Catalog No.
Product Name
Application
Product Information
Citations
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mAChR Antagonist
GS 283 is a muscarinic acetylcholine receptor (mAChR) antagonist that exhibits calcium antagonist properties. This compound effectively modulates smooth muscle contraction by inhibiting contractions induced by carbachol and histamine in guinea pig tracheal smooth muscle, as well as high H+ levels in both guinea pig and rat tracheal smooth muscle. Additionally, GS 283 has been shown to inhibit Ca2+-induced contractions, and at elevated concentrations, it can completely abolish carbachol-induced contractions in a Ca2+-free environment. This makes GS 283 a valuable tool for research related to respiratory physiology and the pharmacological modulation of smooth muscle activity. -
Histamine H3 Receptor Antagonist
AChE/BChE-IN-21 is a histamine H3 receptor antagonist that also functions as a calcium channel blocker and acetylcholinesterase inhibitor. This compound demonstrates neuroprotective properties against oxidative stress induced by H2O2 and amyloid-beta peptide Aβ1-40. Additionally, AChE/BChE-IN-21 has been shown to improve cognitive function in mouse models of Alzheimer's disease, making it a valuable tool for research into neurodegenerative disorders. -
H3R Antagonist
H3R Antagonist 2 is a selective antagonist of the histamine H3 receptor (H3R) with a Ki value of 170 nM for human H3R. This compound demonstrates inhibitory activity against acetylcholinesterase, butyrylcholinesterase, and human monoamine oxidase B (hMAO B), with IC50 values of 180 nM, 880 nM, and 775 nM, respectively. Additionally, H3R Antagonist 2 exhibits promising anti-neuropathic pain and memory-enhancing effects, effectively crossing the blood-brain barrier (BBB). This makes it a valuable tool for research in neuropharmacology and cognitive enhancement studies. -
P2Y Receptor Modulator
Uridine-5'-diphosphate disodium salt functions as an agonist for the P2Y6 receptor, exhibiting high specificity with an EC50 of 300 nM (pEC50=6.52 for the human P2Y6 receptor). This endogenous metabolite plays a crucial role in catalyzing the glucuronidation of various substrates and is also instrumental in RNA biosynthesis. Its modulation of P2Y receptors has significant implications for research in cellular signaling and metabolic processes. -
P2Y Receptor Modulator
Uridine 5'-diphosphate sodium salt is a specific modulator of P2Y receptors, acting as a potent native agonist for the P2Y6 receptor with an EC50 of 300 nM and a pEC50 of 6.52, while also serving as a powerful antagonist at the P2Y14 receptor (pEC50 of 7.28). This endogenous metabolite plays a crucial role in the glucuronidation process of diverse substrates and is integral to nucleic acid biosynthesis, making it a valuable reagent in biochemical and pharmacological research focused on nucleotide signaling pathways and metabolic processes. -
GABAB Receptor Negative Allosteric Modulator
(E/Z)-CLH304a is a negative allosteric modulator of the GABAB receptor, consisting of a mixture of (E)-CLH304a and (Z)-CLH304a. This compound selectively inhibits the GABAB receptor and noncompetitively modulates its activity. Research has demonstrated that (E)-CLH304a is effective in blocking Baclofen-induced ERK1/2 phosphorylation in HEK293 cells that overexpress GABAB receptors, making it a valuable tool for studies investigating GABAB receptor signaling pathways and their implications in neurological disorders. -
P2Y14R Inhibitor
HDB-1 is a selective inhibitor of the P2Y14 receptor (P2Y14R) with an IC50 of 26 pM. This compound effectively blocks the activation of hepatic stellate cells by inhibiting the PKA/Raf1/MEK/ERK signaling pathway associated with P2Y14R, thereby mitigating the progression of liver fibrosis. HDB-1 is valuable for research into the mechanisms underlying liver fibrosis and the development of potential therapeutic strategies. -
Stable Isotope
Propoxur-d3 is the deuterated form of Propoxur, a reversible and competitive acetylcholinesterase (AChE) inhibitor. It crosses the blood-brain barrier and exerts neurotoxic effects by inhibiting AChE activity, leading to increased acetylcholine levels and resultant neurological dysfunction. Additionally, Propoxur-d3 promotes the expression of matrix metalloproteinase-2 (MMP-2) and enhances tumor cell migration and invasion through the generation of intracellular reactive oxygen species (ROS) and the activation of the ERK/Nrf2 signaling pathway. This compound has applications in neurotoxicity studies and cancer research, as well as in assessing pesticide effects in ecological studies. -
α7 nAChR Agonist
A-582941 is a selective α7 nicotinic acetylcholine receptor (nAChR) agonist that effectively crosses the blood-brain barrier. With Ki values of 10.8 nM in rat brain and 17 nM in human frontal cortex, it demonstrates significant biological activity by promoting ERK1/2 and CREB phosphorylation, inhibiting GSK-3β through Ser-9 phosphorylation, and enhancing acetylcholine release. Additionally, A-582941 induces the expression of activity-regulated cytoskeleton-associated protein (Arc) and c-Fos while activating brain regions linked to working memory and attention. This compound is valuable for investigating mechanisms involved in Alzheimer's disease and schizophrenia. -
Stable Isotope
Propoxur-d7 is the deuterium-labeled analog of Propoxur, a reversible and competitive inhibitor of acetylcholinesterase (AChE). This compound exhibits significant neurotoxic effects by inhibiting AChE activity, leading to increased levels of acetylcholine and subsequent neurological dysfunction. Propoxur-d7 also enhances tumor cell migration and invasion through the promotion of matrix metalloproteinase-2 (MMP-2) expression, driven by reactive oxygen species (ROS) generation and activation of the ERK/Nrf2 signaling pathway. Additionally, Propoxur serves as a carbamate insecticide effective against a variety of pests in turf, forestry, and household settings. -
P2Y6 Agonist
MRS2693 trisodium is a selective agonist of the P2Y6 receptor, exhibiting an EC50 value of 0.015 μM. It significantly reduces NF-kappaB activation while activating the ERK1/2 signaling pathway. MRS2693 trisodium demonstrates cytoprotective effects in models of ischemia-reperfusion injury in mouse hindlimb skeletal muscle, making it a valuable tool for research in cellular signaling and tissue injury responses. -
Nicotine Metabolite
(±)-Nornicotine is a significant metabolite of nicotine, acting as a partial agonist of nicotinic acetylcholine receptors (nAChRs) that contain α7 and α6 subunits. This compound is known to disrupt β-catenin and ZO-1 interactions while inducing depolymerization of F-actin, contributing to its biological effects. (±)-Nornicotine has been implicated in research on various conditions, including atherosclerosis, Alzheimer's disease, and schizophrenia, making it a valuable tool for studies involving neural and vascular pathophysiology. -
Stable Isotope
(±)-Nornicotine-d4 is a deuterium-labeled analog of (±)-Nornicotine, a significant metabolite of nicotine. It acts as a partial agonist at nicotinic acetylcholine receptors (nAChRs), particularly those containing α7 and α6 subunits, influencing various biological pathways. This compound has been shown to disrupt β-catenin and ZO-1 interactions while inducing F-actin depolymerization. (±)-Nornicotine-d4 is valuable for research focused on atherosclerosis, Alzheimer's disease, and schizophrenia, providing insights into nicotine's metabolic effects and related neurological conditions. -
γ-Secretase Inhibitor
EVP-0015962 is a potent γ-secretase inhibitor that effectively penetrates the blood-brain barrier, exhibiting an IC50 value of 3.9 μM. By modulating the γ-secretase-mediated cleavage of amyloid precursor protein, EVP-0015962 decreases the production of Aβ42 while increasing Aβ38 levels. This compound has demonstrated efficacy in reducing amyloid aggregates, mitigating amyloid plaque formation, and lowering inflammatory markers in mouse models, thereby enhancing cognitive function. EVP-0015962 serves as a valuable tool in Alzheimer's disease research. -
γ-Secretase Modulator
AZ1136 is a selective γ-secretase modulator (GSM) that effectively reduces the levels of amyloid-beta peptides Aβ42 and Aβ40, with IC50 values of 990 nM and 1400 nM, respectively. Furthermore, AZ1136 increases levels of Aβ39 and Aβ37 while showing no effect on Aβ38. This compound is valuable for research applications investigating the pathogenesis of Alzheimer's disease and the modulation of amyloid-beta metabolism. -
γ- Secretase Modulator
BIIB042 is a selective γ-secretase modulator that effectively alters the processing of amyloid precursor protein, resulting in decreased levels of Aβ42 and increased levels of Aβ38. This compound demonstrates significant brain penetration and has shown efficacy in reducing brain Aβ42 levels in CF-1 mice and Fischer rats, while also lowering plasma Aβ42 levels in cynomolgus monkeys. Additionally, BIIB042 decreases Aβ42 levels and ameliorates Aβ plaque burden in Tg2576 mouse models. This reagent is valuable for research into Alzheimer’s disease. -
γ-secretase Modulator
(E/Z)-Sulindac sulfide is a selective γ-secretase modulator that plays a crucial role in the modulation of amyloid-beta (Aβ) peptide production. This compound notably reduces the production of Aβ42, favoring the generation of shorter Aβ species, making it a valuable tool for research into Alzheimer's disease. Its ability to influence Aβ processing makes (E/Z)-Sulindac sulfide significant for studies focusing on Alzheimer's pathogenesis and potential therapeutic strategies. -
γ-secretase Inhibitor
JNJ-40418677 is a potent orally active inhibitor of γ-secretase, capable of crossing the blood-brain barrier. It effectively inhibits the production of Aβ42 and the activity of NS2B-NS3 protease, with IC50 values of 200 nM and 3.9 μM, respectively. This compound exhibits favorable biological tolerance and is suitable for research applications related to Alzheimer's disease. -
γ-Secretase Modulator
PF-06648671 is an orally active γ-secretase modulator that effectively penetrates the blood-brain barrier. This compound demonstrates the ability to reduce levels of amyloid-beta peptides Aβ42 and Aβ40, while concurrently increasing Aβ37 and Aβ38 in vitro. PF-06648671 is valuable for research applications focused on Alzheimer’s disease and the modulation of amyloid processing pathways. -
γ-secretase Inhibitor
Sulindac sulfide is a noncompetitive inhibitor of γ-secretase, exhibiting an IC50 of 20.2 μM for γ42-secretase activity. This compound plays a crucial role in research involving Alzheimer's disease and other neurodegenerative conditions by modulating the processing of amyloid precursor protein. Its ability to inhibit γ-secretase makes it a valuable tool for studies focused on reducing amyloid-beta peptide formation and investigating related signaling pathways. -
γ-secretase Inhibitor
ELND 006 is a selective γ-secretase inhibitor that effectively reduces amyloid beta (Aβ) generation while preserving Notch signaling pathways. Developed with a focus on metabolic stability, this compound has shown significant efficacy in lowering Aβ levels both in vitro and in vivo during preclinical studies. ELND 006, alongside its structural analog ELND 007, has advanced into human clinical trials, indicating its potential therapeutic applications in Alzheimer's disease research and treatment. -
γ-secretase Modulator
RO7185876 is a selective gamma-secretase modulator that plays a crucial role in the regulation of amyloid precursor protein processing. This compound is primarily investigated for its potential in Alzheimer's disease research, where it may help reduce the production of amyloid-beta peptides. Its unique mechanism of action positions RO7185876 as a valuable tool for studying the pathophysiology of Alzheimer's and exploring therapeutic options. -
γ-secretase Modulator
GSM-1 is a potent γ-secretase modulator that directly targets the transmembrane domain (TMD) 1 of presenilin 1 (PS1). By modulating γ-secretase activity, GSM-1 influences the processing of amyloid precursor protein (APP), making it valuable in Alzheimer's disease research. This compound can be utilized to investigate mechanisms of amyloid-beta peptide generation and potential therapeutic strategies for neurodegenerative disorders. -
gamma-Secretase Inhibitor
Gamma-secretase modulator 6 is a gamma-secretase inhibitor that effectively reduces the secretion of Aβ42 in HEK cells stably expressing amyloid precursor protein (APP), with a pIC50 value of 8.1. This compound plays a crucial role in the study of Alzheimer's disease by modulating gamma-secretase activity, thereby influencing amyloid plaque formation. It is a valuable tool for researchers exploring therapeutic strategies targeting amyloid pathology in neurodegenerative disorders. -
γ-secretase Modulator
FRM-024 is a potent γ-secretase modulator designed for central nervous system applications. It selectively alters the activity of γ-secretase, a critical enzyme involved in the pathogenesis of familial Alzheimer’s disease. This compound has demonstrated the ability to influence amyloid precursor protein processing, making it a valuable tool for research focused on Alzheimer’s therapeutics and disease mechanisms. -
γ-secretase/Aβ42 Inhibitor
Amyloid-β-IN-2 is a selective γ-secretase inhibitor that effectively reduces the secretion of Aβ42 in H4 cells, exhibiting an EC50 value of 226 nM. This compound demonstrates potential for research applications in Alzheimer's disease and other conditions associated with Aβ deposition. Its ability to modulate γ-secretase activity makes it a valuable tool for studying the mechanisms underlying amyloid-related pathologies. -
γ-secretase/Aβ42 Inhibitor
Amyloid-β-IN-3 is a selective inhibitor of γ-secretase that effectively reduces the secretion of Aβ42 in H4 cells, exhibiting an EC50 value of 148 nM. By modulating γ-secretase catalytic activity, it decreases Aβ42 production and helps mitigate the neurotoxicity associated with amyloid deposition. This compound shows potential for research applications in Alzheimer's disease (AD) studies. -
γ-secretase Inhibitor
ELN318463 is a selective inhibitor of γ-secretase, targeting the amyloid precursor protein (APP). It demonstrates differential inhibition of presenilin 1 (PS1) and presenilin 2 (PS2) γ-secretase complexes, with EC50 values of 12 nM and 656 nM, respectively, showcasing a 51-fold greater selectivity for PS1. This compound is primarily utilized in research focused on Alzheimer's disease and related neurodegenerative disorders, making it a valuable tool for studies investigating APP processing and amyloid plaque formation. -
γ-secretase Modulator
(-)-FRM-024 is a potent γ-secretase modulator that effectively penetrates the central nervous system. This compound is instrumental in Alzheimer’s disease research, facilitating the study of amyloid precursor protein processing and its implications in neurodegeneration. Its ability to modulate γ-secretase activity makes it a valuable tool for exploring therapeutic interventions in Alzheimer's pathology. -
γ-Secretase Modulator
γ-Secretase modulator 4 is a potent modulator of the γ-secretase enzyme, characterized by its ability to effectively reduce Aβ42 peptide levels with IC50 values of 0.014 μM in human samples and 0.017 μM in mouse samples. This compound has significant implications in Alzheimer's research, particularly in the study of amyloid-beta production and the related pathophysiology. Its mechanism of action makes it a valuable tool for investigations into therapeutic strategies targeting Alzheimer's disease. -
γ-secretase Inhibitor
(9R)-RO7185876 is a selective inhibitor of γ-secretase, targeting the cleavage of amyloid precursor protein. This compound significantly reduces the secretion of Aβ42 peptides, making it a valuable tool for research on Alzheimer's disease and related disorders, such as cerebral amyloid angiopathy and multi-infarct dementia. Additionally, (9R)-RO7185876 may be utilized to investigate conditions associated with amyloid deposition, including dementia pugilistica and Down syndrome. -
Gamma-Secretase Modulator
Gamma-Secretase Modulator 1 Hydrochloride acts as a modulator of gamma-secretase, a crucial enzyme implicated in the pathogenesis of Alzheimer's disease. This compound is designed to influence the processing of amyloid precursor protein (APP), ultimately affecting the production of amyloid-beta peptide. Its potential applications include studying the modulation of amyloid-beta levels and investigating therapeutic strategies for Alzheimer's disease and related neurodegenerative disorders. -
γ-secretase Modulator
Nivegacetor is a potent γ-secretase modulator that plays a critical role in the modulation of amyloid precursor protein processing. By influencing the activity of γ-secretase, Nivegacetor is valuable for research into Alzheimer's disease and other neurodegenerative conditions. Its ability to alter the production of amyloid-beta peptides makes it a useful tool for exploring therapeutic pathways and understanding the molecular mechanisms underlying these diseases. -
γ-Secretase Modulator
Aβ42-IN-1 is a potent γ-secretase modulator (GSM) designed to target the enzymatic cleavage of amyloid precursor protein, effectively lowering amyloid-beta 42 (Aβ42) levels. With an IC50 value of 0.091 μM, Aβ42-IN-1 demonstrates significant inhibition of Aβ42 production while avoiding CYP3A4 inhibition, indicating a favorable safety profile. Its sustained pharmacokinetic properties make it a valuable tool for research into Alzheimer's disease and related neuropathologies. This compound holds promise for exploring therapeutic strategies aimed at modulating γ-secretase activity in neurodegenerative disorders. -
γ-Secretase Modulator
Aβ42-IN-1 free base is a potent γ-secretase modulator that exhibits high oral bioavailability and significant brain penetration. This compound effectively lowers Aβ42 levels with an IC50 of 0.091 μM, demonstrating substantial reduction of brain Aβ42 levels in murine models. Aβ42-IN-1 free base holds considerable potential for therapeutic applications in Alzheimer's disease research. -
γ-secretase Inhibitor
MK-0752 sodium is a potent, orally bioavailable inhibitor of γ-secretase, exhibiting a dose-dependent reduction of Aβ40 with an IC50 of 5 nM in human SH-SY5Y cells. This compound effectively crosses the blood-brain barrier and demonstrates the ability to decrease newly generated central nervous system Aβ levels in vivo. MK-0752 sodium is primarily utilized in research on Alzheimer’s disease and other neurodegenerative disorders linked to amyloid-beta pathology. -
γ-secretase Modulator
γ-Secretase modulator 10 is a selective modulator of the γ-secretase enzyme complex. It influences the cleavage of amyloid precursor protein (APP), thereby altering the production of amyloid β peptides associated with Alzheimer's disease pathogenesis. This compound is valuable for research applications focused on neurodegenerative diseases and therapeutic strategies aimed at modulating γ-secretase activity. -
γ-Secretase Modulator
γ-Secretase modulator 14 is a selective modulator of the γ-secretase complex, influencing the cleavage of amyloid precursor protein (APP). This compound exhibits potential in Alzheimer's disease research by altering the production of amyloid-beta peptides. Its utility extends to investigating the mechanisms underlying neurodegenerative disorders and developing novel therapeutic strategies aimed at modulating γ-secretase activity. -
γ-secretase Inhibitor
γ-Secretase modulator 11 functions as a potent γ-secretase inhibitor, effectively reducing levels of amyloid beta 42 in vitro and demonstrating significant brain penetration. This compound exhibits minimal inhibition of cytochrome P450 enzymes, highlighting its selective profile. Additionally, γ-secretase modulator 11 has shown considerable efficacy in alleviating cognitive deficits in Alzheimer's disease model mice, making it a valuable tool for research in neurodegenerative disorders. -
γ-secretase Modulator
BPN-15606 besylate is a potent orally active γ-secretase modulator (GSM) that effectively reduces the production of Aβ42 and Aβ40 peptides in SHSY5Y neuroblastoma cells, exhibiting IC50 values of 7 nM and 17 nM, respectively. This compound has demonstrated the ability to lower Aβ42 and Aβ40 levels in the central nervous system of rodent models. Additionally, BPN-15606 besylate features favorable pharmacokinetic and pharmacodynamic properties, including good bioavailability, optimal half-life, and manageable clearance rates, making it valuable for Alzheimer's disease research and neurodegenerative studies. -
γ-secretase Modulator
BMS-932481 is a potent γ-secretase modulator that demonstrates selective reduction of β-amyloid peptides Aβ1-42 and Aβ1-40, exhibiting IC50 values of 6.6 nM and 25.3 nM, respectively. This compound is valuable for research into Alzheimer's disease and mechanisms of amyloid plaque formation, offering insights into potential therapeutic strategies targeting γ-secretase activity. -
γ-Secretase Inhibitor
GSI-18 is a potent γ-secretase inhibitor that disrupts Notch signaling, contributing to its anticancer properties. This compound effectively inhibits the attachment-free growth of pancreatic cancer cells, making it valuable for research into cancer biology and therapeutic interventions. Its mechanism of action offers insights into the regulation of cell proliferation and differentiation in oncogenic contexts. -
γ-secretase Inhibitor
ELND 007 is a selective γ-secretase inhibitor that primarily targets the reduction of amyloid beta (Aβ) generation while minimizing inhibition of Notch signaling. It demonstrates significant biological activity in both in vitro and in vivo settings, effectively decreasing Aβ levels. This compound has shown potential therapeutic benefits for Alzheimer’s disease, particularly as evidenced by reductions in Aβ levels observed in cerebrospinal fluid during human clinical trials, following a strategic emphasis on metabolic stability and chirality in its development. -
γ-secretase Inhibitor
γ-Secretase-IN-2 is a potent inhibitor of γ-secretase, demonstrating an IC50 of 0.06 nM. This compound is instrumental in researching Alzheimer's disease, providing insights into the enzymatic processes involved in neurodegeneration. Its high efficacy makes it a valuable tool for studying the pathophysiology of Alzheimer's and exploring potential therapeutic strategies. -
γ-secretase Inhibitor
LY3056480 is a potent γ-secretase inhibitor that targets Notch signaling pathways. This compound has demonstrated efficacy in enhancing recovery from mild to moderate sensorineural hearing loss, while exhibiting a favorable safety profile. Additionally, intratympanic administration of LY3056480 has been shown to promote hair cell regeneration and contribute to partial auditory recovery in mammalian models, making it a valuable tool for research in hearing restoration and neurodegenerative studies. -
Multitarget Inhibitor
SSZ is a multitarget inhibitor that engages multiple pathological mechanisms associated with Alzheimer's disease (AD). It inhibits key enzymes including acetylcholinesterase, butyrylcholinesterase, β-site amyloid precursor protein cleavage enzyme 1 (BACE1), and γ-secretase. Research demonstrates that SSZ enhances cognitive function and provides neuroprotective effects in murine models of Alzheimer's disease, making it a valuable tool for studying therapeutic strategies in neurodegenerative disorders. -
γ-secretase Modulator
γ-Secretase modulator 12 is a selective modulator of γ-secretase, specifically designed to reduce levels of amyloid-β42 (Aβ42) with an IC50 of 0.39 µM. This compound is valuable for investigating Alzheimer's disease mechanisms and potential therapeutic interventions. Additionally, γ-secretase modulator 12 demonstrates favorable pharmacokinetics with a good brain-to-plasma ratio (Kp, brain = 0.72) in murine models, making it suitable for in vivo studies. -
γ-Secretase Modulator
γ-Secretase modulator 11 hydrochloride is a potent modulator of γ-secretase with an IC50 of 0.029 µM, demonstrating oral bioavailability. It effectively reduces brain Aβ42 levels, a critical factor in Alzheimer's disease pathology. Furthermore, this compound has shown the capability to improve cognitive deficits in Alzheimer's disease model mice, making it valuable for research into therapeutic strategies targeting Alzheimer's disease. -
γ-secretase Inhibitor
III-31-C is a hydroxyethyl urea-based inhibitor of γ-secretase. It demonstrates potent inhibition of amyloid-beta (Aβ) production, with an IC50 value of 10 nM in a cell-free γ-secretase assay and 200 nM in APP-transfected cells. This compound is relevant for research focused on Alzheimer's disease and offers valuable insights into the modulation of Aβ metabolism. -
γ-secretase Modulator
BMS-869780 is an orally active γ-secretase modulator that selectively regulates γ-secretase activity to modify the production profile of β-amyloid proteins. It alters the relative levels of specific β-amyloid subtypes while not inhibiting the overall production of β-amyloid proteins. Additionally, BMS-869780 demonstrates a synergistic effect when used in combination with acidic γ-secretase modulators, resulting in a reduction of total β-amyloid production in cell cultures. This compound is valuable for research into Alzheimer’s disease and related neurodegenerative disorders.
