Catalog No.
Product Name
Application
Product Information
Citations
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β2-Adrenergic Receptor Agonist
Protokylol hydrochloride serves as a potent agonist of the β2-adrenergic receptor. This compound demonstrates significant bronchodilator activity, making it valuable in research related to respiratory function and pulmonary pharmacology. Additionally, it interacts with the TRPV1 receptor, further expanding its potential applications in studying pain pathways and sensory responses. -
Stable Isotope
(Rac)-Talinolol-d5 is a stable isotope of Talinolol, a long-acting, cardioselective β1-adrenergic receptor blocker. This compound demonstrates significant cardioprotective and antihypertensive properties. Additionally, Talinolol serves as a valuable probe substrate for investigating P-glycoprotein (P-gp) activity in pharmacokinetic studies. -
Adrenergic Receptor Inhibitor
Besipirdine is an adrenergic receptor inhibitor that exhibits non-receptor-dependent cholinomimetic properties. This compound is known to inhibit voltage-dependent sodium and potassium channels, contributing to its pharmacological profile. Besipirdine's biological activity makes it relevant for research applications focused on neuropharmacology and the modulation of synaptic transmission. -
TRPV1 Agonist
Protokylol is a TRPV1 agonist that exerts its biological activity through the activation of transient receptor potential vanilloid 1 channels. Its primary application includes functioning as a bronchodilator, which supports airway relaxation and dilation. Research utilizing Protokylol can facilitate investigations into pain modulation, sensory signaling, and respiratory physiology. -
FTO Inhibitor
Meclofenamic acid sodium hydrate is a selective inhibitor of fat mass and obesity-associated enzyme (FTO). Its primary action involves competing with FTO for binding to m(6)A-containing nucleic acids, thereby influencing RNA metabolism. Additionally, it exhibits non-selective gap-junction blocking activity and inhibits potassium channels hKv2.1 and hKv1.1, with IC50 values of 56.0 μM and 155.9 μM, respectively. This compound is valuable in research focused on obesity, metabolic regulation, and the role of RNA modifications in cellular processes. -
Myosin ATPase Activator
Chrysosplenol C is a flavonoid compound that functions as a selective activator of cardiac myosin ATPase, with an EC50 value of 45 µM. It enhances intracellular calcium ion release by activating protein kinase C (PKC), resulting in increased contractility of rat ventricular muscle cells. Chrysosplenol C is applicable in research related to heart failure, providing insights into mechanisms that may improve cardiac function. -
Aliostericeffect for Myosin ATPase 13 Inhibitor
Diazobenzenesulfonic acid, also known as 4-Sulfobenzenediazonium, functions as an allosteric inhibitor of myosin ATPase 13. This compound has significant biological activity by modulating the enzyme's function, thereby influencing muscle contraction mechanisms. It is primarily utilized in research applications aimed at understanding myosin-related pathways and exploring potential therapeutic targets for muscle-related diseases. -
Cardiac Myofibrillar ATPase Inhibitor
DN-F01 is a potent inhibitor of cardiac myofibrillar ATPase, exhibiting a strong calcium-dependent activity with an IC50 value of 11 ± 4 nmol/L. This compound serves as a valuable tool in studying cardiac muscle contractility and ATPase regulation. Its ability to selectively inhibit cardiac myofibrillar ATPase makes it suitable for research in cardiovascular physiology and related pathologies. -
Myosin ATPase Inhibitor
Myosin-IN-2 is a potent Myosin ATPase inhibitor, demonstrating an IC50 of 1.06 μM. This compound plays a critical role in research focused on heart diseases, particularly hypertrophic cardiomyopathy (HCM). By selectively inhibiting Myosin ATPase activity, Myosin-IN-2 provides valuable insights into the mechanisms underlying cardiac function and related pathological conditions. -
AMPA/GluR Antagonist
Tezampanel etibutil is an orally active antagonist of AMPA receptors and glutamate receptor (GluR) subtypes. This compound exhibits significant biological activity in modulating excitatory neurotransmission, making it a valuable tool for research into pain management, migraine mechanisms, and a variety of neurological disorders. Its specific targeting of AMPA receptors facilitates investigations into glutamatergic signaling pathways and their implications in neuropharmacology. -
Proton Pump Inhibitor
Lansoprazole sulfide-d4 is a deuterium-labeled form of Lansoprazole sulfide, a bioactive metabolite of the proton pump inhibitor Lansoprazole. This compound exhibits significant activity against Mycobacterium tuberculosis, demonstrating IC50 values of 0.59 μM intracellularly and 0.46 μM in broth. It is a valuable tool for research into anti-tubercular therapies and the pharmacokinetics of proton pump inhibitors. -
CCR5 Antagonist
AZD-5672 is a potent and selective antagonist of the CCR5 receptor, exhibiting an IC50 of 0.32 nM. This compound demonstrates moderate activity against the hERG ion channel with a binding IC50 of 7.3 μM and acts as a substrate for human P-glycoprotein, inhibiting P-gp-mediated digoxin transport with an IC50 of 32 μM. AZD-5672 is an effective tool for investigating the role of CCR5 in inflammatory diseases, including rheumatoid arthritis. -
CCR8 Antagonist
AZ760 is a potent antagonist of the CCR8 receptor, which plays a significant role in immune response modulation. This compound demonstrates excellent potency and favorable lipophilicity, resulting in a high free fraction in blood. However, it is important to note that AZ760 exhibits unacceptable inhibition of the hERG potassium channel, which may have implications for cardiovascular safety in therapeutic applications. -
CGRP/TRPV1 Inhibitor
Chrysin 6-C-glucoside 8-C-arabinoside is a potent inhibitor of calcitonin gene-related peptide (CGRP) release and the TRPV1 channel activation. This compound exhibits significant biological activity relevant to nociceptive signaling pathways, making it a valuable tool for anti-migraine research. Its mechanism of action offers insights into potential therapeutic strategies for migraine and related pain disorders. -
OCT1 Inhibitor
Hydrastine ((-)-β-Hydrastine; (1R,9S)-β-Hydrastine) selectively inhibits the organic cation transporter OCT1, with an IC50 value of 6.6 μM. This compound also acts as a competitive inhibitor of tyrosine hydroxylase, reducing dopamine biosynthesis with an IC50 of 20.7 μM in PC12 cells. Hydrastine is particularly relevant for research into Parkinson's disease, as it may induce neuronal toxicity through mitochondrial dysfunction and has the potential to exacerbate apoptosis when used in conjunction with L-DOPA. -
Fatty Acid Dopamide
N-Palmitoyl dopamine is a long-chain fatty acid dopamide that interacts with endovaniloids, exhibiting 'entourage' effects on N-arachidonoyl-dopamine (NADA) and anandamide. This compound is not active on the TRPV1 receptor, highlighting its selective profile. N-Palmitoyl dopamine is valuable for research applications focused on cannabinoid and pain signaling pathways, particularly in studies examining the interplay between fatty acid derivatives and endocannabinoid activity. -
Vitamin E
γ-Tocotrienol is an active form of vitamin E that primarily targets the signaling pathway of NF-κB and P-glycoprotein (P-gp). It demonstrates significant biological activity by reversing multidrug resistance (MDR) in breast cancer cells, enhancing the efficacy of chemotherapeutic agents. Additionally, γ-tocotrienol serves as a radioprotective agent, effectively mitigating bone marrow radiation damage associated with targeted radionuclide treatments. Research applications include cancer therapy and protection against radiation-induced injury. -
Active Metabolite
Desacetyl bisacodyl is the active metabolite of the laxative bisacodyl, primarily targeting epithelial chloride channels. This compound is known to stimulate chloride secretion in the colon and rectum of rat models, leading to increased mucus and electrolyte secretion. It is utilized in research applications focused on gastrointestinal physiology and the mechanisms underlying laxative action. -
Tricyclic Antidepressant Trimipramine Active Metabolite
Trimipramine N-oxide is the active metabolite of the tricyclic antidepressant trimipramine, primarily targeting human monoamine transporters. It effectively inhibits noradrenaline (hNAT), serotonin (hSERT), and dopamine (hDAT) transporters, along with human organic cation transporters (hOCT1 and hOCT2), with IC50 values of 11.7, 3.59, 9.4, 9.35, and 27.4 nM, respectively. This compound is valuable for research focused on depression and anxiety, contributing to the understanding of mood disorders and the pharmacological mechanisms of antidepressants. -
Calcium Channel
C18 LPA (PA(18:0e/0:0)) targets calcium channels and serves as a bioactive phospholipid involved in signal transduction via G protein-coupled receptors (GPCRs). This compound promotes smooth muscle contraction, chemotaxis, cytoskeletal rearrangement, and is implicated in neurotransmitter release and cell proliferation. Increased levels of C18 LPA in human plasma are correlated with ovarian cancer and atherosclerosis, indicating its potential utility as a biomarker in oncological and cardiovascular research. -
HCN Channel Blocker
Ivabradine impurity 1 is a derivative of Ivabradine, a hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker. This compound has been utilized in research to investigate the modulation of cardiac rhythms and treatment of conditions such as angina and heart failure. Its biological activity contributes to the understanding of ion channel interactions and cardiac electrophysiology. -
Overoxidized By-product of Lansoprazole
Lansoprazole N-oxide is the overoxidized by-product derived from the synthesis of the proton pump inhibitor Lansoprazole. This compound is of interest for studies related to gastrointestinal disorders, including duodenal and gastric ulcers, reflux esophagitis, and Zollinger–Ellison syndrome. Researchers may utilize Lansoprazole N-oxide to deepen the understanding of proton pump inhibition and its implications in these conditions. -
Drug Metabolite
15-Hydroxy Lubiprostone is an active metabolite of the laxative drug Lubiprostone, primarily targeting chloride channels. This compound exhibits biological activity by promoting fluid secretion in the intestinal lumen, thereby facilitating bowel movements. It is mainly utilized in research applications focused on gastrointestinal pharmacology and the mechanisms of action related to chloride channel activation. -
Overoxidized By-product of Lansoprazole
Lansoprazole sulfone N-Oxide is an overoxidized by-product generated during the synthesis of the proton pump inhibitor Lansoprazole. This compound is relevant for research into gastrointestinal conditions, such as duodenal and gastric ulcers, reflux esophagitis, and Zollinger–Ellison syndrome. Its study may provide insights into the metabolic pathways and potential therapeutic implications related to proton pump inhibition. -
Bupivacaine metabolite
Bupivacaine N-oxide hydrochloride is a metabolite of the local anesthetic Bupivacaine, which primarily acts as an NMDA receptor inhibitor. It also exhibits significant activity by blocking sodium, L-calcium, and potassium channels, particularly SCN5A channels with an IC50 of 69.5 μM. This compound is relevant for research into chronic pain mechanisms and provides insight into the pharmacological action of Bupivacaine and its derivatives. -
Active Metabolite of T-1095
T-1095A is the active metabolite of T-1095, functioning as a sodium-glucose cotransporter (SGLT) inhibitor. This compound demonstrates significant biological activity in the regulation of glucose reabsorption in the renal system and is primarily utilized in research related to diabetes and metabolic disorders. Its mechanism of action aids in the investigation of glucose homeostasis and associated therapeutic strategies. -
Sodium Channel Inhibitor
Decarbamoylsaxitoxin is a potent sodium channel inhibitor that selectively blocks the influx of sodium ions in excitable tissues, such as nerve and skeletal muscle cells, thus preventing action potential generation. As a hydrolysis product of saxitoxin, Decarbamoylsaxitoxin exhibits similar neurotoxic effects, including the ability to inhibit veratridine- and ouabain-induced neuroblastoma cell swelling and lysis. This reagent is valuable for research involving mechanisms of paralytic shellfish poisoning and sodium channel pharmacology. -
Drug Metabolite Control
Nicorandil pyridine oxide is a metabolite of Nicorandil, which acts as an activator of the sulfonylurea receptor 2B (SUR2B) and the ATP-sensitive potassium channel Kir6.2. This compound serves as a crucial tool for drug metabolite control, offering insights into the pharmacokinetics and therapeutic mechanisms of Nicorandil. Its biological activity is important for researchers studying cardiovascular effects and the modulation of ion channels in various biological systems. -
EBP Inhibitor
EBP-IN-1 is a selective inhibitor of emopamil binding protein (EBP) that effectively crosses the blood-brain barrier. This compound demonstrates an IC50 of 8.2 μM against human ERG potassium channels in CHO cells, leading to the inhibition of EBP's sterol isomerase activity and subsequent accumulation of Zymostenol. EBP-IN-1 has been shown to promote oligodendrocyte differentiation in human cortical organoids, making it a valuable tool for research into multiple sclerosis and related neurological disorders. -
VGSC Blocker
KC 12291 hydrochloride is a potent blocker of voltage-gated sodium channels (VGSC). It effectively reduces sustained Na+ current amplitude, demonstrating notable anti-ischemic properties. This compound exhibits significant cardioprotective effects in both in vitro and in vivo studies, making it a valuable tool for cardiac research and the investigation of sodium channel-related pathophysiology. -
Sodium Channels Blocker
Phrixotoxin 3 is a selective blocker of voltage-gated sodium channels, demonstrating IC50 values of 0.6 nM for NaV1.2, 42 nM for NaV1.3, 72 nM for NaV1.4, 288 nM for NaV1.1, and 610 nM for NaV1.5. This compound modulates sodium channel activity by shifting gating kinetics in a depolarized direction while inhibiting the inward sodium current. Phrixotoxin 3 is valuable for research focusing on ion channel modulation, neurophysiology, and the investigation of sodium channel-related pathologies. -
Sodium Current Blocker
F-15845 hydrobromide is a potent persistent sodium current blocker, primarily targeting voltage-gated sodium channels. It demonstrates significant cardioprotective properties and anti-ischemic activity, providing both short- and long-term protection following myocardial infarction. This compound is valuable for investigating functional impairments in the myocardium and exploring therapeutic strategies related to cardiac health. -
Sodium Channel Antagonist
Hainantoxin-IV is an antagonist of voltage-gated sodium channels, specifically targeting tetrodotoxin-sensitive (TTX-S) subtypes. This compound exhibits potent inhibitory activity through its interaction with key residues His28 and Lys32, which facilitate binding to the sodium channel. Hainantoxin-IV, characterized by an inhibitor cystine knot motif, is valuable in research applications exploring sodium channel modulation and related neurophysiological processes. -
AMPAR Agonist
(S)-(-)-5-Fluorowillardiine hydrochloride is a selective agonist of the alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR). This compound exhibits significant biological activity by enhancing synaptic transmission and promoting excitatory neurotransmission in the central nervous system. It is valuable for research applications focused on studying synaptic plasticity, neurophysiology, and potential therapeutic interventions in neurological disorders related to glutamate signaling. -
AMPA Receptor Modulator
AMPA Receptor Modulator-8 selectively modulates AMPA receptors, exhibiting an IC50 of 0.02 nM for TARP-γ2. This compound plays a significant role in the investigation of neurological disorders such as epilepsy, Alzheimer's disease, and Parkinson's disease. Its precise action on AMPA receptor dynamics makes it a valuable tool for advancing research in neuropharmacology and therapeutic development. -
AMPA-type Receptors Positive Allosteric Modulator
S 18986 is a selective positive allosteric modulator of AMPA-type receptors, demonstrating significant brain penetration and oral bioavailability. This compound enhances cognitive function in rodent models, evidenced by its ability to activate the release of noradrenaline and acetylcholine in the rat hippocampus. S 18986 has shown efficacy in improving memory performance in object-recognition tests, making it a valuable tool for research into cognitive enhancement and neuropharmacology. -
AMPA Receptor Antagonist
Selurampanel is a competitive antagonist of the AMPA receptor, demonstrating an IC50 of 190 nM. This compound exhibits significant penetration of the blood-brain barrier, making it suitable for in vivo studies. Selurampanel is primarily employed in research related to epilepsy, providing insights into neuroprotective mechanisms and potential therapeutic applications. -
AMPA Receptor Modulator
AMPA Receptor Modulator-2 is a selective modulator of AMPA receptors, demonstrating a pIC50 of 10.1 for TARPγ8-dependent AMPA receptor activity. This compound enhances synaptic transmission and plasticity, making it a valuable tool for research in neuropharmacology and cognitive disorders. Its ability to influence excitatory neurotransmission positions it as a potential candidate for studies related to neurodegenerative diseases and memory enhancement. -
Anti-parkinson Agent
Budipine is an anti-Parkinson agent that acts primarily as an N-methyl-D-aspartate (NMDA) antagonist while also influencing dopaminergic activity. It enhances dopamine release and inhibits monoamine oxidase type B (MAO-B), contributing to its therapeutic effects. As a substrate of P-glycoprotein (P-gp), Budipine's uptake into the brain is mediated by this transport mechanism. This compound is valuable for research into central nervous system disorders, including Parkinson's disease. -
AMPA Modulator
ZCAN262 is an allosteric modulator of AMPA receptors that effectively inhibits AMPA-mediated excitotoxicity. By targeting a specific allosteric binding site, ZCAN262 enhances the regulation of synaptic transmission. This compound is relevant for research focused on neuroprotection and synaptic plasticity, making it a valuable tool in studies of neurodegenerative diseases and cognitive function. -
AMPA Receptor Positive Allosteric Modulator
AMPA receptor modulator-10 is a positive allosteric modulator of the AMPA receptor, specifically targeting the GluA2 subtype with a potent pEC50 of 5.0. This compound enhances glutamate-induced calcium influx and current responses, demonstrating significant potential for reversing memory impairment induced by Scopolamine. AMPA receptor modulator-10 is applicable in research focused on neurological diseases, including schizophrenia, aiming to improve cognitive function and understanding of synaptic plasticity. -
AMPA Antagonist
BDZ-g is a potent and selective antagonist of the AMPA receptor, a key component in excitatory neurotransmission. This compound demonstrates significant biological activity in modulating synaptic transmission, making it valuable for research related to neurological disorders characterized by excessive AMPA receptor activity, such as epilepsy and neurodegenerative diseases. BDZ-g can serve as an important tool in understanding the role of AMPA receptors in various pathophysiological conditions. -
AMPAR Inhibitor.
D15 is an AMPA receptor (AMPAR) endocytosis inhibitor derived from a 15 amino acid segment of dynamin. It inhibits the interaction of dynamin with amphiphysin 1 and 2, leading to a significant increase in AMPAR excitatory postsynaptic potential (EPSC) amplitude in medium spiny neurons (MSNs) within Sapap3 knockout mice. This peptide has valuable applications in the investigation of neuropsychiatric disorders and related signaling pathways. -
AMPA Receptor Modulator
AMPA Receptor Modulator-3 is an allosteric modulator of the AMPA receptor, exhibiting an EC50 of 4.4 μM. This compound is valuable for investigating the role of AMPA receptors in the mammalian nervous system, particularly in studies related to learning and memory processes. Its modulation of glutamatergic signaling makes it a pertinent tool for neurological research and drug development targeting cognitive functions. -
GluR1/2/AMPA Receptor Agonist
Cl-HIBO is a highly selective agonist for the GluR1 and GluR2 subtypes of AMPA receptors, exhibiting EC50 values of 4.7 μM and 1.7 μM, respectively. This compound demonstrates potent activity as an AMPA receptor agonist with an IC50 of 0.22 μM. Additionally, Cl-HIBO displays desensitizing properties, making it a valuable tool for research in neuropharmacology and studies of synaptic transmission. -
AMPA Receptor Activator
NPEC-caged-(S)-AMPA is a photolabile caged analog of (S)-AMPA, specifically designed to target and activate AMPA receptors. This compound utilizes the NPEC photoprotecting group to selectively release (S)-AMPA upon illumination, enabling precise spatial and temporal control of receptor activation. It serves as a valuable tool in neuroscience research, facilitating studies on synaptic transmission and signal transduction pathways mediated by glutamate receptors. -
AMPA Receptor Modulator
AMPA receptor modulator-11 is a positive allosteric modulator of the AMPA receptor, enhancing synaptic transmission and promoting excitatory neurotransmission. This compound plays a significant role in research related to neuropsychiatric disorders such as depression, schizophrenia, Alzheimer’s disease, and attention deficit hyperactivity disorder (ADHD). Its ability to selectively target AMPA receptors makes it an essential tool for exploring therapeutic strategies in these conditions. -
AMPA Receptor Modulator
JNJ-56022486 is a potent negative modulator of the AMPA receptor, exhibiting a Ki value of 19 nM and selective antagonism for TARP-γ8. This compound demonstrates effective blood-brain barrier permeability, making it suitable for in vivo studies. JNJ-56022486 is primarily utilized in research focused on epilepsy and related neurological disorders, providing a valuable tool for investigating synaptic transmission and excitability in the central nervous system. -
AMPA Receptor Antagonist
CP-465022 hydrochloride is a selective noncompetitive antagonist of the AMPA receptor, exhibiting significant anticonvulsant activity. It effectively inhibits kainate-induced responses in rat cortical neurons with an IC50 of 25 nM. This compound serves as a valuable tool for exploring the physiological and pathophysiological roles of AMPA receptors in various neurological contexts. -
NMDA Receptor Antagonist
Remacemide hydrochloride is a weak uncompetitive antagonist of the NMDA receptor, exhibiting IC50 values of 68 μM for MK-801 binding and 76 μM for NMDA-induced currents. As a moderate inhibitor of sodium channels, this compound demonstrates anticonvulsant properties, making it a valuable tool in the study of neuropharmacology. Research applications include investigating mechanisms underlying seizure disorders and testing potential therapeutic approaches for neurological conditions.
