatory therapies. -
COX-1/2 Inhibitor
Taraxerol acetate is an inhibitor of COX-1 and COX-2, exhibiting IC50 values of 116.3 μM and 94.7 μM, respectively. This compound demonstrates notable anticancer properties and has been shown to induce apoptosis in cancer cells. Taraxerol acetate is valuable for research applications focusing on inflammation, pain relief, and cancer treatment mechanisms. -
Apoptosi
Pamiparib maleate is a highly potent and selective inhibitor of poly (ADP-ribose) polymerase (PARP), targeting apoptotic pathways. This compound effectively penetrates the blood-brain barrier, inducing neurotoxicity manifesting as cerebral hemorrhage, brain atrophy, and movement disorders in zebrafish embryos. It regulates critical enzymes such as acetylcholinesterase (AChE) and adenosine triphosphatase (ATPase), leading to increased oxidative stress that triggers apoptosis and affects the expression of neurodevelopment-related genes. Additionally, pamiparib maleate downregulates the Notch signaling pathway, providing insights into its potential neurotoxic effects during embryonic development and its relevance in neuropharmacology research. -
γ-secretase Inhibitor
MRK 003 is a selective and orally bioavailable inhibitor of γ-secretase. It demonstrates significant reduction of Aβ peptide production in the brain in vivo, making it a valuable tool for Alzheimer's disease research. Additionally, MRK 003 induces caspase-dependent apoptosis and inhibits tumor cell proliferation both in vitro and in vivo, supporting its potential applications in cancer research. -
MAO-B/Acetylcholinesterase Inhibitor
MAO-B-IN-26 is a selective inhibitor of monoamine oxidase B (MAO-B) and acetylcholinesterase, demonstrating neuroprotective properties against β-amyloid (Aβ) induced cytotoxicity in SH-SY5Y cells. This compound effectively mitigates morphological alterations, reactive oxygen species (ROS) generation, and membrane damage associated with neurodegeneration. Additionally, MAO-B-IN-26 suppresses Aβ-induced autophagy and apoptosis, making it a valuable tool for research focused on therapeutic strategies for Alzheimer's disease. -
P2Y6 Receptor Agonist
PSB 0474 (3-phenacyl-UDP) is a selective and potent agonist of the P2Y6 receptor, exhibiting an EC50 of 70 nM. This compound modulates key biological activities, including the inhibition of cell proliferation and the enhancement of nitric oxide release in astrocytes and microglia. Additionally, PSB 0474 promotes apoptosis in astrocytes, making it a valuable tool for research in neurobiology and cell signaling pathways. -
P2Y6 Agonist
MRS2693 ammonium is a selective agonist targeting the P2Y6 receptor, exhibiting an EC50 of 0.015 μM. This compound demonstrates significant biological activity by protecting C2C12 skeletal muscle cells from TNFα-induced apoptosis and reducing NF-kB activation. Additionally, MRS2693 ammonium activates the ERK1/2 signaling pathway and has shown cytoprotective effects in a mouse model of ischemia-reperfusion injury, making it a valuable tool for research in cellular protection and signaling pathways. -
P2Y2 Agonist
Diquafosol is a potent P2Y2 receptor agonist that plays a significant role in modulating cellular responses associated with inflammation and apoptosis. It exhibits the ability to inhibit apoptotic pathways and reduce reactive oxygen species (ROS) generation, thereby promoting cell survival. Diquafosol is primarily used in research related to dry eye therapies, providing valuable insights into potential treatment strategies for this condition. -
BChE Inhibitor
Pteryxin is a potent butyrylcholinesterase (BChE) inhibitor (IC50 = 12.96 μg/mL) with additional multi-target mechanisms including inhibition of NF-κB, MAPK, NLRP3 inflammasome activation, and modulation of the Nrf2/ARE pathways. This compound demonstrates significant anti-inflammatory, antioxidant, and osteoclastogenesis inhibitory activities. Pteryxin is suitable for research applications related to inflammatory diseases, osteoporosis, diabetes, and neurodegenerative disorders such as Alzheimer's disease. -
P2Y14R Antagonist
P2Y14R Antagonist 1 is a highly selective antagonist of the P2Y14 receptor, exhibiting an IC50 of 0.6 nM. It demonstrates significant antagonistic activity against P2Y14R, with both in vitro and in vivo efficacy, along with favorable pharmacokinetic properties. This compound effectively reduces the release of inflammatory mediators and mitigates cell pyroptosis through the NLRP3/Gasdermin D signaling pathway. P2Y14R Antagonist 1 is a valuable tool for research investigating acute gouty arthritis and related inflammatory conditions. -
COX-2/NLRP3 Inhibitor
COX-2/NLRP3-IN-1 is a selective inhibitor targeting both COX-2 and the NLRP3 inflammasome, with an IC50 of 1.53 μM for COX-2. This compound exhibits notable anti-inflammatory properties by disrupting the NF-κB/NLRP3 signaling pathway, making it a valuable tool for research into inflammatory diseases. It is suitable for studying the roles of COX-2 and NLRP3 in various biological processes and therapeutic interventions. -
P2X7 Modulator
GSK-1482160 is a negative allosteric modulator of the P2X7 receptor (P2X7R), with high oral bioavailability and the ability to penetrate the blood-brain barrier. It has demonstrated a human pIC50 of 8.5 and a rat pIC50 of 6.5, effectively reducing ATP's efficacy at the receptor without altering its affinity, which subsequently inhibits IL-1β release. This compound serves as a valuable radioligand for P2X7R imaging using isotopes such as 11C or 18F and is applicable in research related to chronic joint pain and chronic constriction injury (CCI). -
P2X7R Activitor
HEI3090 is a potent P2X7 receptor (P2X7R) activator. It effectively stimulates dendritic cells that express P2X7R to release IL-18, promoting the activation of Natural Killer cells and CD4 T cells. This cascade results in increased production of IFN-γ, thereby fostering a sustained antitumor immune response. HEI3090 is particularly beneficial in enhancing the efficacy of αPD-1 therapy for non-small cell lung cancer (NSCLC). -
Anti-Inflammatory Compound
Cynandione A is an acetophenone compound with anti-inflammatory properties. It has been shown to protect hepatocytes and cortical neurons from toxicity, as well as improve neurological deficits in a rat model of cerebral ischemia. Additionally, Cynandione A exerts significant anti-inflammatory effects through the activation of macrophage α7 nAChR and the expression of IL-10, making it a valuable tool for research in neuroprotection and inflammation. -
P2X7 Receptor Inhibitor
P2X7-IN-2 is a potent inhibitor of the P2X7 receptor, demonstrating an IC50 value of 0.01 nM for the inhibition of IL-1β release. This compound is valuable in research focusing on the mechanisms of autoimmunity, inflammation, and cardiovascular disease. Its selective action on the P2X7 receptor makes it a critical tool for studying inflammatory pathways and potential therapeutic interventions. -
COX Inhibitor
(±)-Aiphanol is a potent inhibitor of cyclooxygenase (COX) enzymes, specifically targeting COX-1 (IC50 = 1.9 μM) and COX-2 (IC50 = 9.9 μM). This compound displays significant anti-inflammatory properties and further inhibits vascular endothelial growth factor receptor 2 (VEGFR2) with an IC50 of 0.92 μM. By impeding both COX-2 and VEGFR2 pathways, (±)-Aiphanol effectively blocks angiogenesis and induces apoptosis, making it a valuable tool in the study of inflammatory diseases and cancer research. The compound demonstrates oral bioactivity, enhancing its potential for in vivo applications. -
AChE/BChE/BACE-1 Inhibitor
AChE/BChE/BACE-1-IN-1 is a potent inhibitor of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and beta-secretase 1 (BACE-1), exhibiting IC50 values of 0.058 μM, 0.082 μM, and 0.115 μM, respectively. This compound demonstrates significant binding affinity for the peripheral anionic site of AChE, facilitates brain penetration, and shows potential in disrupting amyloid-beta (Aβ) aggregates. Additionally, AChE/BChE/BACE-1-IN-1 exhibits neuroprotective properties against Aβ-induced stress and possesses promising antioxidant activity, making it a valuable tool for Alzheimer's disease research and related neurodegenerative studies. -
AChE/BChE Inhibitor
AChE/BChE-IN-9 is a potent inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), exhibiting IC50 values of 5.74 μM and 14.05 μM, respectively. In addition to its enzymatic inhibition, AChE/BChE-IN-9 demonstrates antioxidant properties with an IC50 of 57.35 μM and has the ability to chelate iron, potentially mitigating oxidative stress. This compound also influences the aggregation of amyloid β1-42, making it relevant for research in neurodegenerative diseases and gerontology. Its capacity to cross the blood-brain barrier further enhances its suitability for studies focused on central nervous system disorders. -
AChE/GSK-3β Inhibitor
AChE/GSK-3β-IN-1 is a dual inhibitor targeting acetylcholinesterase (AChE) and glycogen synthase kinase 3 beta (GSK-3β), demonstrating potent inhibition with IC50 values of 1.2 nM for hAChE, 149.8 nM for hBChE, and 22.4 nM for hGSK-3β. This compound effectively penetrates the blood-brain barrier and displays high selectivity for the CMGC kinase family, particularly binding to the ATP site of DYRK1A. Additionally, AChE/GSK-3β-IN-1 has been shown to inhibit reactive oxygen species (ROS) expression, thereby reducing oxidative stress. It is a valuable tool for research into Alzheimer's disease and related neurodegenerative conditions. -
AChE/BChE/BACE-1 Inhibitor
AChE/BChE/BACE-1-IN-2 is a potent oral inhibitor of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-site amyloid precursor protein cleaving enzyme 1 (BACE-1), exhibiting IC50 values of 0.069 μM, 0.127 μM, and 0.097 μM, respectively. This compound demonstrates significant binding affinity to the peripheral anionic site of AChE, high brain permeability, and the ability to disassemble amyloid-beta (Aβ) aggregates. Additionally, AChE/BChE/BACE-1-IN-2 provides neuroprotective effects against Aβ-induced stress and possesses noteworthy antioxidant properties, making it suitable for research in neurodegenerative disease models. -
nAChR Antagonist
Mecamylamine is a nonselective, noncompetitive antagonist of nicotinic acetylcholine receptors (nAChR). It functions as a ganglionic blocker and is capable of crossing the blood-brain barrier. Mecamylamine is utilized in research focused on neuropsychiatric disorders, hypertension, and the development of antidepressant therapies. -
AChE/BChE Inhibitor
AChE-IN-14 is a potent inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), displaying IC50 values of 0.46 μM for electric eel AChE, 0.48 μM for human recombinant AChE, and 0.44 μM for equine serum BChE. In addition to its cholinesterase inhibition, AChE-IN-14 has a high affinity for the human H3 receptor (H3R) with a Ki value of 159.8 nM. This compound is particularly relevant for research focused on neurodegenerative diseases such as Alzheimer’s disease, where the modulation of cholinergic signaling is critical. -
Antihistamine Agent
Difeterol is an antihistamine agent that functions primarily as a histamine-1 receptor antagonist. It also inhibits butyrylcholinesterase (BChE), making it a valuable tool for studying cholinergic pathways. This compound is particularly relevant for research related to Alzheimer's disease, where modulation of histamine and cholinergic systems may provide insights into therapeutic strategies. -
Antioxidant
Contilisant is a potent antioxidant and neuroprotective agent that targets histamine H3 receptors. It effectively inhibits monoamine oxidases and cholinesterases, contributing to its neuroprotective profile. With a binding affinity of 65.23 nM towards human sigma-1 receptor, Contilisant demonstrates significant therapeutic potential. In preclinical studies, it has been shown to restore cognitive deficits induced by Aβ1-42 in the radial maze assay, making it a valuable tool for Alzheimer's disease research.
