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Ion Channel Targets Drugged Strategy

Calcium Homeostasis Neurodegeneration Cellular Stress

Ion channel target drugging uses small molecules, peptides, biologics, natural products, and emerging light-controlled compounds to modulate channels that regulate membrane potential, ion flux, excitability, secretion, contraction, pain signaling, and cellular homeostasis. Ion channels are established therapeutic targets, but they remain underexploited because many clinical agents lack subtype selectivity and can produce toxicity or suboptimal efficacy[1][2].

Mechanistically, drugged ion-channel strategies act through pore blockade, voltage-sensor modulation, ligand-gating control, allosteric regulation, state-dependent inhibition, trafficking effects, and functional stabilization of open, closed, or inactivated states. Voltage-gated sodium, calcium, and potassium channels support action potential generation and propagation in excitable cells, while TRP channels connect structural biology, sensory signaling, pain, respiratory disease, neurological disease, psychiatric disease, diabetes, and cancer research. Structural advances, cryo-electron microscopy, and binding-site mapping now support rational design of channel modulators with improved precision[2][3][4].

Disease applications span pain, epilepsy, cardiac arrhythmia, hypertension, neurological disease, gastrointestinal dysfunction, cancer, diabetes, and viral infection. Sodium-channel blockers are used for pathological firing in pain, epilepsy, and arrhythmia, while calcium-channel blockers support cardiovascular therapy. TRP-channel programs began largely in pain but expanded into respiratory, neurological, psychiatric, metabolic, and oncology indications. Host ion channels also support replication of several viruses, creating opportunities to repurpose ion-channel inhibitors for emerging viral diseases[1][3][5].

The main gaps are subtype selectivity, safety margins, assay throughput, state dependence, tissue specificity, and translation from binding to functional efficacy. Future ion-channel drug discovery should combine automated electrophysiology, structural pharmacology, computational ultra-large library screening, venom-peptide libraries, functional antibody discovery, photopharmacology, and disease-relevant cellular models. Experimental planning should measure channel state, ion selectivity, kinetics, off-target channel panels, cardiac safety, pharmacodynamics, and disease-context biomarkers before advancing ion-channel drug candidates[2][4][6][7].

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Cat. No. Product Name Information Application Publication
HY-100381 Nigericin sodium salt
Nigericin sodium salt is an antibiotic derived from Streptomyces hygroscopicus that act as a K+/H+ ionophore, promoting K+/H+ exchange across mitochondrial membranes. Nigericin sodium salt is a NLRP3 activator. Nigericin sodium salt shows promising anti-cancer activities through decreasing intracellular pH (pHi), and inactivation of Wnt/β-catenin signals. Nigericin sodium salt induces pyroptosis through caspase 1/GSDMD in TNBC.

Source: Streptomyces hygroscopicus

Potassium Channel   NOD-like Receptor (NLR)   Bacterial   Antibiotic   Pyroptosis   Wnt   β-catenin  
Breast Cancer   Colorectal Cancer   Prostate Cancer   Gastric Cancer   Liver Cancer   Ovarian Cancer   Bacterial Infection   Depression   Hypertension   Lung Fibrosis   Rheumatoid Arthritis  
258
HY-127019 Nigericin
Nigericin is an antibiotic derived from Streptomyces hygroscopicus that act as a K+/H+ ionophore, promoting K+/H+ exchange across mitochondrial membranes. Nigericin is a NLRP3 activator. Nigericin shows promising anti-cancer activities through decreasing intracellular pH (pHi), and inactivation of Wnt/β-catenin signals. Nigericin induces pyroptosis through caspase 1/GSDMD in TNBC.
Potassium Channel   NOD-like Receptor (NLR)   Bacterial   Antibiotic   Pyroptosis   Wnt   β-catenin  
Breast Cancer   Colorectal Cancer   Prostate Cancer   Gastric Cancer   Liver Cancer   Ovarian Cancer   Bacterial Infection   Depression   Hypertension   Lung Fibrosis   Rheumatoid Arthritis  
258
HY-17386 Rosiglitazone
Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM), with blood-brain barrier permeability. Rosiglitazone is an TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone can be used in the research of obesity and diabetes, senescence, ovarian cancer.
PPAR   TRP Channel   Autophagy   Ferroptosis   Apoptosis  
Digestive System Disease   Prostate Cancer   Ovarian Cancer   Viral Infection   Depression   Pain   Digestive System Inflammation   Non-Small Cell Lung Cancer   SARS-CoV-2 Infection   Type 2 Diabetes   Obesity  
197
HY-100545 BAPTA-AM
BAPTA-AM is a well-known membrane permeable Ca2+ chelator. BAPTA-AM inhibits hERG channels, hKv1.3 and hKv1.5 channels in HEK 293 cells with IC50s of 1.3 μM, 1.45 μM and 1.23 μM, respectively.
Potassium Channel  
Cardiovascular Disease   Alzheimer's Disease  
155
HY-P1410A GsMTx4 TFA
GsMTx4 TFA is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 TFA also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 TFA is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology.
TRP Channel   Piezo Channel  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease   Blood or Cardio-cerebrovascular Disease  
135
HY-P1410 GsMTx4
GsMTx4 is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology.
TRP Channel   Piezo Channel  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease   Blood or Cardio-cerebrovascular Disease  
135
HY-18723 Yoda 1
Yoda 1 is a potent and selective Piezo1 agonist. Yoda 1 activates purified Piezo1 channels. Yoda 1 potently inhibits macropinocytosis induced by epidermal growth factor (EGF). Yoda 1 enhances Ca2+ influx followed by activation of the calcium-activated potassium channel KCa3.1 and inhibition of Rac1 activation.
Piezo Channel   Akt   ERK   Potassium Channel  
Pancreatic Cancer   Depression   Pain   Digestive System Inflammation   Cardiovascular Disease   Lung Fibrosis  
120
HY-101840 EIPA
EIPA (L593754) is an orally active TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA also enhances autophagy by inhibiting Na+/H+-exchanger 3 (NHE3). EIPA inhibits macropinocytosis as well. EIPA can be used in the research of inflammation and cancers, such as gastric cancer, colon carcinoma, pancreatic carcinoma.
TRP Channel   Prostaglandin Receptor   Autophagy   COX   Na+/H+ Exchanger (NHE)  
Colorectal Cancer   Prostate Cancer   Gastric Cancer   Pancreatic Cancer   Depression   Pain   Rheumatoid Arthritis  
112
HY-L028 CNS-Penetrant Compound Library
The blood-brain barrier (BBB) is the complex network of brain microvessels. It protects the brain from the external bloodstream environment and supplies the brain with the required nutrients for normal function. However, blood-brain barrier is also the obstacle to deliver beneficial drugs to treat CNS (central nervous system) diseases or brain tumors, as it has the least permeable capillaries in the entire body due to physical barriers (tight junctions). Therefore, it is crucial to discover drugs which can cross this barrier for the treatment of brain-based diseases, such as Alzheimer’s disease (AD), Parkinson’s disease (PD) and epilepsy. MCE offers a unique collection of 1,170 compounds with confirmed CNS-Penetrant property. It’s a useful tool for the discovery of drugs used for brain diseases, such as brain tumors, mental disorders, and neurodegenerative diseases.

Compound Characteristic Classified Libraries

91
HY-L011 Membrane Transporter/Ion Channel Compound Library
Most of molecules enter or leave cells mainly via membrane transport proteins, which play important roles in several cellular functions, including cell metabolism, ion homeostasis, signal transduction, the recognition process in the immune system, energy transduction, etc. There are three major types of transport proteins, ATP-powered pumps, channel proteins and transporters. Transport proteins such as channels and transporters play important roles in the maintenance of intracellular homeostasis, and mutations in these transport protein genes have been identified in the pathogenesis of a number of hereditary diseases. In the central nervous system, ion channels have been linked to, but not limited to, many diseases such asataxias, paralyses, epilepsies, and deafness. This indicates the roles of ion channels in the initiation and coordination of movement, sensory perception, and encoding and processing of information. Ion channels are a major class of drug targets in drug development. MCE designs a unique collection of 2,278 smal-molecule modulators that can be used for the research of Ion Channel and Membrane Transporter or high throughput screening (HTS) related drug discovery.

Signaling Pathway Targeting Libraries

90
HY-10448 Capsaicin
Capsaicin ((E)-Capsaicin), an active component of chili peppers, is a TRPV1 agonist. Capsaicin induces a nociceptive response by binding to its receptors. Capsaicin has analgesic effects on neurological disorders. Capsaicin has antioxidant, anti-inflammatory, anti-cancer effects.
Environmental Pollutants   Endogenous Metabolite   Autophagy   TRP Channel   Apoptosis  
Digestive System Disease   Breast Cancer   Prostate Cancer   Viral Infection   Pain   Digestive System Inflammation   SARS-CoV-2 Infection  
87
HY-L109 Protein-protein Interaction Inhibitor Library
Protein protein interactions (PPI) have pivotal roles in life processes. The studies showed that aberrant PPI are associated with various diseases, including cancer, infectious diseases, and neurodegenerative diseases. The classic drug targets are usually enzymes, ion channels, or receptors, the PPI indicate new potential therapeutic targets. Therefore, targeting PPI is a new direction in treating diseases and an essential strategy for the development of new drugs. However, the design of modulators targeting PPI still faces tremendous challenges, such the difficult PPI interfaces for the drug design, lack of ligands reference, lack of guidance rules for the PPI modulators development and high-resolution PPI proteins structures. With the development of high-throughput technology, high-throughput screening is also gradually used for the identification of PPI inhibitors, but the compound library used for conventional target screening is not very effective in screening PPI inhibitors. To improve screening efficiency, MCE carefully selected 826 PPI inhibitors and mainly targeting MDM2-p53, Keap1-Nrf2, PD-1/PD-L1, Myc-Max, etc. MCE Protein-protein Interaction Inhibitor Library is a useful tool for PPI drug discovery and related research.

Signaling Pathway Targeting Libraries

86
HY-L095 Mechanoreceptors Compound Library
Mechanoreceptors convert different stimuli from the outside into electrical signals, enabling us to quickly respond to our environment. Mechanoreceptors are distributed throughout the body, including in the skin, tendons, muscles, joint capsules and viscera. In addition to the channels of TRP and Piezo mentioned in the Nobel Prize, there are also targets such as KCNK, ENaC and ASIC2, which play an important role in the environment perception and homeostasis of living organisms. MCE offers a unique collection of 391 compounds related to mechanoreceptors, which targeting different mechanoreceptors, such as TRP, Piezo, KCNK, ENaC, etc. MCE mechanoreceptors compound library is a powerful tool for studying mechanoreceptors and life perception.

Signaling Pathway Targeting Libraries

85
HY-L099 Targeted Diversity Library
MCE Targeted Diversity Library contains 2,294 compounds, covering more than 1000 targets and isoforms, such as GPCRs, Ion channel, variety of kinases, etc. 1-3 compounds with high potency and selectivity were carefully selected for each target and isoform. The bioactivity information of each compound has been clearly reported in the literatures. This library is a concise collection of small molecule compounds with comprehensive target coverage, which can be used for phenotypic screening at low cost.

General Bioactive Screening Libraries

85
HY-L046 Anti-Cardiovascular Disease Compound Library
Cardiovascular diseases (CVDs) are a group of disorders of the heart and blood vessels which include coronary heart disease, cerebrovascular disease, peripheral arterial disease, rheumatic heart disease, etc. CVDs are the number 1 cause of death globally. Smoking, unhealthy nutrition, aging population, lack of physical activity, arterial hypertension, or diabetes can promote cardiovascular disease like myocardial infarction or stroke. It is multifactorial and encompasses a multitude of mechanisms, such as eNOS uncoupling, reactive oxygen species formation, chronic inflammatory disorders and abnormal calcium homeostasis. Antioxidant, anti-inflammatory and anti-diabetes agents may reduce the cardiovascular disease risk. MCE supplies a unique collection of 2,468 compounds with confirmed anti-cardiovascular activity. These compounds mainly target metabolic enzyme, membrane transporter, ion channel, inflammation related signaling pathways. MCE Anti-Cardiovascular Disease Compound Library can be used for cardiovascular diseases related research and high throughput and high content screening for new drugs.

Disease Focused Libraries

84
HY-L070 Neuroprotective Compound Library
Neurodegenerative diseases are characterised by progressive dysfunction and death of neurons, such as Alzheimer’s disease, Parkinson’s disease, and multiple sclerosis (MS). Neuroprotection is an approach to preserve neurons so that neurons cannot be hurt by different pathological factors in neurodegenerative diseases. Neuroprotectors are some agonists and antagonists targeting some key targets in neuroprotactive signal pathways, such as calcium and sodium channel blockers, GABA receptor agonists, NMDA receptor Antagonists, etc. Current neuroprotectors cannot reverse existing damage, but they may protect against further nerve damage and slow down any degeneration of the central nervous system (CNS) and still play important roles in the treatment of neurodegenerative diseases. MCE offers a unique collection of 1,851 compounds with potential neuroprotective activities. These compounds mainly act on some key targets in neuroprotetive signal pathways, such as calcium channel, sodium channel, adenosine A1 receptor, etc. MCE Neuroprotective Compopund Library is a useful tool in neuroprotective drug discovery.

Compound Characteristic Classified Libraries

84
HY-L121 5-HT Receptor Compound Library
5-HT receptors, also called Serotonin receptors, are a group of G protein-coupled receptors (GPCRs) and ligand-gated ion channels (LGICs) found in the central and peripheral nervous systems. These receptors are now classified into seven families, 5-HT1–7, comprising a total of 14 structurally and pharmacologically distinct mammalian 5-HT receptor subtypes. The 5-HT receptors influence various biological and neurological processes such as aggression, anxiety, appetite, cognition, learning, memory, mood, nausea, sleep, andthermoregulation. The serotonin receptors are the target of a variety of pharmaceutical drugs, including many antidepressants, antipsychotics, anorectics, antiemetics, gastroprokinetic agents, antimigraine agents, hallucinogens, and entactogens. MCE 5-HT Receptor Compound Library consists of 430 5-HT receptor inhibitors and activators, which can be used for neuropsychiatric disorders drugs discovery.

Signaling Pathway Targeting Libraries

84
HY-E0156 8-Channel Handheld Screw Cap Decapper

MCE 8-Channel Handheld Screw Cap Decapper is a necessary tool for handling thousands of screw cap tubes. It can cap and open various types of screw cap tubes, making it convenient and fast to operate. This improves experimental efficiency and meets different needs.
83
HY-E0194 Round Cap Drivers for 8-Channel Handheld Screw Cap Decapper

MCE The MedChemExpress Round Cap Drivers for 8-Channel Handheld Screw Cap Decapper is compatible with 8-Channel Handheld Screw Cap Decapper (HY-E0156), which can be used for Capping/Recapping FluidX Screw Caps.
83
HY-L0104V UORSY New Generation Screening Library
UORSY New Generation Screening Library contains about 1,900,000 compounds. The library is a revolutionary collection of lead-like molecules with outstanding structural quality and diversity—New Generation Screening Library (NGSL). Its core is decorated with interesting building blocks, including important medicinal fragments such as peptide bonds, amino groups and hydroxyl groups. and designed for discovery of new Voltage-gated calcium channel blockers.
83
HY-L062 Neurotransmitter Receptor Compound Library
Neurotransmitter (NT) receptors, also known as neuroreceptors, are a broadly diverse group of membrane proteins that bind neurotransmitters for neuronal signaling. There are two major types of neurotransmitter receptors: ionotropic and metabotropic. Ionotropic receptors are ligand-gated ion channels, meaning that the receptor protein includes both a neurotransmitter binding site and an ion channel. The binding of a neurotransmitter molecule (the ligand) to the binding site induces a conformational change in the receptor structure, which opens, or gates, the ion channel. The term “metabotropic receptors” is typically used to refer to transmembrane G-protein-coupled receptors. Metabotropic receptors trigger second messenger-mediated effects within cells after neurotransmitter binding. In some neurological diseases, the neurotransmitter receptor itself appears to be the target of the disease process. Many neuroactive drugs act by modifying neurotransmitter receptors. A better understanding of neurotransmitter receptor changes in disease may lead to improvements in therapy. MCE designs a unique collection of 2,593 compounds targeting a variety of neurotransmitter receptors. MCE Neurotransmitter Receptor Compound Library is a useful tool for neurological diseases drug discovery.

Signaling Pathway Targeting Libraries

83
HY-L117 Calcium Channel Blocker Library
Calcium channel blockers (CCBs), also called calcium antagonists are compounds that slow the movement of calcium (Ca2+) through calcium channels into the cells of the heart and blood vessel walls. Calcium causes the heart and arteries to squeeze more strongly. By blocking calcium, calcium channel blockers allow blood vessels to relax and open. So calcium channel blockers are usually used to lower blood pressure, relieve chest pain (angina) and control an irregular heartbeat. MCE supplies a unique collection of 226 calcium channel blockers and antagonists, all of which have the identified inhibitory effect on calcium channel. MCE Calcium Channel Blocker Library is a useful tool for discovery of antihypertensive drugs and cardiovascular disease research.

Signaling Pathway Targeting Libraries

83
HY-L118 Sodium Channel Blocker Library
Sodium channels conduct sodium ions (Na+) through a cell's plasma membrane that are the source of excitatory currents for the nervous system and muscle. Na channels are classified according to the trigger that opens the channel for such ions, i.e. either a voltage-change (Voltage-gated, voltage-sensitive, or voltage-dependent sodium channel also called VGSCs or Nav channel) or a binding of a substance (a ligand) to the channel (ligand-gated sodium channels). Dysfunction in voltage-gated sodium channels correlates with neurological and cardiac diseases, including epilepsy, myopathies, pain and cardiac arrhythmias. Sodium channel blockers are used in the treatment of cardiac arrhythmia, pain and convulsion. MCE offers a unique collection of 199 sodium channel blocker and antagonists, all of which have the identified inhibitory effect on sodium channels. MCE Sodium Channel Blocker Library can be used for neurological and cardiac diseases drug discovery and sodium channel research.

Signaling Pathway Targeting Libraries

83
HY-L119 Potassium Channel Compound Library
Potassium channels are the most widely distributed type of ion channel and are found in virtually all living organisms. There are four major classes of K channels: voltage-gated potassium channel, calcium-activated potassium channel, inwardly rectifying potassium channel and tandem pore domain potassium channel. There is growing evidence that dysfunction in potassium channels correlates with several diseases, such as chronic hypertension, diabetes, hypercholesterolemia and atherosclerosis, etc. MCE Potassium Channel Compound Library consists of 337 potassium channel inhibitor and activators, which is a useful tool to discover drugs for cardiovascular diseases and potassium channel research.

Signaling Pathway Targeting Libraries

83
HY-L120 GABA Receptor Compound Library
GABA receptors are a class of receptors that respond to the neurotransmitter gamma-aminobutyric acid (GABA), the chief inhibitory neurotransmitter in the vertebrate central nervous system. There are two classes of GABA receptors: GABAA and GABAB. GABAA receptors are ligand-gated ion channels (also known as ionotropic receptors), whereas GABAB receptors are G protein-coupled receptors (also known asmetabotropic receptors). GABA receptors are significant drug targets in the treatment of neuropsychiatric disorders such as epilepsy, insomnia, and anxiety, as well as in anesthesia in surgical operations. MCE offers a unique collection of 206 GABA receptors inhibitors and activators, which is an efficient tool for neuropsychiatric disorders drugs discovery.

Signaling Pathway Targeting Libraries

83
HY-L145 Antihypertensive Compound Library
The majority of hypertensive patients have primary (or essential) hypertension, that is, hypertension in which secondary causes are not present. Management aims to control arterial pressure, prevent end-organ damage (cerebrovascular, cardiovascular, and renal), and reduce the risk of premature death. Antihypertensive drugs may be divided into two broad groups, the first group being those which directly or indirectly block the renin–angiotensin system (RAS), for example, ACEIs, angiotensin receptor antagonists (ARAs), direct renin inhibitors (DRIs), and to a lesser extent β-blockers. The second group of drugs works by increasing water and sodium excretion, thereby reducing intravascular volume, or by causing vasodilatation through non-RAS pathways, for example, diuretics and calcium channel blockers (CCBs). MCE offers a unique collection of 930 compounds with identified and potential antihypertensive activity. MCE Antihypertensive Compound Library is critical for antihypertensive drug discovery and development.

Disease Focused Libraries

83
HY-L150 Membrane Receptor-targeted Compound Library
Membrane receptors, also known cell surface receptors or transmembrane receptors, are transmembrane proteins embedded into the plasma membrane which play an essential role in maintaining communication between the internal processes within the cell and various types of extracellular signals. They act in cell signaling by receiving (binding to) extracellular molecules, which are also called ligands. These extracellular molecules include hormones, cytokines, growth factors, neurotransmitters, lipophilic signaling molecules such as prostaglandins, and cell recognition molecules. There are three kinds of membrane receptors: ion channel-linked receptors, enzyme-linked receptors and G-protein-linked receptors. They play important roles in keeping human normal physiologic processes. GPCRs and ion channels are important drug targets in drug discovery. MCE provides a unique collection of 7,133 compounds targeting a variety of membrane receptors. MCE Membrane reeptor-targeted Compound Library can be used for membrane receptor-focused screening and drug discovery.

Signaling Pathway Targeting Libraries

83
HY-L158 Highly Selective Inhibitors Library
According to reports, most known kinase inhibitors exert their effects through competitive binding in highly conserved ATP pockets. Although genetic techniques such as RNA interference can inactivate specific genes, most kinases are multi domain proteins, each of which has an independent function. Highly selective inhibitors have higher efficiency than non-selective inhibitors, and the selectivity to the target is at least 100 times higher. Therefore, ensuring the validation of targets with the most selective inhibitors is crucial for a more thorough understanding of the pharmacology of the kinase field. The Highly Selective Inhibitors Library contains 6,342 compounds, covering multiple targets and subtypes, such as GPCR protein family, Ion channel, multiple kinases, etc. The Highly Selective Inhibitors Library is an effective tool for screening different phenotypes

Compound Characteristic Classified Libraries

83
HY-L159 Highly Selective Activators Library
Agonistic drugs activate or stimulate their receptors, triggering responses that increase or decrease cell activity. The highly selective activators can act on specific biological or molecular targets, while non-selective activators may interfere with multiple targets or targets simultaneously. The highly selective activators reduce the likelihood of these non-specific effects by targeting specific targets, making research more precise and reliable. The Highly Selective Activators Library contains 2,192 compounds, covering multiple targets and subtypes, such as GPCR protein family, Ion channel, multiple kinases, etc. The Highly Selective Activators Library is an effective tool for screening different phenotypes.
83
HY-L165 Dopamine Receptor Compound Library
Dopamine receptor (DAR), widely distributed in the brain, plays a key role in regulating motor function, motivation, driving force and cognition. The role of DA is mediated by D1-type (D1, D5) and D2-type receptors (D2S, D2L, D3, D4), which are distributed in presynaptic, postsynaptic and extrasynaptic, projection neurons and interneurons. Each receptor has a different function. D1 and D5 receptors couple with G stimulation sites and activate Adenylyl cyclase. The activation of Adenylyl cyclase leads to the production of the second messenger cAMP, which leads to the production of protein kinase A (PKA), which leads to further transcription in the nucleus. D2 to D4 receptors are coupled to G inhibitory sites to inhibit adenylyl cyclase and activate potassium Ion channel. These receptors utilize phosphorylation cascades or direct membrane interactions to affect the functions of voltage-gated and neurotransmitter-gated channels, cytoplasmic enzymes, and transcription factors. Dopamine receptor plays an important role in daily life. MCE designs a unique collection of 282 small molecules related to dopamine receptor. It is a good tool for screening drugs from nervous system disease.

Signaling Pathway Targeting Libraries

83
HY-L166 Ion Channel Compound Library
Ion channel is a membrane-binding enzyme whose catalytic site is an ion conduction pore, which is opened and closed in response to specific environmental stimuli (voltage, ligand concentration, membrane tension, temperature, etc.). Ion channel provide pores for the passive diffusion of ions on the biofilm. Due to their high selectivity for ion, ion channel are generally classified as sodium (Na+ ), potassium (K+ ), calcium (Ca2+ ), chloride (Cl- ), and non-specific cation channel. Ion channel is an important contributor to cell signal transduction and homeostasis. In addition to electrical signal transduction, ion channel also have many functions: regulating vascular smooth muscle contraction, maintaining normal cell volume, regulating glandular secretion, protein kinase activation, etc. Therefore, dysfunction of ion channel can lead to many diseases, and its mechanism research is particularly important. MCE designs a unique collection of 1,751 small molecules related to ion channel, mainly targeting Na+ channel, K+ channel, Ca2+ channel, GABA receptor, iGluR, etc. It is an essential tool for research of cardiovascular diseases, Nervous system diseases and other diseases.

Signaling Pathway Targeting Libraries

83
HY-L923 Ion Channel Lead-like Compound Library
Ion channels are key proteins on the cell membrane that regulate the flow of ions across membranes. They participate in nearly all physiological processes, including nerve conduction, muscle contraction, heart rhythm, and pain perception. Abnormalities in their function can lead to various serious diseases such as arrhythmia, epilepsy, hypertension, neuropathic pain, and cancer. Therefore, ion channels are highly valuable drug targets—over 15% of approved drugs target ion channels currently, demonstrating their irreplaceable therapeutic value in cardiovascular, neurological, and analgesic fields. MCE has collected a library of over 5,000 reported ion channel-related bioactive compounds targeting major sites such as Na+ channels, K+ channels, Ca2+ channels, GABA receptors, iGluRs, and others. Using AI models, these compounds are characterized through both 2D representations (molecular fingerprints, pharmacophores) and 3D representations (3D conformation) to screen for a collection of lead-like compounds highly similar to known active molecules. Additionally, an hERG channel prediction algorithm integrating XGB and ISE mapping strategy is employed to assess and exclude potential cardiotoxicity in the library.. This step significantly reduces safety risks in subsequent screenings, particularly for ion channel drug development related to cardiovascular systems (e.g., Nav1.5, Cav1.2), effectively minimizing failures due to hERG inhibition and serving as a valuable tool for ion channel drug screening.

Focused and target libraries

83
HY-L950 7-Membered Ring Privileged Scaffold Lead-like Library
Seven-membered rings are privileged medium-sized scaffolds with distinct twist-chair conformations and greater 3D diversity than five- and six-membered rings. Their flexible conformations allow induced-fit protein binding and precise pharmacophore positioning. They also modulate Fsp³, pKa and logP to enhance solubility and permeability. Azepanes, oxepanes and benzodiazepines serve as bioisosteres for hit discovery against GPCRs, ion channels and kinases. Widely found in plant and microbial alkaloids, seven-membered heterocycles show excellent biocompatibility and target affinity. They underpin many approved drugs for CNS, cancer and infectious diseases, including diazepam, imipramine and carbamazepine. Clinical candidates further highlight their unique value. However, high transannular strain and synthetic difficulty limit their availability, leaving them rare in standard screening libraries. MCE 7 Membered Scaffold Library contains 2,792 structurally diverse, lead-like molecules covering azepanes, oxepanes, benzodiazepines and dibenzazepines. With varied substitutions, chiral centers and synthetic accessibility, it fills the shortage of medium-ring scaffolds. Ideal for HTS, virtual screening and SAR studies, these novel, patent-clear compounds offer a distinctive starting point for drug discovery in CNS disorders, oncology, antivirals and challenging targets such as PPIs.

According to Lead-like Structures

83
HY-W009724 2-Aminoethyl diphenylborinate
2-Aminoethyl diphenylborinate (2-APB) is a cell-permeable inhibitor of Inositol triphosphate receptor (IP3R). 2-Aminoethyl diphenylborinate also inhibits the store-operated Ca2+ (SOC) channel and activates some TRP channels (V1, V2 and V3). Additionally, 2-Aminoethyl diphenylborinate has inhibitory effects on vasospasm. At high concentrations, it exhibits specific anti-inflammatory and antioxidant effects in neural tissue.
Calcium Channel   TRP Channel   CRAC Channel  
Inflammation or Immune System Disease   Pain   Hypertension   Lung Fibrosis  
82
HY-17412 Minocycline hydrochloride
Minocycline hydrochloride is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline hydrochloride is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline hydrochloride shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline hydrochloride reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline hydrochloride inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect.
Bacterial   Antibiotic   HIF/HIF Prolyl-Hydroxylase   Apoptosis   MDM-2/p53   Potassium Channel   Calcium Channel  
Metabolic or Endocrine Disease   Breast Cancer   Colorectal Cancer   Prostate Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Ovarian Cancer   Viral Infection   Bacterial Infection   Depression   Digestive System Inflammation   Cardiovascular Disease   SARS-CoV-2 Infection   Lung Fibrosis  
76
HY-B0285 Amiloride
Amiloride (MK-870) is an inhibitor of both epithelial sodium channel (ENaC) and urokinase-type plasminogen activator receptor (uTPA). Amiloride is a blocker of polycystin-2 (PC2; TRPP2) channel.
Sodium Channel   TRP Channel   Apoptosis  
Metabolic or Endocrine Disease   Digestive System Disease   Pain   Digestive System Inflammation   Cardiovascular Disease  
72
HY-100965 Diphenyleneiodonium chloride
Diphenyleneiodonium chloride is a NADPH oxidase (NOX) inhibitor and also functions as a TRPA1 activator with an EC50 of 1 to 3 μM. Diphenyleneiodonium chloride selectively inhibits intracellular reactive oxygen species.
TRP Channel   NADPH Oxidase   Reactive Oxygen Species (ROS)  
Inflammation or Immune System Disease   Pain   Lung Fibrosis  
66
HY-15640 Capsazepine
Capsazepine is a synthetic analogue of the sensory neurone excitotoxin, and an antagonist of TRPV1 receptor with an IC50 of 562 nM.
TRP Channel   Apoptosis  
Cancer   Digestive System Disease   Pain   Digestive System Inflammation  
65
HY-B0545 Probenecid
Probenecid is a potent and selective agonist of transient receptor potential vanilloid 2 (TRPV2) channels. Probenecid also inhibits pannexin 1 channels.
TRP Channel   Bacterial   HIV  
Cancer   Metabolic or Endocrine Disease   Viral Infection   Bacterial Infection   Pain  
50
HY-19545A SCH-23390 hydrochloride
SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 hydrochloride is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM.
Dopamine Receptor   5-HT Receptor   Potassium Channel  
Depression   Alzheimer's Disease   Obesity  
35
HY-17504 Rosuvastatin Calcium
Rosuvastatin Calcium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Calcium potently blocks hERG current with an IC50 of 195 nM. Rosuvastatin Calcium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Calcium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
HMG-CoA Reductase (HMGCR)   Autophagy   Potassium Channel   Bacterial  
Prostate Cancer   Viral Infection   Bacterial Infection   Cardiovascular Disease   Glucose Metabolism   Alzheimer's Disease  
29
HY-15206 Glibenclamide
Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR). Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability. Glibenclamide can induce autophagy.
Potassium Channel   Mitochondrial Metabolism   Autophagy   CFTR   P-glycoprotein  
Digestive System Disease   Ovarian Cancer   Digestive System Inflammation   Glucose Metabolism   Alzheimer's Disease  
28
HY-W728531 Ac4ManNAz
Ac4ManNAz can be taken up by cells and is an azide-containing metabolic glycoprotein labeling reagent that selectively modifies proteins. Commonly used for cell labeling, tracking and proteomic analysis. Ac4ManNAz contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Ac4ManNAz can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
Biochemical Assay Reagents   p38 MAPK   Potassium Channel   Mitochondrial Metabolism  
Cancer  
17
HY-N2333 Resiniferatoxin
Resiniferatoxin ((+)-Resiniferatoxin), is a selective agonist of transient receptor potential vanilloid 1 (TRPV1) receptor agonist. Resiniferatoxin can be isolated from the Euphorbia resinifera plant. Resiniferatoxin eliminates TRPV1+ primary sensory afferents and blunt cardiac sympathetic afferent reflex for a relatively long period.
TRP Channel  
Cancer   Blood or Cardio-cerebrovascular Disease  
14
HY-B0112 Minoxidil
Minoxidil (U10858) is an ATP-sensitive potassium (KATP) channel opener, a potent oral antihypertensive agent and a peripheral vasodilator that promotes vasodilation also affects hair growth. Minoxidil is also a potent inhibitor of soybean lipoxygenaseare with an IC50 of 20 μM.
Potassium Channel  
Ovarian Cancer   Hypertension  
11
HY-117275 Meclofenamic acid
Meclofenamic acid (Meclofenamate) is a non-steroidal anti-inflammatory agent. Meclofenamic acid is a highly selective FTO (fat mass and obesity-associated) enzyme inhibitor. Meclofenamic acid competes with FTO binding for the m(6)A-containing nucleic acid. Meclofenamic acid is a non-selective gap-junction blocker. Meclofenamic acid inhibits hKv2.1 and hKv1.1, with IC50 values of 56.0 and 155.9 μM, respectively.
Fat Mass and Obesity-associated Protein (FTO)   Potassium Channel   Gap Junction Protein  
Inflammation or Immune System Disease   Alzheimer's Disease  
9
HY-D1297 ER-Tracker Green
ER-Tracker dye is a derivative of BODIPY series dyes coupled with Glibenclamide (HY-15206), highly selective binding to the endoplasmic reticulum, non-toxic to cells at low concentrations, this type of dye is an environmentally sensitive probe, and formaldehyde treatment can still retain part of the fluorescence, with high fluorescence life, good extinction coefficient and other characteristics. Glibenclamide is an atp-dependent K+ channel blocker (Kir6, KATP) and CFTR Cl-channel blocker that binds in the endoplasmic reticulum. ER-Tracker is not suitable for staining cells after fixation.
Fluorescent Dye  
8
HY-D0143 Quinine
Quinine is an orally active alkaloid extracted from cinchona bark, possessing various biological activities including antimalarial, antidengue virus (DENV), and anticancer properties. Quinine is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100 mV with an IC50 of 169 μM.
Parasite   Potassium Channel   Dengue Virus   Flavivirus  
Infection  
7
HY-W009356A L-Cystine monohydrochloride
L-Cystine monohydrochloride is an amino acid. L-Cystine is converted to L-Cysteine in the body. Moreover, L-Cystine/L-Cysteine conversion system is a channel on the cell membrane, which can maintain the internal REDOX homeostasis of E. coli.
Biochemical Assay Reagents  
5
HY-B1494 Picrotoxinin
Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors. Picrotoxinin inhibits α1β2γ2L GABAA receptor with an IC50 of 1.15 μM.
Chloride Channel   GABA Receptor  
Alzheimer's Disease   Parkinson's Disease  
4
HY-N6691 Veratridine
Veratridine (3-Veratroylveracevine) is a plant neurotoxin, a voltage-gated sodium channels (VGSCs) agonist. Veratridine inhibits the peak current of Nav1.7, with an IC50 of 18.39 µM. Veratridine regulates sodium ion channels mainly by activating sodium ion channels, preventing channel inactivation and increasing sodium ion flow.
Sodium Channel  
Neurological, Eye or Ear Disease  
4
HY-P10234 Poneratoxin
Poneratoxin is the modulator for voltage-gated sodium channel (NaV, EC50 for NaV1.6 and NaV1.7 is 97 nM and 2.3 µM), that lowers the voltage threshold for activation and inhibits the inactivation of channels, enhances the excitability of neurons, and leads to the transmission of pain signals.
Sodium Channel  
Neurological, Eye or Ear Disease  
3
HY-116330 Hyperforin
Hyperforin is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin modulates Ca2+ levels by activating Ca2+-conducting non-selective canonical TRPC6 channels and triggers adipose tissue thermogenesis via the Dlat-AMPK signaling axis to suppress obesity. Hyperforin also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model.
Calcium Channel   TRP Channel  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease  
3
HY-P2270Y Phalloidin-TRITC (solution)
Phalloidin-TRITC (solution) is a fluorescein derivative of Phalloidin, which can specifically label myof lin and display red fluorescence when labeled and can be observed using Tesred channels.
Arp2/3 Complex   Fluorescent Dye  
3
HY-P10234A Poneratoxin acetate
Poneratoxin acetate is the acetate salt form of Poneratoxin (HY-P10234). Poneratoxin acetate is the modulator for voltage-gated sodium channel (NaV, EC50 for NaV1.6 and NaV1.7 is 97 nM and 2.3 µM), that lowers the voltage threshold for activation and inhibits the inactivation of channels, enhances the excitability of neurons, and leads to the transmission of pain signals.
Sodium Channel  
Neurological, Eye or Ear Disease  
3
HY-P2270 Phalloidin-TRITC
Phalloidin-TRITC is a fluorescein derivative of Phalloidin, which can specifically label myof lin and display red fluorescence when labeled and can be observed using Tesred channels.
Fluorescent Dye   Arp2/3 Complex  
3
HY-116330A Hyperforin dicyclohexylammonium salt
Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca2+ levels by activating Ca2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin dicyclohexylammonium salt modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model.
TRP Channel   Calcium Channel  
Cancer   Neurological, Eye or Ear Disease  
3
HY-W004260 Arachidic acid
Arachidic acid is an orally bioavailable membrane fluidity modulator and receptor/ion channel effector. Arachidic acid does not activate arachidonic acid-sensitive K+ channels in rat midbrain and hypothalamic neurons. Arachidic acid alleviates age-related spatial cognitive impairment. Arachidic acid is applicable for research related to age-related spatial cognitive impairment.

Source: Bee Pollen

Endogenous Metabolite  
Neurodegenerative Disease  
3
HY-P0062 Ziconotide
Ziconotide (SNX-111), a peptide, is a potent and selective block of N-type calcium channels antagonist. Ziconotide reduces synaptic transmission, and can be used for chronic pain research.
Calcium Channel  
Cancer   Neurological, Eye or Ear Disease   Inflammation or Immune System Disease  
2
HY-P0062A Ziconotide TFA
Ziconotide TFA (SNX-111 TFA), a peptide, is a potent and selective block of N-type calcium channels antagonist. Ziconotide TFA reduces synaptic transmission, and can be used for chronic pain research.
Calcium Channel  
Cancer   Experimental Autoimmune Encephalomyelitis   Experimental Autoimmune Encephalomyelitis  
2
HY-P1075A CALP3 TFA
CALP3 TFA, a Ca2+-like peptide, is a potent Ca2+ channel blocker that activates EF hand motifs of Ca2+-binding proteins. CALP3 TFA can functionally mimic increased [Ca2+]i by modulating the activity of Calmodulin (CaM), Ca2+ channels and pumps. CALP3 TFA has the potential in controlling apoptosis in diseases such as AIDS or neuronal loss due to ischemia.
Calcium Channel  
Cancer   Neurological, Eye or Ear Disease  
2
HY-P1075 CALP3
CALP3, a Ca2+-like peptide, is a potent Ca2+ channel blocker that activates EF hand motifs of Ca2+-binding proteins. CALP3 can functionally mimic increased [Ca2+]i by modulating the activity of Calmodulin (CaM), Ca2+ channels and pumps. CALP3 has the potential in controlling apoptosis in diseases such as AIDS or neuronal loss due to ischemia.
Calcium Channel  
Cancer   Neurological, Eye or Ear Disease   Hypertension  
2
HY-B1500 2,2,2-Trichloroethanol
2,2,2-Trichloroethanol, the active form of Chloral hydrate, is an agonist for the nonclassical K2P channels TREK-1 (KCNK2) and TRAAK (KCNK4).
Potassium Channel   Endogenous Metabolite  
Neurological, Eye or Ear Disease  
2
HY-P5712 Gramicidin S
Gramicidin S (Gramicidin soviet) is a cationic cyclic peptide antibiotic that selectively targets bacterial cell membranes and has anticancer activity. Gramicidin S also exerts antibacterial activity by destroying membrane integrity and interfering with membrane protein function. Gramicidin S inserts into the phospholipid bilayer through hydrophobic amino acid residues, specifically binds to negatively charged membrane lipids and disrupts membrane structure, thereby inhibiting cell division and cell wall synthesis, and ultimately causing bacterial death. Gramicidin S also inhibits ion channels, with IC50s of 41 μM, 24 μM, and 3 μM for Na+/K+-ATPase, tobacco leaf plasma membrane Mg2+/K+-ATPase, and rat heart plasma membrane Ca2+-ATPase, respectively.
Antibiotic   Bacterial   Na+/K+ ATPase  
Bacterial Infection  
2
HY-P0062B Ziconotide acetate
Ziconotide acetate (SNX-111 acetate), a peptide, is a potent and selective block of N-type calcium channels antagonist. Ziconotide acetate reduces synaptic transmission, and can be used for chronic pain research.
Calcium Channel  
Cancer   Inflammation or Immune System Disease   Blood or Cardio-cerebrovascular Disease  
2
HY-Y0669 Pipecolic acid
Pipecolic acid is an orally bioavailable, blood-brain barrier-permeable metabolite of lysine with antioxidant, inhibitor, and inducer activity. Pipecolic acid modulates the YAP-GPX4 signaling pathway, reduces retinal vascular tube formation, and mitigates ferroptosis. Pipecolic acid potentiates voltage-sensitive Ca2+ channel currents and induces neuronal apoptosis. Pipecolic acid can be used for the research of diabetic retinopathy.
Endogenous Metabolite   YAP   Glutathione Peroxidase   Ferroptosis  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease   Metabolic or Endocrine Disease  
2
HY-K1052 Amphotericin B, Sterile

MCE Amphotericin B, Sterile (250 μg/mL) is a filtered and sterilized antibiotic solution that can be used directly in cell culture. Amphotericin B is a polyene antifungal antibiotic produced by Streptomyces nodosus. It can bind with sterols to form transmembrane channels, resulting in the leakage of intracellular substances, thus inhibiting fungal and yeast contamination.

Cell Biology Cell Culture Sterile Antibiotic Solution

2
HY-B1173 (+)-Camphor
(+)-Camphor (D-(+)-Camphor; (1R)-(+)-Camphor) is an isomer of Camphor. Camphor is an agonist of monoterpenoid transient receptor potential (TRP) channels (such as TRPV1, TRPV3, TRPM8) and an inhibitor of TRPA1 channels. Camphor's derivatives have multiple biological activities, including antibacterial, antiviral, antioxidant, analgesic and anticancer. Camphor can selectively activate cold-sensitive TRP channels and inhibit TRPA1-mediated nociceptive signals. Camphor stimulates the cold-sensing nerve endings in the skin and regulates the activity of ion channels to exert analgesic, anti-inflammatory and anti-itching effects. It also has anti-proliferative and anti-mutagenic activities on tumor cells, which may be related to inhibiting ribosome function or inducing cell apoptosis. Camphor can be absorbed through the skin and (+)-Camphor can be used in the study of muscle and joint pain and inflammation.
Environmental Pollutants   Bacterial  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease   Breast Cancer   Leukemia/Lymphoma/Myeloma   Bacterial Infection  
1
HY-P1651A SOR-C13 TFA
SOR-C13 TFA, a carboxy-terminal truncated peptide, is a high-affinity TRPV6 antagonist with an IC50 value of 14 nM. TRPV6 is a non-voltage gated calcium channel that is associated with malignancy and poor prognosis in breast cancer. SOR-C13 TFA has anticancer activity.
TRP Channel  
Cancer  
1
HY-P1604 ATX-II
ATX-II is a selective sodium channel modulator toxin. ATX-II enhances late sodium current, prevents full sodium channel inactivation, and generates persistent current fractions. ATX-II has pro-arrhythmic effect. ATX-II slows intrinsic heart rate, prolongs QT interval and sinus node recovery time, and causes sinus pauses and arrests. ATX-II can be used for the research of atrial fibrillation, long QT syndrome, and long QT3 syndrome.
Sodium Channel  
Inflammation or Immune System Disease   Arrhythmias  
1
HY-P1651 SOR-C13
SOR-C13, a carboxy-terminal truncated peptide, is a high-affinity TRPV6 antagonist with an IC50 value of 14 nM. TRPV6 is a non-voltage gated calcium channel that is associated with malignancy and poor prognosis in breast cancer. SOR-C13 has anticancer activity.
TRP Channel  
Cancer  
1
HY-P1604A ATX-II TFA
ATX-II TFA is a selective sodium channel modulator toxin. ATX-II TFA enhances late sodium current, prevents full sodium channel inactivation, and generates persistent current fractions. ATX-II TFA has pro-arrhythmic effect. ATX-II TFA slows intrinsic heart rate, prolongs QT interval and sinus node recovery time, and causes sinus pauses and arrests. ATX-II TFA can be used for the research of atrial fibrillation, long QT syndrome, and long QT3 syndrome.
Sodium Channel  
Inflammation or Immune System Disease   Arrhythmias  
1
HY-Y0537E Potassium chloride, for cell culture
Potassium chloride, for cell culture is potassium chloride that can be used for cell culture. Potassium chloride, for cell culture increases extracellular potassium ion concentration to induce cellular depolarization, thereby activating voltage-gated calcium channels and regulating intracellular calcium signaling. Potassium chloride, for cell culture upregulates Brn-5. Potassium chloride, for cell culture inhibits the proliferation of neurons and some plant cells.
Environmental Pollutants   Biochemical Assay Reagents   Potassium Channel   Calcium Channel  
Neurological, Eye or Ear Disease  
1
HY-113037C Farnesyl pyrophosphate ammonium
Farnesyl pyrophosphate (Farnesyl diphosphate) ammonium is a metabolic intermediate in the mevalonate (MVA) pathway. It is a TRP channel (TRPM2) agonist that triggers Ca2+ influx and cell death. Farnesyl pyrophosphate ammonium is a key branch substrate for cholesterol synthesis, ubiquinone synthesis, protein farnesylation, and geranylgeranyl pyrophosphate (GGPP) synthesis. Farnesyl pyrophosphate ammonium is used in research on cerebral ischemia, neurodegenerative diseases, pancreatic cancer, inflammation, and autoimmune diseases.
TRP Channel   Endogenous Metabolite   Calcium Channel  
Cancer   Neurological, Eye or Ear Disease   Inflammation or Immune System Disease  
1
HY-101238 Agmatine sulfate
Agmatine sulfate exerts modulatory action at multiple molecular targets, such as neurotransmitter systems, ion channels and nitric oxide synthesis. It is an endogenous agonist at imidazoline receptor and a NO synthase inhibitor.
Imidazoline Receptor   NO Synthase   Endogenous Metabolite  
Cancer   Neurological, Eye or Ear Disease  
1
HY-B0317BS Amlodipine-d4 besylate
Amlodipine-d4 (besylate) is the deuterium labeled Amlodipine besylate. Amlodipine besylate (Amlodipine benzenesulfonate), an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine besylate can be used for the research of high blood pressure and cancer.
Isotope-Labeled Compounds   Calcium Channel  
Cancer   Blood or Cardio-cerebrovascular Disease  
/
HY-108506S1 Licarbazepine-d4
Licarbazepine-d4 is the deuterium labeled Licarbazepine (HY-108506). Licarbazepine is a voltage-gated sodium channel blocker with anticonvulsant and mood-stabilizing effects.
Sodium Channel   Isotope-Labeled Compounds  
Neurological, Eye or Ear Disease  
/
HY-B0339S Primidone-d5
Primidone-d5 is the deuterium labeled Primidone. Primidone is the orally active inhibitor for TRPM3 (IC50 = 0.6 μM), RIP kinase and voltage-gated sodium channel, and the antagonist for GABA receptor. Primidone can be used as the analgesic and anticonvulsant agent.
Isotope-Labeled Compounds   RIP kinase   TRP Channel   Sodium Channel   GABA Receptor   Necroptosis  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease  
/
HY-P1218 Phrixotoxin 3
Phrixotoxin 3 is a potent blocker of voltage-gated sodium channels, with IC50s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and NaV1.5, respectively. Phrixotoxin 3 modulates voltage-gated sodium channels with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current.
Sodium Channel  
Neurological, Eye or Ear Disease  
/
HY-B1500R 2,2,2-Trichloroethanol (Standard)
2,2,2-Trichloroethanol (Standard) is the analytical standard of 2,2,2-Trichloroethanol. This product is intended for research and analytical applications. 2,2,2-Trichloroethanol, the active form of Chloral hydrate, is an agonist for the nonclassical K2P channels TREK-1 (KCNK2) and TRAAK (KCNK4).
Reference Standards   Potassium Channel   Endogenous Metabolite  
Neurological, Eye or Ear Disease  
/
HY-P5177 GsAF-II
GsAF-II is a peptide toxin that blocks hERG1 subtype potassium channels in a voltage-dependent manner. GsAF-II blocks Nav1.x subtype sodium channels.
Sodium Channel   Potassium Channel  
Neurological, Eye or Ear Disease  
/
HY-N15782 18:0-PhoDAG
18:0-PhoDAG is a photoswitchable diacylglycerol (DAG) that allows rapid photoactivation of these DAG-sensitive TRP channels.
TRP Channel  
Neurological, Eye or Ear Disease  
/
HY-B0347S3 Lacidipine-13C4
Lacidipine-13C4 is 13C labeled Lacidipine (HY-B0347). Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI).
Calcium Channel   Apoptosis   Reactive Oxygen Species (ROS)   Caspase   Isotope-Labeled Compounds  
Blood or Cardio-cerebrovascular Disease  
/
HY-P5159 Crotamine
Crotamine is a Na+ channel modulator. Crotamine is a 42 amino acid toxin cross-linked by three disulfide bridges. Crotamine has analgesic activity. Crotamine also interacts with lipid membranes and shows myonecrotic activity. Crotamine can be isolated from Crotalus durissus terrificus venom.
Sodium Channel  
Inflammation or Immune System Disease  
/
HY-A0093S1 Mexiletine-d3 hydrochloride
Mexiletine-d3 (hydrochloride) is deuterium labeled Mexiletine (hydrochloride). Mexiletine hydrochloride (KOE-1173 hydrochloride), a Class IB antianhythmic, is a non-selective voltage-gated sodium channel blocker[1][2].
Isotope-Labeled Compounds   Sodium Channel  
Blood or Cardio-cerebrovascular Disease  
/
HY-P5772 Jingzhaotoxin-II
Jingzhaotoxin-II, a 32 amino acid residues including two acidic and two basic residues, is a neurotoxin. Jingzhaotoxin-II inhibits voltage-gated sodium channels (VGSC) that significantly slows rapid inactivation of TTX-resistant (TTX-R) VGSC on cardiac myocytes with the IC50 of 0.26 μM.
Sodium Channel  
Neurological, Eye or Ear Disease  
/
HY-D1528 MTSEA-Fluorescein
MTSEA-Fluorescein is a fluorescent probe that can be used for ion channel research.
Sodium Channel  
Neurological, Eye or Ear Disease  
/
HY-P5179 Huwentoxin I
Huwentoxin I (HWTX-I) is a peptide toxin that inhibits voltage-gated sodium channels and N-type calcium channels. Huwentoxin I inhibits sodium channels in rat hippocampus and cockroach dorsal unpaired median (DUM) neurons with IC50 values of 66.1 and 4.80 nM, respectively.
Calcium Channel   Sodium Channel  
Neurological, Eye or Ear Disease  
/
HY-111157 Dezinamide
Dezinamide (ADD94057) is an antiepileptic agent. Dezinamide binds to the voltage-sensitive sodium channel.
Sodium Channel  
Neurological, Eye or Ear Disease  
/
HY-B1090S Cinnarizine-d8
Cinnarizine-d8 is a deuterium labeled Cinnarizine. Cinnarizine is an antihistamine and a calcium channel blocker.
Calcium Channel   Histamine Receptor  
Blood or Cardio-cerebrovascular Disease   Metabolic or Endocrine Disease  
/
HY-P5954 PLTX-II
PLTX-II is a calcium channel blocker. PLTX-II has a 44-residue peptide containing ten Cys residues and an O-palmitoylated threonine amide at the carboxy-terminus.
Calcium Channel  
/
HY-175395 Onychocin B
Onychocin B is a cyclic tetrapeptide isolated from Onychocola sclerotica. Onychocin B is a calcium channel blocker with an IC50 of 7.1 μM for Cav1.2.

Source: Onychocola sclerotica

Calcium Channel  
Blood or Cardio-cerebrovascular Disease  
/
HY-B1837S Cyfluthrin-d6
Cyfluthrin-d6 (β-Cyfluthi-d6) is deuterium labeled Cyfluthrin. Cyfluthrin is a type II pyrethroid and has effects on various insects. Cyfluthrin is a modulator of Nav1.8 sodium channels by repetitive stimulation. Cyfluthrin can be applied in agriculture,veterinary, insecticide,pyrethroid and stored product.
Isotope-Labeled Compounds   Sodium Channel  
Infection  
/
HY-P3065 Calcicludine
Calcicludine is a protein toxin from the venom of the green mamba that inhibits high-voltage-activated calcium channel, especially L-type calcium channel.

Source: Ceratogyrus cornuatus

Calcium Channel  
Neurological, Eye or Ear Disease  
/
HY-170424 D-myo-Inositol-1,3,4,5-tetrakisphosphate potassium
D-myo-Inositol-1,3,4,5-tetrakisphosphate potassium increases the extracellular Ca2+ entry through upregulation of voltage-gated calcium channels.
Biochemical Assay Reagents  
/
HY-N21842 Vincapusine
Vincapusine is an inhibitor of CaV3.1 calcium channel, with a IC50 of 11.83 μM against the human target. Vincapusine suppresses the functional activity of the CaV3.1 calcium channel. Vincapusine exerts antihypertensive activity by inhibiting the CaV3.1 calcium channel. Vincapusine is used in hypertension-related research.
Calcium Channel  
Hypertension  
/
HY-118328 Hymenidin
Hymenidin is a natural antagonist of serotonergic receptor and inhibitor of voltage-gated potassium channels. Hymenidin also induces cancer cell apoptosis.
5-HT Receptor   Potassium Channel  
/
HY-B0703S Eslicarbazepine acetate-d4
Eslicarbazepine acetate-d4 is deuterated labeled Eslicarbazepine acetate (HY-B0703). Eslicarbazepine acetate (BIA 2-093), an antiepileptic agent, is a dual a dual Inhibitor of β-Secretase and voltage-gated sodium channel.
Beta-secretase   Sodium Channel   Isotope-Labeled Compounds  
Neurological, Eye or Ear Disease  
/
HY-P2707 α-Dendrotoxin
α-Dendrotoxin (α-DTX) is a voltage-gated K+ channel blocker and an acid-sensing ion channel (ASIC) inhibitor. α-Dendrotoxin blocks Kv1.1, Kv1.2, Kv1.6 and D-type (ID) voltage-gated K+ channels, and reversibly inhibits slowly inactivating potassium currents. α-Dendrotoxin induces epilepsy-related behaviors in mice. α-Dendrotoxin can be used in studies related to tonic-clonic seizures.
Sodium Channel   Potassium Channel  
Epilepsy  
/
HY-P1218A Phrixotoxin 3 TFA
Phrixotoxin 3 TFA is a potent blocker of voltage-gated sodium channels, with IC50s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and NaV1.5, respectively. Phrixotoxin 3 TFA modulates voltage-gated sodium channels with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current.
Sodium Channel  
Neurological, Eye or Ear Disease  
/
HY-101238S Agmatine-d8 sulfate
Agmatine-d8 sulfate is a deuterium labeled Agmatine sulfate (HY-101238). Agmatine sulfate exerts modulatory action at multiple molecular targets, such as neurotransmitter systems, ion channels and nitric oxide synthesis. It is an endogenous agonist at imidazoline receptor and a NO synthase inhibitor.
Isotope-Labeled Compounds   Endogenous Metabolite   NO Synthase   Imidazoline Receptor  
Cancer   Neurological, Eye or Ear Disease  
/
HY-W094477D Magnesium sulfate heptahydrate, for molecular biology
Magnesium sulfate heptahydrate (for molecular biology) is a molecular biology-grade form of Magnesium sulfate (HY-Y1267). Magnesium sulfate is a calcium antagonist and a potent L-type calcium channel inhibitor, as well as a uterine contraction inhibitor. Magnesium sulfate has anti-inflammatory, anticonvulsant, vasodilatory, and neuroprotective effects. Magnesium sulfate can be used in research on diseases such as preeclampsia/eclampsia.
Environmental Pollutants   Interleukin Related   Phospholipase   COX   Calcium Channel   Biochemical Assay Reagents   NO Synthase   NF-κB  
Inflammation or Immune System Disease   Traumatic Brain Injury   Arrhythmias  
/
HY-W740651 Jasmolin II
Jasmolin II is an insecticide targeting voltage-gated sodium channels in insects. Jasmolin II leads to neuronal hyperexcitation and insect paralysis. Jasmolin II is promising for research of agricultural pests.
Insecticide   Sodium Channel  
Infection  
/
HY-B0563BS Ropivacaine-d7 hydrochloride
Ropivacaine-d7 hydrochloride is a deuterium labeled Ropivacaine (hydrochloride) (HY-B0563B). Ropivacaine hydrochloride is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane. Ropivacaine is widely used for neuropathic pain management in vivo.
Isotope-Labeled Compounds   Sodium Channel   Potassium Channel  
Neurological, Eye or Ear Disease  
/
HY-13764A dl-Tetrandrine
dl-Tetrandrine is an orally active and brain-penetrant calcium channel blocker that inhibits voltage-dependent calcium channels. dl-Tetrandrine selectively blocks Ca2+ influx with an IC50 value of approximately 1-10 μM. dl-Tetrandrine exerts anti-inflammatory, immunosuppressive, and anti-arrhythmic activities by inhibiting intracellular calcium overload, and can reverse multidrug resistance in tumor cells. dl-Tetrandrine is promising for research of autoimmune diseases (such as rheumatoid arthritis), cardiovascular diseases, and tumor drug resistance reversal.
Calcium Channel  
Inflammation or Immune System Disease   Blood or Cardio-cerebrovascular Disease  
/
HY-P5771 Jingzhaotoxin-IX
Jingzhaotoxin-IX, a C-terminally amidated peptide composed of 35 amino acid residues, is a neurotoxin. Jingzhaotoxin-IX inhibits voltage-gated sodium channels (both tetrodotoxin-resistant and tetrodotoxin-sensitive isoforms) and Kv2.1 channel. Jingzhaotoxin-IX has no effect on delayed rectifier potassium channel Kv1.1, 1.2 and 1.3.
Sodium Channel  
Neurological, Eye or Ear Disease  
/
HY-187605 Gymnopusin
Gymnopusin is an L-type voltage-dependent calcium channel blocker and vasorelaxant. Gymnopusin inhibits KCl- and Norepinephrine-induced contractility as well as CaCl2-induced contractions. Gymnopusin induces endothelium-independent relaxation involving the opening of ATP-sensitive and calcium-activated potassium channels. Gymnopusin disrupts membranes through tonoplast lysis, leading to electrolyte leakage, chlorophyll loss, and photobleaching in duckweed. Gymnopusin inhibits radicle elongation in Amaranthus hypochondriacus seedlings and exhibits phytotoxicity against duckweed. Gymnopusin shows moderate cytotoxicity against mammalian cell lines. Gymnopusin can be used for research on hypertension.
Calcium Channel  
Hypertension  
/
HY-W699451 MTSET chloride
MTSET chloride is a membrane-impermeable, thiol-specific reagent that primarily acts as an inhibitor of the Nav1.5 sodium channel. MTSET chloride reduces the peak sodium current amplitude of most mutant Nav1.5 channels, induces a hyperpolarizing shift in steady-state inactivation, and slows the recovery process, but shows no activity against wild-type and non-inactivating Nav1.5 channel mutants. MTSET chloride reacts covalently with T336C mutant P2X2 receptors, partially reversibly blocks ATP-induced cation currents, and exerts no effect on wild-type P2X2 receptors.
Sodium Channel  
/
HY-P3055 Dendrotoxin-I
Dendrotoxin-I (DTX-I) is a potent K+ channels blocker with IC50s of 0.13-50 nM for voltage-gated potassium channel subunits KV1.1, KV1.2 and KV1.6, respectively. Dendrotoxin-I, a neurotoxin, has the potential for cancer research.

Source: Dendroaspis polylepis and angusticeps

Potassium Channel  
Neurological, Eye or Ear Disease  
/
HY-P2949 Pandinotoxin Kα
Pandinotoxin Kα, isolated from the venom of Pandinus imperator, is the inhibitor of A-type potassium channel.
Potassium Channel  
Cancer  
/
HY-12515AS2 Nicardipine-d4 hydrochloride
Nicardipine-d4 hydrochloride is deuterated labeled Nicardipine hydrochloride (HY-12515A). Nicardipine hydrochloride (YC-93) is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine hydrochloride acts as an agent for chronic stable angina and for controlling blood pressure.
Autophagy   Calcium Channel   Isotope-Labeled Compounds  
Cancer   Neurological, Eye or Ear Disease  
/
HY-N3729 (-)-Denudatin B
(-)-Denudatin B is an antiplatelet agent. (-)-Denudatin B relaxed vascular smooth muscle by inhibiting the Ca2+ influx through voltage-gated and receptor-operated Ca2+ channels. And (-)-Denudatin B has nonspecific antiplatelet action
Calcium Channel  
Neurological, Eye or Ear Disease   Hypertension  
/
HY-B0517S Mepivacaine-d3
Mepivacaine-d3 is the deuterium labeled Mepivacaine. Mepivacaine is an amide-type local anesthetic agent. Mepivacaine binds to specific voltage-gated sodium ion channels in neuronal cell membranes, which inhibits both sodium influx and membrane depolarization.
Sodium Channel  
Neurological, Eye or Ear Disease  
/
HY-B1319S1 Pramocaine-d9 hydrochloride
Pramocaine-d9 (Pramoxine-d9) hydrochloride is the d9-labeled Pramocaine hydrochloride (HY-B1319). Pramocaine hydrochloride is a topical surface anesthetic and antipruritic agent. Pramocaine hydrochloride reversibly inhibits voltage-gated sodium channel, reduces transmembrane permeability of sodium ions, stabilizes cell membranes, prevents depolarization, blocks action potential conduction, and inhibits peripheral slow C-fiber pathways associated with pain, pruritus and thermoception. Pramocaine hydrochloride can be used in research related to chronic pruritus, renal pruritus, atopic dermatitis, xerotic pruritus, uremic pruritus, and cutaneous hyperalgesia/pain.
Isotope-Labeled Compounds   Sodium Channel  
Neurological, Eye or Ear Disease  
/
HY-142050 (R)-IDHP
(R)-IDHP is an isomer of IDHP, a salvia metabolite that exerts vasorelaxant effects by inhibiting Ca2+ release and Ca2+ inward flow in voltage-dependent and receptor-operated calcium channels in vascular smooth muscle cells. IDHP is used in studies of cardiovascular disease.
Calcium Channel  
Blood or Cardio-cerebrovascular Disease  
/
HY-P1281 Kaliotoxin
Kaliotoxin is a peptidyl inhibitor of neuronal BK-Type. Kaliotoxin can specific inhibit Kv channels and calcium-activated potassium channels. Kaliotoxin can be used for the research of the regulation of membrane potential and neuron excitability.
Potassium Channel  
Neurological, Eye or Ear Disease  
/
HY-D2266 FluoBar1
FluoBar1 is an imaging fluorescence probe modified by a barbiturate ligand with fluorescent coumarin. FluoBar1 can monitor L-type voltage-gated calcium channels (LTCC) in living cells in real time for the study of neurological diseases .
Fluorescent Dye  
Neurological, Eye or Ear Disease  
/
HY-N19650 Paspalicine
Paspalicine is an indole diterpenoid fungal metabolite with no tremorgenic activity in animals. Paspalicine targets the large-conductance calcium-activated potassium (maxi-K) channel, blocks channel activity, and modulates the binding of Charybdotoxin (HY-P0191) to the maxi-K channel via a positive allosteric mechanism that enhances toxin binding. Paspalicine can be used in studies related to ryegrass staggers.

Source: Claviceps paspali

Potassium Channel  
/
HY-P5920 Urotoxin
Urotoxin is an inhibitor of the potassium channel. Urotoxin has a selective affinity for hKv1.2 channel.
Potassium Channel  
Neurological, Eye or Ear Disease  
/
HY-W707161 4-Methyl-2-(1-piperidinyl)-quinoline-d10
4-Methyl-2-(1-piperidinyl)-quinoline-d10 is the deuterium labeled ML204 (HY-12949). ML204 is a potent, selective TRPC4/TRPC5 channel inhibitor, with at least 19-fold selectivity against TRPC6 and no appreciable effect on all other TRP channels, nor on voltage-gated sodium, potassium, or Ca2+ channels.
Isotope-Labeled Compounds   TRP Channel  
Neurological, Eye or Ear Disease  
/
HY-W094475D Magnesium sulfate heptahydrate, meets analytical specification of Ph. Eur. BP USP FCC
Magnesium sulfate heptahydrate, meets analytical specification of Ph. Eur. BP USP FCC (Magnesium sulfate heptahydrate, meets analytical specification of Ph. Eur. BP USP FCC) is a hydrate of Magnesium sulfate (HY-Y1267) suitable for cell culture. Magnesium sulfate is a calcium antagonist and a potent L-type calcium channel inhibitor, as well as a uterine contraction inhibitor. Magnesium sulfate has anti-inflammatory, anticonvulsant, vasodilatory, and neuroprotective effects. Magnesium sulfate can be used in research on diseases such as preeclampsia/eclampsia.
COX   Calcium Channel   NO Synthase   NF-κB   Interleukin Related   Phospholipase  
Inflammation or Immune System Disease   Traumatic Brain Injury   Arrhythmias  
/
HY-D2333 RhFNMB
RhFNMB is a dualchannel/localization single-molecule fluorescence probe for ATP and HOCl, with independent fluorescence responses in the light red channel with ATP (λex = 520 nm, λem = 586 nm) and deep red channel with HOCl (λex = 620 nm, λem = 688 nm).
Fluorescent Dye  
Inflammation or Immune System Disease  
/
HY-P5869 Kurtoxin
Kurtoxin is a selective Cav3 (T-type) voltage-gated Ca2+ channel gating inhibitor with a Kd of 15 nM for Cav3.1 (α1G T-type) Ca2+ channel. Kurtoxin can interact with high affinity with native neuronal high-threshold L-type, N-type, and P-type Ca2+ channels in central and peripheral neurons. Kurtoxin also shows cross-reactivity with voltage-gated Na+ channel.
Calcium Channel   Sodium Channel  
Neurological, Eye or Ear Disease  
/
HY-P5925 Ssm spooky toxin
Ssm Spooky Toxin is found in Scolopendra mutilans that potently inhibits KCNQ (voltage-gated potassium channel family 7) channels, with IC50s of 2.8 μM, 5.26 μM and 0.1-0.3 M for Kv7.4, Kv1.3, and Shal channel, respectivily. Ssm Spooky Toxin inhibits cytokine generation by specifically acting on the KV1.3 channel in T cells. Ssm Spooky Toxin plays an essential role in the centipede’s circulatory system .
Potassium Channel  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease  
/
HY-B1221S Flufenamic acid-d4
Flufenamic acid-d4 is deuterium labeled Flufenamic acid. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca2+ channels, modulating non-selective cation channels (NSC), activating K+ channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
Isotope-Labeled Compounds   COX   AMPK   Potassium Channel   Chloride Channel   Calcium Channel   Parasite  
Inflammation or Immune System Disease  
/
HY-W744263 Eslicarbazepine Acetate-d3
Eslicarbazepine Acetate-d3 is the deuterium labeled Eslicarbazepine acetate (HY-B0703). Eslicarbazepine acetate (BIA 2-093), an antiepileptic agent, is a dual a dual Inhibitor of β-Secretase and voltage-gated sodium channel.
Isotope-Labeled Compounds   Sodium Channel   Beta-secretase  
Neurological, Eye or Ear Disease  
/
HY-P2710 Noxiustoxin
Noxiustoxin is a toxin from the venom of the Mexican scorpion Centruroides noxius which block voltage-dependent potassium channel (Kv1.3, IC50 = 360 nM), and calcium-activated potassium channel. Noxiustoxin plays an important role in neuroinflammatory disease.
Potassium Channel  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease  
/
HY-D2223 Sulfo-Cy5 dUTP
Sulfo-Cy5 dUTP is a modified nucleoside triphosphate used for DNase labeling. Sulfo-Cy5 dUTP is a bright far-red emitting dye for the Cy5 channel.
Fluorescent Dye  
/
HY-116330AR Hyperforin dicyclohexylammonium salt (Standard)
Hyperforin dicyclohexylammonium salt (Standard) is the analytical standard of Hyperforin dicyclohexylammonium salt. This product is intended for research and analytical applications. Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca2+ levels by activating Ca2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin dicyclohexylammonium salt modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model.
Reference Standards   TRP Channel   Calcium Channel  
Neurological, Eye or Ear Disease  
/
HY-P5142 ω-Hexatoxin-Hv1a
ω-Hexatoxin-Hv1a (ω-ACTX-Hv1; ω-Atracotoxin-HV1) is an orally active insecticidal neurotoxin containing an inhibitor cystine knot motif and a selective calcium channel inhibitor. ω-Hexatoxin-Hv1a blocks L-type voltage-dependent Ca2+ channels and reduces intracellular calcium ion concentration, thereby decreasing apoptosis, necroptosis and oxidative stress, and promoting cell recovery and energy level elevation. ω-Hexatoxin-Hv1a causes larval paralysis and death by impairing neurotransmission in the central nervous system of insects. It shows high injectable toxicity against insects of multiple orders, but exhibits weak oral toxicity. ω-Hexatoxin-Hv1a is widely applicable to studies related to ischemia-reperfusion injury, atopic dermatitis, and ischemic injury of cardiomyocytes and neurons.
Insecticide   Calcium Channel   Apoptosis   Necroptosis  
Atopic Dermatitis   Ischemic Stroke  
/
HY-W777434 Mitiglinide calcium hydrate-d8
Mitiglinide (calcium hydrate)-d8 is the deuterium labeled Mitiglinide (calcium hydrate) (HY-B0682A). Mitiglinide calcium hydrate (KAD-1229), an insulinotropic agent, is an ATP-sensitive K+ (KATP) channel antagonist. Mitiglinide calcium hydrate is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell KATP channel). Mitiglinide Calcium hydrate can be used for the research of type 2 diabetes.
Isotope-Labeled Compounds   Potassium Channel  
Metabolic or Endocrine Disease  
/
HY-B0317AS1 Amlodipine-d9 maleate
Amlodipine-d9 maleate is deuterated labeled Amlodipine maleate (HY-B0317A). Amlodipine maleate is a dihydropyridine calcium channel blocker, acts as an orally active antianginal agent. Amlodipine maleate blocks the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine maleate can be used for the research of high blood pressure and cancer.
Calcium Channel   Isotope-Labeled Compounds  
Blood or Cardio-cerebrovascular Disease  
/
HY-17404S Cilnidipine-d7
Cilnidipine-d7 is deuterium labeled Cilnidipine. Cilnidipine is a long-acting, second-generation dihydropyridine Ca2+-channel blocker on L and N-type Ca2+ channel. Antihypertensive effects.
Isotope-Labeled Compounds   Calcium Channel  
Blood or Cardio-cerebrovascular Disease  
/
HY-B1751S1 Quinidine-13C, d2 hydrochloride
Quinidine-13C, d2 hydrochloride is the 13C, d2 labeled Quinidine hydrochloride (HY-W115674). Quinidine hydrochloride is an orally active antiarrhythmic agent. Quinidine hydrochloride reduces the expression level of P-gp, inhibits P-gp-mediated efflux, increases the intracellular accumulation of P-gp substrates, induces PARP cleavage and Caspase-3 activation, and elevates the proportion of Apoptotic cells at the sub-G1 phase. Quinidine hydrochloride exerts sustained block and open-channel block effects on IK(f). Quinidine hydrochloride alters the urinary metabolic ratio of Amphetamine, modulates the Pentylenetetrazol-induced seizure threshold, and regulates the anticonvulsant effect of Dextromethorphan. Quinidine hydrochloride can be used in studies related to uterine sarcoma and seizures.
Isotope-Labeled Compounds   P-glycoprotein   PARP   Caspase   Apoptosis   Potassium Channel  
Cervical Cancer   Epilepsy   Heart Disease  
/
HY-113037 (E/Z)-Farnesyl pyrophosphate
(E/Z)-Farnesyl pyrophosphate ((E/Z)-Farnesyl diphosphate), a 15-carbon isoprenoid, is a metabolic intermediate of the mevalonate (MVA) pathway. (E/Z)-Farnesyl pyrophosphate is a TRPM2 (TRP Channel) agonist, activates TRPM2 opening for ion influx. (E/Z)-Farnesyl pyrophosphate is a key branch substrate for cholesterol synthesis, ubiquinones synthesis, protein farnesylation decoration, and geranyl-geranyl pyrophosphate (GGPP) synthesis.
TRP Channel   Endogenous Metabolite  
Neurological, Eye or Ear Disease  
/
HY-N6691R Veratridine (Standard)
Veratridine (Standard) is the analytical standard of Veratridine. This product is intended for research and analytical applications. Veratridine (3-Veratroylveracevine) is a plant neurotoxin, a voltage-gated sodium channels (VGSCs) agonist. Veratridine inhibits the peak current of Nav1.7, with an IC50 of 18.39?μM. Veratridine regulates sodium ion channels mainly by activating sodium ion channels, preventing channel inactivation and increasing sodium ion flow.
Reference Standards   Sodium Channel  
Neurological, Eye or Ear Disease  
/
HY-N21823 Methyl isoplatydesmine
Methyl isoplatydesmine is a cholinesterase inhibitor with spasmolytic activity, with a Ki value of 30.0 μM against electric eel acetylcholinesterase and a Ki value of 19.0 μM against horse serum butyrylcholinesterase. Methyl isoplatydesmine mediates spasmolytic activity by blocking voltage-dependent calcium channels. Methyl isoplatydesmine can be used in the research of Alzheimer's disease and related dementias.
Cholinesterase (ChE)   Calcium Channel  
Alzheimer's Disease   Vascular Dementia  
/
HY-B0347S1 Lacidipine-13C8
Lacidipine-13C8 is the deuterium labeled Lacidipine. Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI).
Apoptosis   Caspase   Calcium Channel   Reactive Oxygen Species (ROS)  
Blood or Cardio-cerebrovascular Disease  
/
HY-P5152 Scorpion toxin Tf2
Scorpion toxin Tf2 is a selective human voltage-gated sodium channel Nav1.3 (hNav1.3) activator. Scorpion toxin Tf2 selectively shifts the channel's activation voltage to more negative values, enabling channel opening at resting membrane potentials. Scorpion toxin Tf2 can be used for the research of epilepsy, nociception (after spinal cord injury).
Sodium Channel  
Epilepsy   Pain  
/
HY-B0380S2 Trimebutine-d3 hydrochloride
Trimebutine-d3 hydrochloride is deuterium labeled Trimebutine hydrochloride. Trimebutine hydrochloride is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine hydrochloride inhibits L-type Ca2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine hydrochloride also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine hydrochloride also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine hydrochloride also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).
Apoptosis   Isotope-Labeled Compounds   Calcium Channel   ERK   Akt   Toll-like Receptor (TLR)   IRAK   NF-κB   Opioid Receptor   Potassium Channel   JNK  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease   Metabolic or Endocrine Disease  
/
HY-117275R Meclofenamic acid (Standard)
Meclofenamic acid (Standard) is the analytical standard of Meclofenamic acid. This product is intended for research and analytical applications. Meclofenamic acid (Meclofenamate) is a non-steroidal anti-inflammatory agent. Meclofenamic acid is a highly selective FTO (fat mass and obesity-associated) enzyme inhibitor. Meclofenamic acid competes with FTO binding for the m(6)A-containing nucleic acid. Meclofenamic acid is a non-selective gap-junction blocker. Meclofenamic acid inhibits hKv2.1 and hKv1.1, with IC50 values of 56.0 and 155.9 μM, respectively.
Reference Standards   Fat Mass and Obesity-associated Protein (FTO)   Potassium Channel   Gap Junction Protein   Endogenous Metabolite  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease   Metabolic or Endocrine Disease  
/
HY-P5155 Stromatoxin 1
Stromatoxin 1 is an inhibitor of Potassium Channel, a peptide which can be isolated from tarantulas. Stromatoxin 1 selectively inhibits K(V)2.1, K(V)2.2, K(V)4.2, and K(V)2.1/9.3 channels. K(V)2.1 and K(V)2.2, but not K(V)4.2, channel subunits play a key role in opposing both myogenic and neurogenic urinary bladder smooth muscle (UBSM) contractions in rats.
Potassium Channel  
Neurological, Eye or Ear Disease  
/
HY-B0233S2 Isradipine-d7
Isradipine-d7 is deuterated labeled Isradipine (HY-B0233). Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease.
Calcium Channel   Autophagy   Isotope-Labeled Compounds  
Neurological, Eye or Ear Disease   Blood or Cardio-cerebrovascular Disease  
/
HY-B0380S1 Trimebutine-d5 fumarate
Trimebutine-d5 fumarate is deuterium labeled Trimebutine fumarate. Trimebutine fumarate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine fumarate inhibits L-type Ca2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine fumarate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine fumarate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine fumarate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).
Apoptosis   Isotope-Labeled Compounds   Calcium Channel   ERK   Akt   Toll-like Receptor (TLR)   IRAK   NF-κB   Opioid Receptor   Potassium Channel   JNK  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease   Metabolic or Endocrine Disease  
/
HY-P5144 Aah II
Aah II is a sodium channel modulator. Aah II is a toxin that can be isolated from the venom of scorpion Androctonus australis.
Sodium Channel  
Inflammation or Immune System Disease  
/
HY-B1494R Picrotoxinin (Standard)
Picrotoxinin (Standard) is the analytical standard of Picrotoxinin. This product is intended for research and analytical applications. Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors. Picrotoxinin inhibits α1β2γ2L GABAA receptor with an IC50 of 1.15 μM.
Reference Standards   Chloride Channel   GABA Receptor  
Neurological, Eye or Ear Disease  
/
HY-N8372 Nalanthalide
Nalanthalide is a voltage-gated potassium channel Kv1.3 blocker (IC50=3.9 µM) and a potential immunosuppressant. Nalanthalide can be used for research on inflammatory immune diseases, such as neuroinflammation.

Source: Nalanthamala sp.

Potassium Channel  
Inflammation or Immune System Disease  
/
HY-W094475E Magnesium sulfate heptahydrate, United States Pharmacopeia (USP) Reference Standard
Magnesium sulfate heptahydrate, United States Pharmacopeia (USP) Reference Standard (Epsom salts (Pharmaceutical primary standard, USP)) is a reference standard for Magnesium sulfate (HY-Y1267). Magnesium sulfate is a calcium antagonist and a potent L-type calcium channel inhibitor, as well as a tocolytic. Magnesium sulfate has anti-inflammatory, anticonvulsant, vasodilatory, and neuroprotective effects. Magnesium sulfate can be used in the research of diseases such as preeclampsia/eclampsia.
Environmental Pollutants   Interleukin Related   Phospholipase   COX   Calcium Channel   Biochemical Assay Reagents   NO Synthase   NF-κB  
Inflammation or Immune System Disease   Traumatic Brain Injury   Arrhythmias  
/
HY-N1369S1 Menthol-d2
Menthol-d2 is deuterated labeled Menthol (HY-N1369). Menthol is an analgesic and TRPM8 modulator. TRPM8 is a cold temperature sensing ion channel, and Menthol can regulate TRPM8 to exert analgesic and anti-irritation mechanisms. Menthol stimulates cold receptors and produces a cooling sensation by inhibiting Ca++ currents in neuronal cell membranes.
Calcium Channel   Isotope-Labeled Compounds  
Neurological, Eye or Ear Disease  
/
HY-B1173R (+)-Camphor (Standard)
(+)-Camphor (Standard) is the analytical standard of (+)-Camphor. This product is intended for research and analytical applications. (+)-Camphor (D-(+)-Camphor; (1R)-(+)-Camphor) is an isomer of Camphor. Camphor is an agonist of monoterpenoid transient receptor potential (TRP) channels (such as TRPV1, TRPV3, TRPM8) and an inhibitor of TRPA1 channels. Camphor's derivatives have multiple biological activities, including antibacterial, antiviral, antioxidant, analgesic and anticancer. Camphor can selectively activate cold-sensitive TRP channels and inhibit TRPA1-mediated nociceptive signals. Camphor stimulates the cold-sensing nerve endings in the skin and regulates the activity of ion channels to exert analgesic, anti-inflammatory and anti-itching effects. It also has anti-proliferative and anti-mutagenic activities on tumor cells, which may be related to inhibiting ribosome function or inducing cell apoptosis. Camphor can be absorbed through the skin and (+)-Camphor can be used in the study of muscle and joint pain and inflammation.
Reference Standards   Bacterial  
Cancer   Neurological, Eye or Ear Disease   Inflammation or Immune System Disease  
/
HY-100168R BAPTA (Standard)
BAPTA (Standard) is the analytical standard of BAPTA. This product is intended for research and analytical applications. BBAPTA is a selective and cell-impermeant chelator for calcium. BAPTA, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA is widely used as an intracellular buffer for investigating the effects of Ca2+ release from intracellular stores or influx via Ca2+-permeable channels in the plasma membrane. BAPTA can also inhibit phospholipase C activity independently of their role as Ca2+ chelators.
Reference Standards   Phospholipase  
/
HY-126752R Ophthalmic acid (Standard)
Ophthalmic acid (Standard) is the analytical standard of Ophthalmic acid (HY-126752). This product is intended for research and analytical applications. Ophthalmic acid is a ubiquitous metabolite and glutathione modulator, with a Ki of 0.95 mM for glyoxalase I. Ophthalmic acid competitively inhibits glyoxalase I, glutathione S-transferase, glutaredoxin, glutamate-cysteine ligase, protein disulfide reductase (glutathione), as well as non-selective cation channels. Ophthalmic acid is applicable in diabetes-related research.
Reference Standards   Reactive Oxygen Species (ROS)  
Glucose Metabolism  
/
HY-101017R Palmitoylcarnitine chloride (Standard)
Eslicarbazepine acetate (Standard) is the analytical standard of Eslicarbazepine acetate. This product is intended for research and analytical applications. Eslicarbazepine acetate (BIA 2-093), an antiepileptic agent, is a dual a dual Inhibitor of β-Secretase and voltage-gated sodium channel.
Reference Standards   Endogenous Metabolite   Akt   Calcium Channel  
Cancer   Inflammation or Immune System Disease  
/
HY-17404S1 Cilnidipine-d4
Cilnidipine-d4 (FRC-8653-d4) is deuterium labeled Cilnidipine. Cilnidipine is a long-acting, second-generation dihydropyridine Ca2+-channel blocker on L and N-type Ca2+ channel. Antihypertensive effects.
Isotope-Labeled Compounds   Calcium Channel  
Blood or Cardio-cerebrovascular Disease  
/
HY-108506S Licarbazepine-d3
Licarbazepine-d3 is the deuterium labeled Licarbazepine (HY-108506). Licarbazepine is a voltage-gated sodium channel blocker with anticonvulsant and mood-stabilizing effects.
Sodium Channel  
Neurological, Eye or Ear Disease  
/
HY-B0682S Mitiglinide-d8 calcium hydrate
Mitiglinide-d8 calcium hydrate (KAD-1229-d8) is the deuterium labeled Mitiglinide calcium hydrate. Mitiglinide calcium hydrate (KAD-1229), an insulinotropic agent, is an ATP-sensitive K+ (KATP) channel antagonist. Mitiglinide calcium hydrate is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell KATP channel). Mitiglinide Calcium hydrate can be used for the research of type 2 diabetes.
Potassium Channel  
Metabolic or Endocrine Disease  
/
HY-N22000 N-Stearoyl valine
N-Stearoyl valine is an N-acyl derivative of valine. N-Stearoyl valine antagonizes intracellular calcium mobilization by binding to the TRPV3 channel as a bioactive endogenous ligand of transient receptor potential (TRP) channels. N-Stearoyl valine participates in physiological processes such as lipid metabolism and cell signal transduction as an endogenous metabolite. N-Stearoyl valine is also a flavor compound. N-Stearoyl valine can be used in research on biomarker detection, animal nutrition and amino acid metabolism, and the development of the food and beverage industry.
Endogenous Metabolite   TRP Channel  
/
HY-100168BR BAPTA tetrapotassium (Standard)
BAPTA tetrapotassium (Standard) is the analytical standard of BAPTA tetrapotassium (HY-100168B). This product is intended for research and analytical applications. BAPTA tetrapotassium is a selective and cell-impermeant chelator for calcium. BAPTA tetrapotassium, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA tetrapotassium is widely used as an intracellular buffer for investigating the effects of Ca2+ release from intracellular stores or influx via Ca2+-permeable channels in the plasma membrane. BAPTA tetrapotassium can also inhibit phospholipase C activity independently of their role as Ca2+ chelators.
Reference Standards   Phospholipase  
/
HY-A0093S Mexiletine-d6 hydrochloride
Mexiletine-d6 (hydrochloride) is a deuterium labeled Mexiletine hydrochloride (KOE-1173 hydrochloride). Mexiletine hydrochloride, a Class IB antianhythmic, is a non-selective voltage-gated sodium channel blocker.
Sodium Channel  
Blood or Cardio-cerebrovascular Disease  
/
HY-P5184 Hainantoxin-IV
Hainantoxin-IV is a specific antagonist of Sodium Channel, targeting to tetrodotoxin-sensitive (TTX-S) voltage-gated sodium channels. His28 and Lys32 are the key resiudes of Hainantoxin-IV for binding with target, while Hainantoxin-IV adopts an inhibitor cystine knot motif.
Sodium Channel  
Neurological, Eye or Ear Disease  
/
HY-N7875 Celangulin
Celangulin is an insecticidal component isolated from Celastrus angulatus. Celangulin activates the calcium channel on the plasma membrane with increasing the intracellular Ca2+ after influx from the external. Celangulin activates the calcium channel in the ER.
Others  
/
HY-149203 MQA-P
MQA-P is a multifunctional near-infrared (NIR) fluorescent probe for simultaneously detecting ONOO-, viscosity, and polarity within mitochondria. MQA-P exhibits a remarkable turn-on response to ONOO- (λem=645 nm) and is highly sensitive to viscosity/polarity in the NIR channel with λem>704 nm. MQA-P exhibits excited-state intramolecular charge transfer (ESICT) feature that is highly polarity-sensitive by engineering N,N-dimethylamino as the electron donor and a quinoline cationic unit as the electron acceptor. MQA-P is used for ferroptosis or cancer diagnosis in vitro and in vivo via dual-channel images.
Fluorescent Dye  
Cancer  
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HY-N3710 Dehydrocrenatidine
Dehydrocrenatidine, a natural alkaloid, is a specific JAK inhibitor. Dehydrocrenatidine inhibits voltage-gated sodium channels and ameliorates mechanic allodia in a rat model of neuropathic pain.
JAK   Apoptosis  
Cancer   Neurological, Eye or Ear Disease  
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HY-113066S2 Guanosine 5'-diphosphate-d13 dilithium
Guanosine 5'-diphosphate-d13 (GDP-d13) dilithium is deuterium labeled Guanosine 5'-diphosphate (HY-113066). Guanosine 5'-diphosphate (GDP) is a nucleoside diphosphate that activates adenosine 5'-triphosphate-sensitive K+ channel. Guanosine 5'-diphosphate is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Guanosine 5'-diphosphate can be used in the research of inflammation, such as anemia of inflammation (AI).
Isotope-Labeled Compounds   Endogenous Metabolite   Potassium Channel  
Inflammation or Immune System Disease  
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HY-N3806 Enniatin B
Enniatin B is a Fusarium mycotoxin that acts as an ionophore to form cation-selective membrane channels, disrupt ion homeostasis and mitochondrial function, inhibit cell proliferation, and induce apoptosis, while modulating ERK, p38 MAPK, and STAT3 signaling pathways. Enniatin B is used in research on atherosclerosis, hypercholesterolemia, cervical cancer, and colon adenocarcinoma.

Source: Fusarium spp.

Apoptosis   ERK   p38 MAPK   STAT  
Cervical Cancer   Atherosclerosis and Inflammation   Hypercholesterolemia  
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HY-70057S1 Safinamide-d4-1
Safinamide-d4-1 is deuterium labeled Safinamide. Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 μM) over MAO-A (IC50=580 μM). Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8?μM) than at resting (IC50=262?μM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al.
Isotope-Labeled Compounds   Monoamine Oxidase  
Neurological, Eye or Ear Disease  
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HY-12515AS Nicardipine-d3 hydrochloride
Nicardipine-d3 hydrochloride (YC-93 D3) is the deuterium labeled Nicardipine hydrochloride. Nicardipine hydrochloride is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine hydrochloride acts as an agent for chronic stable angina and for controlling blood pressure.
Calcium Channel  
Neurological, Eye or Ear Disease  
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HY-W040263 TAPS sodium
TAPS sodium is a biological buffer that protects the structural integrity of lysozyme bacteria and prevents them from thermal denaturation at high temperatures. A pKa of 8.1 for TAPS results in half-maximal connexin channel activity.
Biochemical Assay Reagents  
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HY-P2785 Phrixotoxin-1
Phrixotoxin 1, from the venom of the theraphosid spider Phrixotrichus auratus, is a specific peptide inhibitor of Kv4 potassium channel.
Potassium Channel  
Neurological, Eye or Ear Disease  
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HY-N3741 Didrovaltrate
Didrovaltrate (Didrovaltratum) is an L-type calcium channel blocker, ROS scavenger, autophagy enhancer, and lipid accumulation inhibitor. Didrovaltrate blocks L-type calcium currents in a concentration-dependent manner, shifts the current-voltage curve upward, modulates steady-state inactivation kinetics, and inhibits the nuclear translocation of glucocorticoid receptors. Didrovaltrate reduces ROS levels, downregulates the expression of muscle atrophy-related genes, enhances autophagy via lipophagy, and decreases Oleic acid-induced lipid accumulation. Didrovaltrate exhibits cytotoxic activity against cancer cells. Didrovaltrate can be used in research related to skeletal muscle atrophy, non-alcoholic fatty liver disease, breast cancer, lung cancer, gastric cancer, and prostate cancer.
Calcium Channel   Reactive Oxygen Species (ROS)   Autophagy  
Lung Cancer   Breast Cancer   Prostate Cancer   Gastric Cancer   Digestive System Inflammation  
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HY-B0317AS Amlodipine-d4 maleate
Amlodipine-d4 (maleate) is the deuterium labeled Amlodipine maleate. Amlodipine maleate is a dihydropyridine calcium channel blocker, acts as an orally active antianginal agent. Amlodipine maleate blocks the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine maleate can be used for the research of high blood pressure and cancer.
Isotope-Labeled Compounds   Calcium Channel  
Cancer   Blood or Cardio-cerebrovascular Disease  
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HY-N8404 Chlorahololide C
Chlorahololide C, a lindenane sesquiterpenoid dimer, is isolated from Chloranthus holostegius. Chlorahololide C is a potent and selective potassium channel blocker, with an IC50 of 3.6 μM.
Potassium Channel  
Inflammation or Immune System Disease  
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HY-D0143R Quinine (Standard)
Quinine (Standard) is the analytical standard of Quinine (HY-D0143). This product is intended for research and analytical applications. Quinineis an orally active alkaloid extracted from cinchona bark, possessing various biological activities including antimalarial, antidengue virus (DENV), and anticancer properties. Quinine is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100 mV with an IC50 of 169 μM.
Dengue Virus   Flavivirus   Reference Standards   Parasite   Potassium Channel  
Infection  
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HY-B0545S Probenecid-d14
Probenecid-d14 is the deuterium labeled Probenecid. Probenecid is a potent and selective agonist of transient receptor potential vanilloid 2 (TRPV2) channels. Probenecid also inhibits pannexin 1 channels.
Isotope-Labeled Compounds   TRP Channel   Bacterial   HIV  
Metabolic or Endocrine Disease  
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HY-113066S Guanosine 5'-diphosphate-15N5 dilithium
Guanosine 5'-diphosphate-15N5 (GDP-15N5) dilithium is 15N labeled Guanosine 5'-diphosphate (HY-113066). Guanosine 5'-diphosphate (GDP) is a nucleoside diphosphate that activates adenosine 5'-triphosphate-sensitive K+ channel. Guanosine 5'-diphosphate is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Guanosine 5'-diphosphate can be used in the research of inflammation, such as anemia of inflammation (AI).
Isotope-Labeled Compounds   Endogenous Metabolite   Potassium Channel  
Inflammation or Immune System Disease  
/
HY-B1221S1 Flufenamic acid-13C6
Flufenamic acid-13C6 is the 13C6 labeled Flufenamic acid. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca2+ channels, modulating non-selective cation channels (NSC), activating K+ channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
Isotope-Labeled Compounds   COX   AMPK   Potassium Channel   Chloride Channel   Calcium Channel   Parasite  
Inflammation or Immune System Disease  
/
HY-113066S1 Guanosine 5'-diphosphate-13C10 dilithium
Guanosine 5'-diphosphate-13C10 (GDP-13C10) dilithium is 13C-labeled Guanosine 5'-diphosphate (HY-113066). Guanosine 5'-diphosphate (GDP) is a nucleoside diphosphate that activates adenosine 5'-triphosphate-sensitive K+ channel. Guanosine 5'-diphosphate is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Guanosine 5'-diphosphate can be used in the research of inflammation, such as anemia of inflammation (AI).
Isotope-Labeled Compounds   Endogenous Metabolite   Potassium Channel  
Inflammation or Immune System Disease  
/
HY-B0317S1 Amlodipine-d4
Amlodipine-d4 is a deuterium labeled Amlodipine (HY-B0317). Amlodipine, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer.
Isotope-Labeled Compounds   Calcium Channel  
Cancer  
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HY-D1543 Pyronin B
Pyronin B is an organic cationic dye used for the staining of bacteria, mycobacteria and ribonucleic acids. Pyronin B is also used as a small hydrophobic (SH) protein channel inhibitor.
DNA Stain  
Infection  
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HY-P5182A HsTX1 TFA
HsTX1 (TFA) toxin, from the scorpion Heterometrus spinnifer, is a 34-residue, C-terminally amidated peptide cross-linked by four disulfide bridges. HsTX1 (TFA) is an the inhibitor of potassium channel, with IC50 for Kv1.3 of 12 pM and inhibits TEM cell activation and attenuates inflammation in autoimmunity.
Potassium Channel  
Inflammation or Immune System Disease  
/
HY-P1218B Phrixotoxin 3-NH2 TFA
Phrixotoxin 3-NH2 TFA is a derivative of Phrixotoxin 3 TFA (HY-P1218A). Phrixotoxin 3 TFA is a potent blocker of voltage-gated sodium channels, with IC50s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and NaV1.5, respectively. Phrixotoxin 3 TFA modulates voltage-gated sodium channels with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current.
Sodium Channel  
Neurological, Eye or Ear Disease  
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HY-W357818 Glycinexylidide
Glycinexylidide (GX) is the active metabolite of Lidocaine. Lidocaine is a local agent that can suppress or relieve pain, that inhibits sodium channels involving complex voltage and dependence. Lidocaine also reduces the growth, migration and invasion of gastric cancer cells. Glycinexylidide has research potential for use in anesthesia, cancer, and cardiovascular disease.
Sodium Channel   NF-κB   MEK   ERK   Drug Metabolite  
Breast Cancer   Colorectal Cancer   Prostate Cancer   Gastric Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Ovarian Cancer   Depression   Pain   Digestive System Inflammation   Obesity   Rheumatoid Arthritis  
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HY-P5159A Crotamine TFA
Crotamine TFA is a Na+ channel modulator. Crotamine is a 42 amino acid toxin cross-linked by three disulfide bridges. Crotamine has analgesic activity. Crotamine also interacts with lipid membranes and shows myonecrotic activity. Crotamine can be isolated from Crotalus durissus terrificus venom.
Sodium Channel  
Inflammation or Immune System Disease  
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HY-N3320 Marmin
Marmin is a histamine receptor inhibitor and tracheal smooth muscle relaxant. Marmin antagonizes histamine- and methacholine-induced contraction of tracheal smooth muscle. Marmin inhibits histamine release from mast cells, and also blocks extracellular calcium influx via voltage-dependent calcium channels as well as calcium release from intracellular calcium stores, thereby effectively inhibiting calcium-mediated smooth muscle contraction. Marmin slightly enhances the relaxant effect of isoprenaline, and induces epithelial-dependent tracheal smooth muscle relaxation independent of nitric oxide, cGMP or β2-adrenergic pathways through the release of prostaglandin E2.
5-HT Receptor   Histamine Receptor  
Neurological, Eye or Ear Disease  
/
HY-B0407AS Chlorpromazine-d6 hydrochloride
Chlorpromazine-d6 (hydrochloride) is the deuterium labeled Chlorpromazine. Chlorpromazine is an inhibitor of dopamine receptor, 5-HT receptor, potassium channel, sodium channel.
Dopamine Receptor   5-HT Receptor   Sodium Channel   Potassium Channel  
Cancer   Neurological, Eye or Ear Disease  
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HY-B0341S Nicorandil-d4
Nicorandil-d4 (SG-75-d4) is the deuterium labeled Nicorandil. Nicorandil (SG-75) is a potent potassium channel activator and targets vascular nucleoside diphosphate-dependent K+ channels and cardiac ATP-sensitive K+ channels (KATP). Nicorandil is a nicotinamide ester with vasodilatory and cardioprotective effects and has the potential for angina and forischemic heart diseases.
Isotope-Labeled Compounds   Potassium Channel  
Blood or Cardio-cerebrovascular Disease  
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HY-100545R BAPTA-AM (Standard)
BAPTA-AM (Standard) is the analytical standard of BAPTA-AM. This product is intended for research and analytical applications. BAPTA-AM is a well-known membrane permeable Ca2+ chelator. BAPTA-AM inhibits hERG channels, hKv1.3 and hKv1.5 channels in HEK 293 cells with IC50s of 1.3 μM, 1.45 μM and 1.23 μM, respectively.
Reference Standards   Potassium Channel  
Blood or Cardio-cerebrovascular Disease  
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HY-N1847 3'-Methoxydaidzein
3'-Methoxydaidzein is a isoflavone and a Sodium Channel inhibitor. 3'-Methoxydaidzein inhibits subtypes NaV1.7, NaV1.8 and NaV1.3 with IC50 of 181 nM, 397 nM, and 505 nM, respectively. 3'-Methoxydaidzein exerts analgesic activity by inhibiting voltage-gated sodium channels.
Sodium Channel  
Neurological, Eye or Ear Disease  
/
HY-113037CS Farnesyl pyrophosphate-d2 triammonium
Farnesyl pyrophosphate-d2 (Farnesyl diphosphate-d2) triammonium is a deuterium labeled Farnesyl pyrophosphate triammonium (HY-113037C). Farnesyl pyrophosphate ammonium is a metabolic intermediate in the mevalonate (MVA) pathway. It is a TRP channel (TRPM2) agonist that triggers Ca2+ influx and cell death. Farnesyl pyrophosphate ammonium is a key branch substrate for cholesterol synthesis, ubiquinone synthesis, protein farnesylation, and geranylgeranyl pyrophosphate (GGPP) synthesis. Farnesyl pyrophosphate ammonium is used in research on cerebral ischemia, neurodegenerative diseases, pancreatic cancer, inflammation, and autoimmune diseases.
Isotope-Labeled Compounds   TRP Channel   Endogenous Metabolite   Calcium Channel  
Cancer   Neurological, Eye or Ear Disease   Inflammation or Immune System Disease  
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HY-B0448S Phenytoin-d10
Phenytoin-d10 is the deuterium labeled Phenytoin. Phenytoin (5,5-Diphenylhydantoin) is a potent Voltage-gated Na+ channels (VGSCs) blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice.
Isotope-Labeled Compounds   Sodium Channel   Virus Protease  
Cancer   Neurological, Eye or Ear Disease  
/
HY-P3055A Dendrotoxin-I TFA
Dendrotoxin-I (DTX-I) TFA is a potent K+ channel blocker with IC50s of 0.13-50 nM for voltage-gated potassium channel subunits KV1.1, KV1.2 and KV1.6. Dendrotoxin-I TFA, a neurotoxin, has the potential for cancer research.
Potassium Channel  
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HY-101238R Agmatine sulfate (Standard)
Agmatine (sulfate) (Standard) is the analytical standard of Agmatine (sulfate). This product is intended for research and analytical applications. Agmatine sulfate exerts modulatory action at multiple molecular targets, such as neurotransmitter systems, ion channels and nitric oxide synthesis. It is an endogenous agonist at imidazoline receptor and a NO synthase inhibitor.
Reference Standards   Imidazoline Receptor   NO Synthase   Endogenous Metabolite  
Cancer   Neurological, Eye or Ear Disease  
/
HY-129763 Di-4-ANEPPS
Di-4-ANEPPS is a voltage-sensitive dye that acts on voltage-gated ion channels (such as sodium channels) and inhibits sodium current, significantly reducing sodium current density, although specific values like IC50 remain unclear. It mainly binds to the voltage-sensitive regions on the cell membrane, changing its fluorescence properties to reflect membrane potential changes and thus affecting the function of ion channels to exert its activity. This substance can be used in cardiovascular research, such as the electrophysiology of cardiomyocytes, myocardial ischemia, and the effects of drugs on cardiomyocytes. It is of great value in evaluating drug cardiotoxicity and exploring the mechanisms of arrhythmias.
Fluorescent Dye  
Blood or Cardio-cerebrovascular Disease  
/
HY-Y1267D Magnesium sulfate, for cell culture
Magnesium sulfate, for cell culture is a bioreagent. Magnesium sulfate is a calcium antagonist and a potent L-type calcium channel inhibitor, as well as a tocolytic. Magnesium sulfate has anti-inflammatory, anticonvulsant, vasodilatory, and neuroprotective effects. Magnesium sulfate can be used in the research of diseases such as preeclampsia/eclampsia.
Environmental Pollutants   Interleukin Related   Phospholipase   COX   Calcium Channel   Biochemical Assay Reagents   NO Synthase   NF-κB  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease   Blood or Cardio-cerebrovascular Disease  
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HY-W094475C Magnesium sulfate heptahydrate, for cell culture
Magnesium sulfate heptahydrate, for cell culture (Epsom salts, for cell culture) is a hydrate of magnesium sulfate (HY-Y1267) suitable for cell culture applications. Magnesium sulfate is a calcium antagonist and a potent L-type calcium channel inhibitor, as well as a tocolytic. Magnesium sulfate has anti-inflammatory, anticonvulsant, vasodilatory, and neuroprotective effects. Magnesium sulfate can be used in the research of diseases such as preeclampsia/eclampsia.
Biochemical Assay Reagents   NO Synthase   NF-κB   Interleukin Related   Phospholipase   COX   Calcium Channel  
Inflammation or Immune System Disease   Traumatic Brain Injury   Arrhythmias  
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HY-D0877 TAPS
TAPS is an aminosulfonate-based lysozyme stabilizer and connexin channel inhibitor. TAPS maintains the native structure of lysozyme in aqueous solution at pH 7.0 and significantly protects it from heat-induced denaturation. TAPS directly inhibits the activity of heteromeric connexin 32/connexin 26 channels (Cx32/Cx26) via its protonated form, and this inhibitory effect is dependent on the presence of connexin 26. TAPS reduces connexin channel-mediated solute exchange in a recombinant liposome system, resulting in a decreased degree of liposome density shift in transport-specific separation assays. TAPS is a critical compound for investigating the structure and function of connexin channels.
Biochemical Assay Reagents   Connexin  
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HY-W002179 4-Iodobenzaldehyde
4-Iodobenzaldehyde is an aromatic halobenzaldehyde derivative and synthetic intermediate. 4-Iodobenzaldehyde is used for the synthesis of various bioactive molecules such as chalcones, heterocycles, receptor antagonists and channel blockers.
Biochemical Assay Reagents   GABA Receptor  
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HY-126752 Ophthalmic acid
Ophthalmic acid is a ubiquitous metabolite and glutathione modulator, with a Ki of 0.95 mM for glyoxalase I. Ophthalmic acid competitively inhibits glyoxalase I, glutathione S-transferase, glutaredoxin, glutamate-cysteine ligase, protein disulfide reductase (glutathione), as well as non-selective cation channels. Ophthalmic acid is applicable in diabetes-related research.

Source: animal kingdom

Reactive Oxygen Species (ROS)  
Glucose Metabolism  
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HY-107754 Cesium chloride
Cesium chloride is a blocker of potassium channel. Cesium chloride prevents the decrease of Na+ transport produced by Alloxan. Cesium chloride has induced cardiac arrhythmias, including torsade de pointes in animal models.
Potassium Channel  
Cardiovascular Disease   Alzheimer's Disease  
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HY-KD1116 R-PE Rapid Labeling Kit
R-PE (R for phycoerythrin) is the brightest and most commonly used orange-red fluorescent protein probe in flow cytometry and immunofluorescence; it is particularly suitable for detecting low-expressing antigens. Excitation wavelengths: 488 nm (most common) and 561 nm; emission wavelength: 575 nm; flow cytometry channels: PE / 585/40 channels.

Protein Biology Labeling Kit

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Keywords

ion channel drug discovery | ion channel targets | voltage-gated sodium channels | TRP channels | potassium channels | calcium channels | automated electrophysiology | channel modulators