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Catalog No.
Product Name
Application
Product Information
Citations
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AChE/BuChE Inhibitor
Ipidacrine hydrochloride is a potent inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), with IC50 values of 1 μM and 1.9 μM, respectively. This compound also acts as a partial agonist at M2-cholinergic receptors and exhibits reversible cholinesterase inhibition. Ipidacrine hydrochloride facilitates neuromuscular transmission and demonstrates moderate analgesic properties. It shows promise in preclinical models for various conditions, including Alzheimer’s disease, ischemic stroke, facial nerve neuropathy, and diabetes-associated erectile dysfunction, highlighting its potential in investigating cholinergic system-related disorders. -
Sodium Channel Inhibitor
Dibucaine hydrochloride is a sodium channel inhibitor that effectively blocks the influx of sodium ions, thereby preventing the propagation of action potentials in excitable tissues. This compound exhibits potent activity as an anesthetic and is utilized in various research applications, including studies of nerve conduction and muscle excitability. Additionally, it serves as a significant inhibitor of serum cholinesterase, contributing to its utility in pharmacological investigations and the development of anesthetic protocols. -
μ-Opioid Receptor Agoinst/AChE Inhibitor
Eseroline is a potent μ-opioid receptor agonist and a selective, competitive inhibitor of acetylcholinesterase (AChE), with Ki values of 0.1 μM for AChE and 200 μM for butyrylcholinesterase (BuChE). This compound also acts as a nicotinic acetylcholine receptor allosteric enhancing ligand, enhancing acetylcholine signal transduction without directly activating the receptor. Eseroline's neurotoxic effects include cell membrane damage and energy metabolism disruption, making it a valuable tool for investigating Alzheimer's disease pathology and cholinergic signaling. -
P2Y12 Receptor Inhibitor
(±)-Clopidogrel bisulfate is an inhibitor of the platelet P2Y12 receptor and serves as an adenosine diphosphate (ADP) receptor antagonist. By blocking ADP binding to its receptors on platelet membranes, (±)-Clopidogrel bisulfate effectively attenuates ADP-mediated glycoprotein GPIIb/IIIa complex activation. This compound is utilized in research investigating its role in reducing vascular inflammation and mitigating the progression of angiotensin II-induced abdominal aortic aneurysms, as well as exploring its anti-inflammatory properties. -
P2Y Receptor Inhibitor
PSB-16133 sodium is a potent P2Y receptor inhibitor that selectively targets various P2Y receptor subtypes. This compound is valuable for studying purinergic signaling pathways and understanding their roles in physiological and pathological processes. PSB-16133 sodium can be utilized in research applications focusing on inflammation, cardiovascular disorders, and neuronal signaling. -
P2Y₁₂ Receptor Inhibitor
R-138727 is a potent and selective irreversible antagonist of the P2Y12 receptor, functioning as a key inhibitor with an IC50 of 2.5 μM. This compound covalently binds to the P2Y12 receptor present on platelet surfaces, effectively blocking adenosine diphosphate-mediated platelet activation and aggregation. R-138727 is valuable for research applications targeting stroke, cerebral infarction, and associated neurological deficits. -
P2Y11 Receptor Inhibitor
NF340 is a selective inhibitor of the P2Y11 receptor, achieving a pIC50 of 7.3-7.7 in human cells. It effectively blocks nociceptive signaling and alleviates the upregulation of P2Y11 receptors in the spinal dorsal horn following spinal cord injury. NF340 further inhibits the NFκB signaling pathway induced by IL-1β, leading to a reduction in pro-inflammatory cytokine expression and a decrease in intracellular ROS levels. Additionally, it suppresses ATP-induced calcium influx and cell migration in human hepatocellular carcinoma cells. NF340 is relevant for research into neuropathic pain, myocardial ischemia/reperfusion injury, inflammatory pain, rheumatoid arthritis, and hepatocellular carcinoma. -
mAChR Inhibitor
Tematropium is a selective muscarinic acetylcholine receptor (mAChR) inhibitor known for its soft anticholinergic properties. It demonstrates significant biological activity in modulating bronchoconstriction and respiratory secretions. Tematropium is commonly used in research focused on respiratory diseases, exploring its potential in the treatment of asthma and chronic obstructive pulmonary disease (COPD). -
mAChR Inhibitor
Timepidium bromide is a muscarinic acetylcholine receptor (mAChR) inhibitor that exhibits anticholinergic properties. It is primarily utilized in research investigating acetylcholine signaling pathways and the role of mAChR in various physiological and pathological processes. This compound is valuable for studying conditions influenced by cholinergic activity, including respiratory and gastrointestinal disorders. -
PA2/5-LOX/COX Inhibitor
LY256548 is a potent inhibitor of phospholipase A2, 5-lipoxygenase (5-LOX), and cyclooxygenase (COX), demonstrating significant anti-ischemic and anti-inflammatory properties. This compound effectively reduces leukotriene B4 production in response to A23187 stimulation. In preclinical models, LY256548 has shown efficacy in mitigating bone damage and paw swelling in rat models of Freund's complete adjuvant-induced arthritis (FCA), making it a valuable tool for research into inflammatory diseases and analgesic mechanisms. -
Vesicular Acetylcholine Transporter Inhibitor
(-)-Vesamicol is a vesicular acetylcholine transporter inhibitor that exerts its action by reversibly and non-competitively inhibiting the transport of acetylcholine into synaptic vesicles. This compound effectively blocks the activity of vesicular acetylcholine transporters in medial amygdala neurons, making it a valuable tool for studies related to neurotransmission and neurodevelopmental disorders. Its specific application is in research focused on central precocious puberty, providing insights into the role of acetylcholine transport in this condition. -
Aβ Inhibitor
Fustin (3,7,3',4'-Tetrahydroxyflavanone) is a potent inhibitor of amyloid β (Aβ), demonstrating significant effects on neurochemical markers associated with Alzheimer's disease. It enhances acetylcholine (ACh) levels and stimulates choline acetyltransferase (ChAT) activity while decreasing acetylcholinesterase (AChE) activity and expression. Additionally, Fustin promotes the expression of muscarinic M1 receptor genes and enhances receptor binding activity. This compound is valuable for research in Alzheimer's disease and neurodegenerative processes involving Aβ toxicity. -
Diacylglycerol Lipase Inhibitor
RHC 80267 is a potent and selective inhibitor of diacylglycerol lipase (DAGL), exhibiting an IC50 of 4 μM in canine platelets. This compound is valuable for research applications focusing on the modulation of lipid signaling pathways, particularly in the context of acetylcholine-induced relaxation. Additionally, RHC 80267 demonstrates inhibitory effects on cholinesterase with an IC50 of 4 μM and also inhibits cyclooxygenase (COX) and the hydrolysis of phosphatidylcholine (PC), making it a versatile tool for exploring lipid metabolism and neuronal signaling. -
mAChR Inhibitor
Arborine is a potent mAChR inhibitor that modulates the peripheral actions of acetylcholine, leading to a significant reduction in blood pressure. This compound is particularly valuable in research applications focused on cardiovascular physiology and the mechanistic study of cholinergic signaling pathways. Its ability to influence blood pressure dynamics makes it an important tool for investigating therapeutic interventions in hypertension and related disorders. -
M4 Inhibitor
VU6008055 is a potent, selective allosteric modulator targeting the M4 muscarinic acetylcholine receptor, with EC50 values of 73.4 nM for human M4 and 19.5 nM for rat M4. This compound is capable of crossing the blood-brain barrier and exhibits oral bioactivity, making it a valuable tool for neuropharmacological research. VU6008055 demonstrates antipsychotic-like effects, contributing to its potential applications in studying psychiatric disorders and related therapeutic approaches. -
mAChR Inhibitor
(Rac)-Sabcomeline hydrochloride is a selective agonist of the M1 muscarinic acetylcholine receptor (mAChR). It exhibits potential neuroprotective effects and is of significant interest in research related to Alzheimer's disease and cognitive disorders. This compound is utilized in studies aimed at understanding the role of muscarinic receptors in synaptic plasticity and memory function. -
mAChR Inhibitor
BTM-1042 is a selective muscarinic acetylcholine receptor (mAChR) inhibitor with notable antispasmodic properties. It effectively inhibits electrical stimulation-induced contraction in the guinea pig ileum and demonstrates a dose-dependent reduction in spontaneous movement of the rabbit stomach. BTM-1042 displays similar activity to atropine in blocking muscarinic receptors while having a minimal impact on other receptor types. Additionally, it suppresses ileal responses triggered by nicotine and 5-hydroxytryptamine, highlighting its potential utility in gastrointestinal research applications and studies related to smooth muscle contraction modulation. -
Detrusor Muscle Contraction Inhibitor
FK 584 is a potent detrusor muscle contraction inhibitor that primarily exhibits antimuscarinic activity alongside weak calcium channel blocking properties. This compound has shown significant efficacy in inhibiting detrusor muscle contractions across various experimental models, making it a valuable tool for research on overactive bladder (OAB). FK 584 presents a manageable risk of mydriasis, enabling detailed exploration of its therapeutic potential in bladder function studies. -
mAChR Inhibitor
(S)-Tolterodine is a selective muscarinic acetylcholine receptor (mAChR) inhibitor, exhibiting an IC50 value of 588 nM. This compound is primarily used in studies related to bladder overactivity and other cholinergic signaling pathways. Its pharmacological properties make it a valuable tool for investigating the mechanisms of mAChR modulation in both clinical and preclinical research. -
mAChR Inhibitor
Phenglutarimid hydrochloride is identified as a muscarinic acetylcholine receptor (mAChR) inhibitor. This compound exhibits anticholinergic properties and is primarily utilized in research related to Parkinson's disease and other neurological disorders. Its ability to modulate cholinergic signaling makes it a valuable tool for investigating therapeutic approaches for movement disorders and cognitive function. -
mAChR inhibitor
Heliosupine N-oxide is a potent inhibitor of muscarinic acetylcholine receptors (mAChR), exhibiting an IC50 value of 350 μM. As a metabolite of Heliosupine and classified as a pyrrolizidine alkaloid, Heliosupine N-oxide serves as a valuable tool for research into cholinergic signaling pathways and related neurological studies. Its inhibitory properties can aid in elucidating the role of mAChR in various physiological and pathological processes. -
mAChR Inhibitor
Phenglutarimid is a muscarinic acetylcholine receptor (mAChR) inhibitor that exhibits anticholinergic properties. It is primarily utilized in research related to Parkinson's disease and other cholinergic dysfunctions. Its ability to modulate neurotransmitter activity makes it a valuable tool for investigating the therapeutic mechanisms underlying movement disorders. -
M1/M3 Receptor Inhibitor
Imidafenacin hydrochloride is an orally active inhibitor of muscarinic M1 and M3 receptors. It effectively inhibits bladder contraction in vivo, demonstrating significant antidiuretic effects through the enhancement of vasopressin signaling. This compound is particularly relevant for research focused on overactive bladder and related conditions, making it a valuable tool in the study of urinary disorders. -
mAChR Inhibitor
Cyclobuxine D is a steroidal alkaloid that functions as a muscarinic acetylcholine receptor (mAChR) inhibitor. It exhibits a notable bradycardic effect in rat models and effectively inhibits contractions induced by acetylcholine and Ba++ in isolated rabbit jejunum muscle. Due to its biological activities, Cyclobuxine D is valuable for research in pharmacology and cardiovascular studies. -
Acetylcholinesterase Inhibitor
Trimethylammonium chloride is a non-competitive inhibitor of acetylcholinesterase, targeting the enzymatic activity responsible for the hydrolysis of the neurotransmitter acetylcholine. By reversibly blocking the deacetylation process of acetylcholinesterase, this reagent plays a critical role in studies related to neurobiology and the modulation of synaptic transmission. Its application extends to research investigating cholinergic signaling pathways and potential therapeutic strategies for neurological disorders. -
Cholinesterase (ChE) Inhibitor
Vomifoliol is a cholinesterase (ChE) inhibitor that exhibits significant antiacetylcholinesterase activity, comparable to that of abscisic acid (ABA). Additionally, this compound shows moderate antileishmanial activity, making it a valuable tool for research into neurodegenerative disorders and parasitic infections. Its unique structure, featuring a modified 2,4-pentadiene side chain, further contributes to its biological activity, offering potential applications in pharmacological studies. -
Prolyl Endopeptidase (PREP) Inhibitor
ONO 1603 is a selective inhibitor of prolyl endopeptidase (PREP), investigated for its potential in antidementia therapy. This compound has demonstrated neuroprotective properties and neurotrophic effects in cerebellar granule cells, enhancing neuronal survival and promoting neurite outgrowth at a concentration of 0.03 µM. Additionally, ONO 1603 increases m3-muscarinic acetylcholine receptor (mAChR) mRNA levels and stimulates mAChR-mediated signaling pathways. These pharmacological properties suggest that ONO 1603 could be a promising therapeutic agent for Alzheimer's disease by enhancing cholinergic neurotransmission and supporting neuronal function. -
AAK1 Inhibitor
BMS-986176 is a potent and selective inhibitor of adaptor associated kinase 1 (AAK1) with an IC50 value of 2 nM. This compound is designed for effective brain penetration, making it a valuable tool in the investigation of neurodegenerative diseases. It is applicable in research focused on the modulation of AAK1 pathways and their implications in various neurological disorders. -
AAK1 Inhibitor
AAK1-IN-12 is a selective inhibitor of the AP2-associated kinase 1 (AAK1) that demonstrates oral bioavailability and the ability to cross the blood-brain barrier. This compound has important implications for research into neurodegenerative disorders, including schizophrenia, Parkinson's disease, neuropathic pain, and Alzheimer's disease. AAK1-IN-12 serves as a valuable tool for investigating the therapeutic potential of AAK1 modulation in various neurological contexts. -
AAK1 Inhibitor
LP-922761 is a selective inhibitor of adapter protein-2 associated kinase 1 (AAK1), demonstrating potent activity with IC50 values of 4.8 nM in enzyme assays and 7.6 nM in cellular assays. Additionally, LP-922761 inhibits BMP-2-inducible protein kinase (BIKE) at an IC50 of 24 nM. Importantly, it shows no significant activity against cyclin G-associated kinase (GAK), opioid receptors, adrenergic α2 receptors, or GABAa receptors, making it a valuable tool for studying AAK1-related signaling pathways and its role in cellular processes. -
AAK1 Inhibitor
BMT-124110 is a highly selective inhibitor of AAK1 (AP2-associated protein kinase 1) with an IC50 value of 0.9 nM. This compound exhibits notable antinociceptive activity, making it relevant in pain management research. Additionally, BMT-124110 inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50 values of 17 nM and 99 nM, respectively, further supporting its utility in kinase-related studies. -
AAK1 Inhibitor
SGC-AAK1-1N is a selective inhibitor of AAK1 (AP2 associated kinase 1) with an IC50 value of 1.8 μM. This compound is utilized in research to elucidate the role of AAK1 in cellular processes, particularly in clathrin-mediated endocytosis and signaling pathways. Its potency makes it a valuable tool in studies focused on understanding the therapeutic potential of AAK1 modulation in various diseases. -
AAK1 Inhibitor
BMS-901715 is a highly selective inhibitor of adaptor protein-2 associated kinase 1 (AAK1) with an IC50 of 3.3 nM. This compound disrupts clathrin-mediated endocytosis, making it valuable for studying cellular processes related to membrane trafficking. BMS-901715 is particularly useful in research applications focused on viral infections and the modulation of synaptic transmission. -
AAK1 Inhibitor
AAK1-IN-2 TFA is a selective and potent inhibitor of Adaptor Protein 2-Associated Kinase 1 (AAK1), demonstrating an IC50 value of 5.8 nM. This compound effectively penetrates the blood-brain barrier, making it a valuable tool for research in neuropathic pain mechanisms. AAK1-IN-2 TFA enables the investigation of AAK1's role in various neurological conditions, providing insights into potential therapeutic targets for pain management. -
AAK1 Inhibitor
AAK1-IN-3 is a potent inhibitor of adaptor protein 2-associated kinase 1 (AAK1), exhibiting an IC50 of 11 nM. This quinoline analogue effectively penetrates the blood-brain barrier, making it suitable for investigating the role of AAK1 in neuropathic pain mechanisms. AAK1-IN-3 is a valuable tool for research focused on neuropharmacology and the modulation of pain pathways. -
AAK1 Inhibitor
AAK1-IN-4 is a selective inhibitor of adaptor protein-2-associated kinase 1 (AAK1), demonstrating an IC50 of 4.6 nM. This orally active compound effectively penetrates the central nervous system, with a filtration Ki of 0.9 nM and a cell IC50 of 8.6 nM. AAK1-IN-4 is primarily utilized in research studies focused on neuropathic pain, offering insights into its underlying mechanisms and potential therapeutic applications. -
AAK1 Inhibitor
AAK1-IN-3 TFA is a quinoline derivative that selectively inhibits adaptor protein 2-associated kinase 1 (AAK1) with an IC50 of 11 nM. This compound demonstrates significant brain penetration and is suitable for investigating neuropathic pain mechanisms. Its ability to modulate AAK1 activity makes it a valuable tool for research applications focused on pain pathways and related neurobiological processes. -
AAK1 Inhibitor
HW161023 is a potent inhibitor of AP2-associated protein kinase 1 (AAK1), demonstrating an IC50 of 5.4 nM against AAK1 and a much higher IC50 of 11.9 μM against hERG. This compound has shown efficacy in alleviating pain in a chronic constriction injury model of the sciatic nerve in rats. HW161023 is valuable for research in pain mechanisms and the modulation of AAK1-related signaling pathways. -
AAK1 Inhibitor
AAK1-IN-10 is a selective inhibitor of adapter-associated kinase 1 (AAK1), exhibiting potent enzyme inhibitory activity with an IC50 of 9.62 nM. This compound primarily functions by impairing the activity of AAK1, a kinase involved in various cellular processes. AAK1-IN-10 demonstrates low cardiotoxicity, with an IC50 of 13.7 μM, making it a suitable candidate for research into conditions such as diabetic neuropathy and postherpetic pain. Its distinct mechanism and safety profile facilitate investigations into therapeutic applications targeting nerve pain and associated disorders. -
AAK1 Inhibitor
AAK1-IN-2 is a selective inhibitor of Adaptor Protein 2-Associated Kinase 1 (AAK1), exhibiting an IC50 of 5.8 nM. This compound demonstrates the ability to penetrate the blood-brain barrier, making it suitable for neurological research. AAK1-IN-2 is particularly relevant for studies investigating the mechanisms underlying neuropathic pain. -
AAK1 Inhibitor
AAK1-IN-5 is a selective inhibitor of adaptor protein-2-associated kinase 1 (AAK1), demonstrating an IC50 of 1.2 nM and a filtrate Ki of 0.05 nM, along with a cell-based IC50 of 0.5 nM. This compound is notable for its ability to penetrate the central nervous system and is orally active, making it suitable for in vivo studies. AAK1-IN-5 is primarily used in research focused on neuropathic pain, providing a valuable tool for understanding AAK1's role in pain pathways. -
AAK1 Inhibitor
BMT-046091 is a selective inhibitor of adaptor-associated kinase 1 (AAK1), targeting its activity to modulate cellular processes. This compound effectively inhibits the phosphorylation of the μ2 peptide by AAK1, demonstrating an IC50 value of 2.8 nM. BMT-046091 is useful in research applications studying AAK1's role in endocytic trafficking and signaling pathways, contributing to a better understanding of its implications in various diseases. -
Aβ Aggregation Inhibitor
TDI-2760 is an Aβ aggregation inhibitor with an IC50 of 1.67 μM, specifically targeting the aggregation of amyloid-beta peptides. This compound effectively inhibits Aβ-fibrinogen interactions and modulates contact system activation induced by Aβ42. TDI-2760 is suitable for research focused on Alzheimer's disease, particularly in the study of vascular abnormalities associated with Aβ aggregation. -
BACE1/BACE2 Inhibitor
NB-360 is a potent dual inhibitor of β-secretase 1 and 2 (BACE1/BACE2) with IC50 values of 5 nM and 6 nM, respectively. This compound is brain-penetrable and orally active, effectively inhibiting the accumulation of amyloid-β proteins. NB-360 is valuable for research in inflammation and neurological diseases, particularly Alzheimer's disease. -
Amyloid Inhibitor
4-Hydroxyindole is an amyloid inhibitor that plays a critical role in the disruption of amyloid fibrillization. This compound has been shown to induce alterations in liver function, thyroid activity, and blood glucose levels in preclinical models. Its unique properties make 4-Hydroxyindole a valuable tool for investigating neurodegenerative diseases and metabolic disorders. Researchers can leverage its potential to explore therapeutic avenues for amyloid-related pathologies. -
TDP-43 Inhibitor
ACI-19626 is a TDP-43 inhibitor that targets TDP-43 aggregation. This compound is valuable for investigating the role of TDP-43 in neurodegenerative diseases, including amyotrophic lateral sclerosis (ALS) and frontotemporal dementia (FTD). Its utility in preclinical studies helps elucidate the molecular mechanisms underlying these conditions and aids in the identification of potential therapeutic strategies. -
Aβ1-42 Aggregation Inhibitor
Aβ1–42 aggregation inhibitor 1 is a potent inhibitor of Aβ1-42 aggregation, targeting its self-mediated aggregation pathway. This compound effectively inhibits acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) with IC50 values of 2.64 μM and 1.29 μM, respectively. At a concentration of 25 μM, it reduces Aβ1-42 aggregation by 51.29%. Aβ1–42 aggregation inhibitor 1 is suitable for research applications focused on the mechanisms of Alzheimer's disease and potential therapeutic interventions. -
AChE Inhibitor
Phenserine is a potent, noncompetitive inhibitor of acetylcholinesterase (AChE), derived from Physostigmine. It selectively targets AChE and has been shown to reduce the formation of β-amyloid precursor protein (APP) and β-amyloid peptide (Aβ). This compound is primarily utilized in research related to cognitive function and the progression of Alzheimer's disease, demonstrating potential therapeutic benefits in enhancing cognitive performance. -
QPCTL Inhibitor
QP5038 is a specific inhibitor of the enzyme QPCTL, exhibiting an IC50 value of 3.8 nM. This compound demonstrates significant antitumor activity, making it a valuable tool for research in cancer biology. QP5038 can be utilized in studies focused on understanding the role of QPCTL in tumor metabolism and potential therapeutic strategies. -
Glutaminyl Cyclase Inhibitor
PBD-150 is a selective inhibitor of human glutaminyl cyclase (hQC), specifically targeting the Y115E-Y117E variant with a Ki value of 490 nM. This compound exhibits significant inhibitory activity, making it a valuable tool for studying the role of glutaminyl cyclase in neurodegenerative diseases. PBD-150 can be applied in research focused on pathologies associated with abnormal protein aggregation and its therapeutic potential.
