Catalog No.
Product Name
Application
Product Information
Citations
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IK blocker
AM-92016 hydrochloride is a specific blocker of rectifier potassium current (IK). -
Iron mobilizer
Guanosine 5'-diphosphate is a nucleoside diphosphate. Guanosine 5'-diphosphate is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulating the interleukin-6 (IL-6)/stat-3 pathway. -
Kv3.1/Kv3.2 modulator
Kv3 modulator 4 is a Kv3.1 (pEC50=5.45) and Kv3.2 modulator extracted from patent WO2018020263A1, Cyclobutyl structure. -
Kv3.1/Kv3.2/Kv3.3 channels modulator
Kv3 modulator 3 (Compound 4) is a selective modulator of Kv3.1 and/or Kv3.2 and/or Kv3.3 channels extracted from patent WO2017098254A1, compound 4, has analgesic activity for use in the prophylaxis o or treatment of pain. -
Kv3 voltage-gated potassium channel modulator
Kv3 modulator 1 is a Kv3 voltage-gated potassium channel modulator extracted from patent WO2018020263A1, Compound X. Kv3 modulator 1 can be used to treat inflammatory pain. -
Potassium channel blocker
Cesium chloride is a potassium channel blocker; inhibits the pacemaker current (If) and the hyperpolarization-activated cationic current (Ih). Prevents activation of caspase-3 and neuronal apoptosis in serum- and potassium-deprived cerebellar granule neurons by inactivating GSK-3β. -
5-HT3 receptor inhibitor
Eucalyptol is a bicyclic monoterpene that has been found in Eucalyptus and other plants. It is an inhibitor of 5-HT3 receptor ,potassium channel, TNF-α and IL-1β. -
Kir6.2/SUR inhibitor
Glimepiride is a potent Kir6.2/SUR inhibitor with IC50 of 3.0 nM, 5.4 nM, and 7.3 nM for SUR1, SUR2A and SUR2B, used in the treatment of type 2 diabetes mellitus. - Hydralazine hydrochloride is a hydrochloride salt of hydralazine (Apresoline) that is a direct-acting smooth muscle relaxant with an IC50 of 1.9 mM.
- Minoxidil (U-10858) is a selective ATP dependent K+ (Kir6) channel activator.
- Nateglinide(Starlix) is an insulin secretagog agent that lowers blood glucose levels by stimulating insulin secretion from the pancreas.
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KCa2.1 channels activator
GW 542573X is an activator of small-conductance Ca2+-activated K+ channels (KCa2). -
Potassium Channel inhibitor
Repaglinide is a potent short-acting insulin secretagogue that acts by closing ATP-sensitive potassium (KATP) channels in the plasma membrane of the pancreatic beta cell. -
Nucleotide Analogue
Uridine 5'-monophosphate disodium salt is a nucleotide analogue that activates mitochondrial ATP-dependent potassium channels, providing cardioprotective effects. This compound facilitates the synthesis of CDP-choline and induces apoptosis in intestinal epithelial cells, supporting gut development and reducing the incidence of diarrhea. It serves as a valuable tool for studies related to cardiac health and gastrointestinal function. -
Calcium Sensitiser
OR-1896 is a potent calcium sensitizer and active metabolite of Levosimendan, primarily targeting phosphodiesterase (PDE) III isoforms. It exhibits significant vasodilatory effects and can activate ATP-sensitive potassium channels, enhancing calcium sensitivity. OR-1896 has been shown to reduce cardiomyocyte apoptosis, alleviate cardiac remodeling, and mitigate myocardial inflammation, making it valuable for research in cardiovascular disease therapies. -
Kv2.1 Inhibitor
Kv2.1-IN-1 is a selective inhibitor of the Kv2.1 potassium channel, demonstrating a potent inhibitory activity with an IC50 of 0.07 μM. It exhibits over 130-fold selectivity against other potassium, sodium, and calcium channels. Kv2.1-IN-1 has been shown to reduce H2O2-induced apoptosis in HEK293 cells and provides significant neuroprotective effects in models of middle cerebral artery occlusion (MCAO) in rats. This compound is useful for research into ischemic stroke and related neurological conditions. -
Potassium Binder
Patiromer is a selective, non-absorbable intestinal potassium binder that targets potassium ions through a reversible exchange with calcium ions. It effectively lowers serum potassium levels while promoting fecal potassium excretion and reducing serum aldosterone levels. Patiromer is utilized in research on hyperkalemia associated with conditions such as chronic kidney disease, diabetes, and heart failure, and is particularly beneficial in studies aimed at enhancing the efficacy of renin-angiotensin-aldosterone system inhibitor (RAASi) therapies. -
Stable Isotope
Hydrochlorothiazid-d2 is the deuterated form of Hydrochlorothiazide, a thiazide diuretic known for its role in inhibiting the transforming growth factor-beta (TGF-β)/Smad signaling pathway. This compound exhibits direct vascular relaxation by activating calcium-activated potassium channels, contributing to its antihypertensive properties. Hydrochlorothiazid-d2 is valuable in research applications involving the study of cardiovascular function, fibrosis reduction, and the overall effects of diuretics on systemic blood pressure regulation. -
Stable Isotope
Hydrochlorothiazid-13C,d2 is a stable isotope-labeled form of Hydrochlorothiazide (HCTZ), a thiazide diuretic that functions by inhibiting the TGF-β/Smad signaling pathway. This compound exhibits direct vascular relaxant effects through the activation of calcium-activated potassium channels. Hydrochlorothiazide is primarily utilized in research to improve cardiac function, reduce fibrosis, and exhibit antihypertensive properties, making it a valuable tool for studies on cardiovascular health and hypertension management. -
Stable Isotope
Hydrochlorothiazide-15N2,13C,d2 is a stable isotope-labeled derivative of hydrochlorothiazide, incorporating 15N and deuterium for enhanced tracking in metabolic studies. As a thiazide diuretic, hydrochlorothiazide inhibits the TGF-β/Smad signaling pathway, which plays a crucial role in cardiovascular remodeling. This compound exhibits direct vascular relaxation by activating calcium-activated potassium channels, thereby improving cardiac function, reducing fibrosis, and delivering antihypertensive effects. It is ideal for research applications focusing on cardiovascular health and the mechanisms of diuretic therapy. -
Kir2.1 Agonist
Tetramisole acts as a selective agonist for the inward rectifier potassium channel Kir2.1, displaying an EC50 of approximately 30 μM. This compound enhances the forward transport of Kir2.1 channels, hyperpolarizing the resting potential and shortening action potential duration, while also inhibiting intracellular calcium overload and PKA signaling. Additionally, Tetramisole exhibits anti-arrhythmic and anti-myocardial remodeling properties. It is valuable in cardiac electrophysiology studies and investigations focused on myocardial ischemia and heart failure. -
Stable Isotope
Tolbutamide-d9 is a deuterated form of Tolbutamide, which primarily targets ATP-sensitive potassium channels. As a first-generation sulfonylurea, it functions as an oral hypoglycemic agent, playing a critical role in glucose regulation. This stable isotope is valuable for metabolic research and isotopic tracing studies, facilitating investigations into pharmacokinetics and the mechanism of action of sulfonylureas. -
Autophagy Inducer
Desethylamiodarone hydrochloride is a significant active metabolite of Amiodarone, primarily functioning as an autophagy inducer. It is produced through the action of CYP3A isoenzymes and plays a critical role in cellular processes affecting autophagy. This compound is utilized in research applications focusing on cardiovascular pharmacology and cellular stress responses, due to its influence on potassium channels and potential therapeutic implications in arrhythmias. -
Stable Isotope
Amiodarone-d4 hydrochloride is a deuterium-labeled derivative of the Class III antiarrhythmic agent, Amiodarone hydrochloride, which primarily targets the human ether-a-go-go-related gene (hERG) potassium channel with an IC50 of approximately 45 nM. This compound influences vital cellular processes, promoting fibroblast proliferation and myofibroblast differentiation through the activation of ERK1/2 and p38 MAPK signaling pathways. Amiodarone-d4 hydrochloride is an essential tool for research into supraventricular and ventricular arrhythmias, providing valuable insights into arrhythmia mechanisms and potential therapeutic strategies. -
Stable Isotope
Amiodarone-d10 hydrochloride is a deuterium-labeled derivative of Amiodarone. This compound acts primarily as an antiarrhythmic agent, exerting its effects through the inhibition of ATP-sensitive potassium channels, with an IC50 value of 19.1 μM. It is utilized in pharmacokinetic studies and research focused on cardiovascular diseases, providing insights into drug metabolism and action mechanisms. -
Stable Isotope
Uridine 5'-monophosphate-13C9,15N2 dilithium is a stable isotope-labeled form of uridine 5'-monophosphate, incorporating both 13C and 15N isotopes. This compound acts as an orally active mitochondrial ATP-dependent potassium channel activator, demonstrating cardioprotective effects. Additionally, uridine 5'-monophosphate promotes the synthesis of CDP-choline and induces apoptosis in intestinal epithelial cells, making it valuable for research in gut development and in studies related to gastrointestinal health. -
Antiarrhythmic Agent
Quinidine sulfate is an antiarrhythmic agent that primarily targets cardiac ion channels, particularly potassium channels. It exhibits potent K+ channel blocking activity with an IC50 of 19.9 μM and has been shown to induce apoptosis in various cell types. Additionally, quinidine sulfate is utilized in malaria research, making it valuable for studies related to both cardiovascular and infectious diseases. -
Antiarrhythmic Agent
Quinidine polygalacturonate is an antiarrhythmic agent that primarily targets potassium channels, exhibiting an IC50 of 19.9 μM. It also functions as a selective inhibitor of cytochrome P450db and has the capability to induce apoptosis. This compound is particularly useful in research focused on cardiac arrhythmias and malaria studies, making it a valuable reagent for pharmacological investigations. -
Vasodilator
KMUP-1 is a xanthine derivative that acts as a vasodilator through the inhibition of phosphodiesterase (PDE) and activation of soluble guanylyl cyclase (sGC). It stimulates the nitric oxide/sGC/cyclic GMP signaling pathway and facilitates the opening of potassium channels. Additionally, KMUP-1 has been shown to reduce ischemia-induced cardiomyocyte apoptosis. This compound is relevant for studies in cardiovascular health and anti-inflammatory research. -
Potassium Channel Inhibitor
DPO-1 is a selective inhibitor of Kv1.5 and Kv1.3 potassium channels (EC50 = 3.1 μM) with notable immunomodulatory and anti-inflammatory properties. It effectively reduces Kv1.3 current density, diminishes Ca2+ influx in calcium-depleted Jurkat cells, and inhibits IL-2 secretion in activated Jurkat cells. Additionally, DPO-1 obstructs uric acid sodium (MSU)-induced NLRP3 inflammasome activation by interfering with Kv1.5-mediated K+ efflux. This reagent is valuable for research into immunological disorders and atrial fibrillation. -
CO Donor
Tricarbonyldichlororuthenium(II) dimer serves as a carbon monoxide (CO) donor, facilitating various biological processes. This compound demonstrates notable anti-inflammatory and antioxidant properties, in addition to its protective effects on gastric mucosa. Furthermore, Tricarbonyldichlororuthenium(II) dimer exhibits CO-independent effects on several potassium channels, highlighting its significance in cellular physiology and potential therapeutic applications. -
Antiarrhythmic Agent
Quinidine gluconic acid is an antiarrhythmic agent primarily targeting potassium channels, exhibiting an IC50 of 19.9 μM. This compound is a potent, orally active inhibitor of cytochrome P450 enzymes and has been shown to induce apoptosis in certain cell types. Quinidine gluconic acid is utilized in research related to cardiac arrhythmias as well as malaria studies, providing valuable insights into these complex biological processes. -
SERT/NET Inhibitor
Amitriptyline is a tricyclic antidepressant that primarily inhibits the serotonin transporter (SERT) and norepinephrine transporter (NET), enhancing synaptic levels of serotonin and norepinephrine. With a Ki value of 3.45 nM for SERT and 13.3 nM for NET, Amitriptyline demonstrates significant antidepressant activity. Additionally, it exhibits agonistic properties at α2A adrenergic and TrkA/TrkB receptors, contributing to its analgesic and neurotrophic effects. Furthermore, Amitriptyline interacts with various receptors, including muscarinic cholinergic and H1 receptors, which may lead to a variety of side effects, while its ability to block sodium channels and hERG potassium channels raises concerns regarding cardiotoxicity. -
K+ channel blocker?€?
E-4031 dihydrochloride is a selective blocker of KV11.1 (hERG) channels; inhibits the rapid delayed-rectifier K+ current (IKr). -
iron mobilizer
Guanosine 5'-diphosphate disodium salt is a nucleoside diphosphate. Guanosine 5'-diphosphate is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulating the interleukin-6 (IL-6)/stat-3 pathway. -
non-narcotic antitussive
Tipepidine hydrochloride, a non-narcotic antitussive, exerts an antidepressant-like effect. -
OPRM1/OPRD1 agonist
ML335 (CYM 51010, CID-23723457) is an agonist for OPRM1(μ-opioid receptor)-OPRD1(δ-opioid receptor) heterodimerization with EC50 of 403 nM demonstrating selectivity over the individual OPRM1 and OPRD1 receptors and the serotonin HT5A receptor with EC50 of 14.9 μM, 1.1 μM, and >40 μM, respectively.
