Catalog No.
Product Name
Application
Product Information
Citations
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Antiarrhythmic Agent
Nifekalant is a class III antiarrhythmic agent that functions as a blocker of IKr potassium channels, exhibiting an IC50 value of 10 μM. This compound is primarily utilized in research focused on refractory ventricular tachyarrhythmias, providing valuable insights into cardiac rhythm management. Its ability to modulate potassium channel activity makes it an essential tool for studying arrhythmic conditions and potential therapeutic interventions. -
Potassium Channel Activator
Phe-Met-Arg-Phe, amide is a potent potassium channel activator that reliably elicits K+ current activation in peptidergic caudodorsal neurons, with an effective dose (ED50) of 23 nM. This compound is critical for studies involving ion channel modulation and neuronal signaling, making it an essential tool in neurobiology research and pharmacological investigations. -
Potassium Channel Activator
KRN4884 is a potassium channel activator that stimulates KATP channels in the presence of intracellular ATP at a concentration of 1 mM. It enhances channel activity in a concentration-dependent manner, with an EC50 value of 0.55 μM. This compound is useful for researchers investigating the physiological roles of KATP channels and their implications in cellular signaling and metabolic regulation. -
Potassium Channel Inhibitor
CS476 is a potent inhibitor of potassium channels, exhibiting significant hypoglycemic activity. This compound may facilitate research into the modulation of glucose homeostasis and has potential applications in the study of diabetes-related pathways. Its ability to influence potassium channel activity makes it a valuable tool for investigating various cellular processes linked to metabolic regulation. -
Potassium Channel Activator
Potassium Channel Activator 1 is a selective potassium channel activator that facilitates the opening of potassium channels, contributing to membrane potential regulation. This compound exhibits significant biological activity that may influence cellular excitability and neurotransmitter release. It is primarily utilized in research focused on dopaminergic system disorders, providing insights into potential therapeutic strategies for neurological and psychiatric conditions. -
Potassium Channel
U89232 is a selective opener of the ATP-sensitive potassium (KATP) channels. This compound primarily acts on cardiac tissues, promoting vasodilation and potentially offering protective effects against ischemic conditions. It is valuable for research into cardiovascular pharmacology and the modulation of KATP channels in various therapeutic contexts. -
Potassium-Competitive Acid Blocker
Vonoprazan Fumarate is a potent potassium-competitive acid blocker (P-CAB) that exerts its effect by inhibiting H+,K+-ATPase activity, demonstrating an IC50 of 19 nM at pH 6.5 in porcine gastric microsomes. This compound exhibits significant antisecretory activity, making it valuable for investigating acid-related disorders. Research applications include studies related to gastroesophageal reflux disease and peptic ulcer disease, where it may provide insights into therapeutic mechanisms. -
Proton Pump/Potassium-competitive Acid Inhibitor
Abeprazan hydrochloride is a potassium-competitive acid inhibitor that selectively targets H+, K+-ATPase, providing a mechanism of action distinct from traditional proton pump inhibitors. By reversibly binding in a potassium-competitive manner, Abeprazan hydrochloride effectively reduces gastric acid secretion without requiring acid activation. This compound is being investigated for its therapeutic potential in treating various acid-related gastrointestinal disorders. -
Proton Pump/Potassium-competitive Acid Inhibitor
Abeprazan is a potassium-competitive acid inhibitor primarily targeting the H+, K+-ATPase enzyme. By reversibly binding to this enzyme through potassium-competitive ionic interactions, it effectively reduces gastric acid secretion without the need for acid activation. Abeprazan is being developed as a potential alternative to traditional proton pump inhibitors for the management of acid-related disorders, providing a novel approach to acid control in clinical applications. -
Potassium Channel Inhibitor
RY785 is a potent and selective inhibitor of voltage-gated potassium channels, specifically targeting KV2.2 with an IC50 of 0.05 μM. This compound exhibits notable analgesic activity, making it valuable for research into pain management and related therapeutic applications. Its specificity towards KV2 channels allows for exploration of their role in various physiological and pathological processes. -
Antiarrhythmic Agent
Encainide is an antiarrhythmic agent classified as a class IC antiarrhythmic. It functions by blocking voltage-dependent potassium channels, thus modulating cardiac excitability. This compound shows promise in research focused on life-threatening ventricular arrhythmias, symptomatic ventricular arrhythmias, and supraventricular arrhythmias. Its role in these conditions makes it valuable for studies aimed at understanding and treating various cardiac arrhythmias. -
σ Receptor Agonist
threo-Ifenprodil hemitartrate is a sigma (σ) receptor agonist, exhibiting Kis of 59.1 nM and 2 nM for σ1 and σ2 receptors, respectively. This compound also acts as a NR2B subunit-selective NMDA receptor antagonist, with an IC50 of 0.22 μM, and demonstrates inhibition of the hERG potassium channel with an IC50 of 88 nM, indicating potential antiarrhythmic activity. threo-Ifenprodil hemitartrate serves as a valuable tool in neuropharmacology and cardiovascular research. -
KATP Opener
Iptakalim hydrochloride is a selective ATP-sensitive potassium channel (KATP) opener that exhibits significant lipophilicity. In addition to its primary mechanism, it also acts as an antagonist of α4β2-containing nicotinic acetylcholine receptors (nAChRs). This dual activity positions Iptakalim hydrochloride as a valuable tool for research in cardiovascular physiology and neuropharmacology, providing insights into potassium channel regulation and cholinergic signaling. -
P-gp Inhibitor/Potassium Channel Activator
GPV0057 is a selective and potent inhibitor of P-glycoprotein (P-gp) and a specific activator of the potassium channel Kir2.1. By competitively binding to the substrate-binding site of P-gp, GPV0057 inhibits ATP-dependent drug efflux, effectively reversing multidrug resistance in tumor cells. Additionally, it stabilizes the open state of Kir2.1, facilitating potassium ion influx. This compound holds potential for research in tumors characterized by high P-gp expression and in conditions such as heart failure and Andersen-Tawil Syndrome that involve Kir2.1 deficiency. -
GABAA Receptor Antagonist
Bicuculline (methochloride) is a selective antagonist of the GABAA receptor, exhibiting an IC50 value of 3 μM. This compound is known to induce clonic-tonic convulsions in mammals and is also capable of blocking Ca2+-activated potassium channels. Bicuculline (methochloride) is utilized in research focused on epilepsy and related psychiatric disorders, providing valuable insights into neuronal excitability and inhibitory transmission. -
Potassium Channel Opener
Flupirtine is a non-opioid analgesic that acts primarily as a potassium channel opener, specifically targeting Kv7 channels. This compound exhibits notable neuroprotective properties by stabilizing blood-brain barrier integrity, reducing oxidative stress, and counteracting focal cerebral ischemia. Flupirtine is utilized in research related to pain management, Alzheimer's disease, multiple sclerosis, and neuroprotection due to its ability to lessen neuronal excitotoxicity and maintain resting membrane potential without exhibiting antipyretic or antiphlogistic effects. -
Potassium Channel Opener
Flupirtine hydrochloride is a potassium channel opener (Kv7 activator) recognized for its analgesic and neuroprotective properties. This compound acts as a non-opioid analgesic while also antagonizing NMDA receptors and activating GABA receptors. Flupirtine hydrochloride enhances neuronal stability by reducing oxidative stress and calcium influx, thereby protecting neurons from excitotoxicity and ischemia. It is applicable in research focused on conditions such as focal cerebral ischemia, pain management, Alzheimer’s disease, and multiple sclerosis. -
GABAA Receptor Antagonist
Bicuculline methobromide is a selective antagonist of the GABAA receptor, exhibiting an IC50 value of 3 μM. This compound is known to induce clonic-tonic convulsions in mammalian models, making it a valuable tool for investigating epilepsy and associated neurological disorders. Additionally, bicuculline methobromide functions as a blocker of Ca2+-activated potassium channels, further expanding its utility in pharmacological research focused on ion channel dynamics and excitability in neuronal systems. -
Stable Isotope
Flupirtine-d4 hydrochloride is a deuterium-labeled variant of Flupirtine hydrochloride, a non-opioid analgesic that crosses the blood-brain barrier. This compound functions primarily as a neuronal potassium channel opener (Kv7 activator) and exhibits properties as an NMDA receptor antagonist and GABA receptor activator. It is utilized in research focused on pain management, neuroprotection, and conditions such as Alzheimer’s disease and multiple sclerosis, offering insights into pathways of ischemic neuron death, oxidative stress modulation, and the maintenance of blood-brain barrier integrity. Flupirtine-d4 hydrochloride serves as a valuable tool for studying the underlying mechanisms and therapeutic approaches for neurological disorders. -
Kv1.3/Kv1.4 Blocker
CP 339818 hydrochloride is a selective blocker of Kv1.3 and Kv1.4 ion channels, with an IC50 of 200 nM for Kv1.3. This compound also inhibits HCN channels, displaying IC50 values of 18.9 μM and 43.4 μM for HCN1 and HCN4, respectively, while having minimal effect on other Kv channels such as Kv1.1 and Kv1.2. By selectively targeting Kv1.3, CP 339818 hydrochloride attenuates the activation of human T cells, making it a valuable tool for investigating the physiological roles of HCN and Kv channels in cellular processes. -
HCN/Potassium Channels Blocker
KIO-301 chloride is a photoswitch compound that selectively blocks hyperpolarisation-activated cyclic nucleotide-gated (HCN) channels and voltage-gated potassium channels upon exposure to visible light. This compound can be employed in research to investigate the role of these ion channels in cellular excitability and signaling pathways. Its unique mechanism offers insights into ion channel modulation and potential therapeutic applications in neurobiology and cardiac research. -
Kv1.3/Kv1.4 Channel Blocker
CP-339818 is a selective blocker of the Kv1.3 and Kv1.4 potassium channels, exhibiting an IC50 of 200 nM for Kv1.3. This compound also inhibits HCN channels, with IC50 values of 18.9 μM and 43.4 μM for HCN1 and HCN4, respectively, while demonstrating minimal effects on other Kv channels, such as Kv1.1 and Kv1.2. CP-339818 is valuable for investigating the role of Kv1.3 in T cell activation and the physiological functions of HCN and Kv channels in cellular contexts. -
NMDA Receptor Inhibitor
Bupivacaine is an NMDA receptor inhibitor that modulates neuronal excitability by blocking sodium, L-calcium, and potassium channels. It exhibits potent inhibition of SCN5A channels, with an IC50 of 69.5 μM. This compound is primarily utilized in research focused on chronic pain mechanisms and therapeutic interventions. -
Potassium Supplement
Potassium chloride, AR, 99.5% serves as an essential potassium supplement, playing a critical role in various biochemical applications. This compound is particularly valuable in research related to hyperkalemia, where it aids in studying potassium ion regulation in biological systems. Additionally, it functions as a potassium source in agronomy, contributing to plant nutrition and growth. -
Potassium Channel Blocker
Azimilide dihydrochloride is a class III antiarrhythmic agent that functions primarily as a potassium channel blocker, targeting both IKs and IKr channels with IC50 values of 2.6 μM and 1 μM, respectively. Additionally, it inhibits the HERG channel at frequencies of 0.1 and 1 Hz, with IC50 values of 1.4 μM and 5.2 μM. Azimilide dihydrochloride also suppresses L-type calcium current and sodium current, with IC50 values of 17.8 μM and 19 μM, respectively. This compound is valuable for researching conditions such as atrial fibrillation and ventricular fibrillation. -
NMDA Receptor Inhibitor
Bupivacaine-d9 is a deuterium-labeled analog of Bupivacaine, primarily targeting NMDA receptors. This compound exhibits inhibitory effects on sodium, L-calcium, and potassium channels, with a notable potency against SCN5A channels, characterized by an IC50 value of 69.5 μM. Bupivacaine-d9 is utilized in research related to chronic pain mechanisms and the modulation of excitatory neurotransmission, offering valuable insights into therapeutic applications in pain management. -
Potassium/Sodium Channel Inhibitor
Huwentoxin I is a peptide toxin that specifically inhibits voltage-gated sodium channels and N-type calcium channels. This compound has demonstrated significant inhibitory effects on sodium channels in both rat hippocampus and cockroach dorsal unpaired median (DUM) neurons, with IC50 values of 66.1 nM and 4.80 nM, respectively. Huwentoxin I is valuable for studies focused on neuronal excitability and channelopathy-related research applications. -
NMDA Receptor Inhibitor
Bupivacaine hydrochloride monohydrate is an NMDA receptor inhibitor that effectively modulates excitatory neurotransmission. It possesses the ability to block sodium, L-calcium, and potassium channels, with a notable potency in inhibiting SCN5A channels, exhibiting an IC50 value of 69.5 μM. This compound is primarily utilized in research focused on chronic pain mechanisms and the development of analgesic strategies. -
Antiarrhythmic Agent
AZD-1305 is an antiarrhythmic agent that selectively blocks sodium and potassium channels in the atria. This compound significantly prolongs action potential duration and reduces excitability, leading to atrial-selective effective refractory period (ERP) prolongation and acute termination of atrial fibrillation. AZD-1305 is a valuable tool for research related to atrial fibrillation and its underlying mechanisms. -
Stable Isotope
Ranolazine-d5 is a deuterium-labeled analogue of Ranolazine, which primarily targets the late phase of inward sodium current (INa) and potassium channels (IKr), exhibiting IC50 values of 6 μM and 12 μM, respectively. This compound functions as an anti-anginal agent by alleviating myocardial ischemia without influencing heart rate or blood pressure. Additionally, Ranolazine-d5 serves as a partial inhibitor of fatty acid oxidation (FAO), making it valuable for research in cardiovascular pharmacology and metabolic studies. -
N-type Calcium Channel Antagonist
Huwentoxin XVI is a selective antagonist of N-type calcium channels, demonstrating a potent inhibitory effect with an IC50 of approximately 60 nM. Derived from the Chinese tarantula Ornithoctonus huwena, it serves as an analgesic and exhibits no activity against voltage-gated T-type calcium channels, potassium channels, or sodium channels. This specificity makes Huwentoxin XVI valuable in research aimed at understanding pain mechanisms and the role of calcium channels in various physiological processes. -
Potassium/Calcium/Sodium Channel Blocker
NIP-142 is a benzopyran derivative that functions as a potassium, calcium, and sodium channel blocker. It selectively inhibits potassium channels abundant in atrial muscle, leading to an increase in the effective refractory period (ERP) and action potential duration (APD) in the atrium, while sparing ventricular repolarization. Additionally, NIP-142 dampens L-type and T-type calcium channels and sodium channels, enhancing its anti-arrhythmic properties. This compound is particularly useful in the study of atrial fibrillation and related arrhythmias. -
Hypoglycemic Agent
AZ-DF 265 is a hypoglycemic agent that promotes insulin secretion through the inhibition of ATP-sensitive potassium channels and the activation of voltage-dependent calcium channels. This results in the influx of calcium ions, which is crucial for insulin release. AZ-DF 265 is applicable in diabetes research, providing insights into glucose metabolism and insulin regulation mechanisms. -
Vasodilating Agent
HUP30 is a potent vasodilating agent that primarily stimulates soluble guanylyl cyclase. Its mechanism of action includes the activation of potassium channels and inhibition of extracellular calcium influx. This compound is valuable for research applications focused on vascular biology, cardiovascular diseases, and the modulation of blood pressure. -
Cav1.2 Blocker
Calciseptine is a natural polypeptide toxin derived from the venom of the black mamba snake (Dendroaspis p. polylepis). It serves as a selective blocker of the L-type Cav1.2 calcium channel, showcasing an IC50 value of 92 nM, while sparing other calcium channels such as Cav3.1 and Cav2.2, as well as sodium and potassium channels. Calciseptine induces negative inotropic and relaxant effects in murine models without impacting heart rate or sinoatrial node action potentials. This compound is valuable for investigations into cardiovascular diseases. -
Potassium/Calcium Channel Blocker
SB-237376 free base is a potent inhibitor of potassium and calcium channels, primarily targeting the rapidly activating delayed rectifier potassium current I(Kr) with an IC50 of 0.42 μM. Additionally, at elevated concentrations, it effectively blocks the L-type calcium current I(Ca,L). In studies utilizing rabbit ventricular models, SB-237376 free base has been shown to induce early afterdepolarizations (EADs) at a concentration of 3 µM. This compound presents a lower proarrhythmic risk compared to other known I(Kr) inhibitors, making it valuable for investigations into arrhythmia-related conditions. -
Endogenous Metabolite
ISQ-1 hydrochloride is an isoquinolinone compound that functions as an inhibitor of the IKur potassium channel. It demonstrates potential to influence cardiac electrophysiology by modulating arrhythmic activity in atrial tissues. This reagent is primarily utilized in research focused on cardiac rhythm disorders and electrophysiological studies of heart functions. -
Starting CompoundsFor The Synthesis of KV7.2/3 Openers
2,6-Dichloro-3-nitropyridine is a key starting compound in the synthesis of sulfide analogs of Flupirtine, which function as KV7.2/3 channel openers. This compound exhibits potential biological activity relevant to pain research, making it a valuable reagent for studies focused on the modulation of neuronal excitability and analgesic mechanisms. Its utility in the development of KV7.2/3 activators positions it as an important tool in therapeutic research. -
Biochemical Assay Reagents
6-FAM-AEEAc-Stichodactyla helianthus Neurotoxin (ShK) is a fluorescent-labeled polypeptide that primarily targets voltage-gated potassium channels. This reagent exhibits potent inhibitory activity on ion channel function, making it valuable for biochemical assays focused on channel pharmacology and neurobiology. Its applications extend to studies investigating ion channel modulation and neurotoxin interactions in cellular models. -
Biochemical Reagent
Glycopyramide is a sulfonylurea compound that primarily targets and inhibits the ATP-sensitive potassium channels in pancreatic beta cells. This inhibition promotes insulin secretion, making it relevant in the study of diabetes and glucose metabolism. It can be utilized in biochemical research to explore mechanisms of insulin release and the regulation of blood glucose levels. -
Anti-malarial Agent
Quinine hydrochloride dihydrate is an anti-malarial agent primarily known for its inhibitory action on potassium channels. It effectively inhibits wild-type mouse Slo3 (KCa5.1) channel currents in response to voltage pulses, exhibiting an IC50 value of 169 μM. This compound is essential for research into malaria treatment and the study of ion channel modulation in various biological contexts. -
K+ Channel Blocker
Dendrotoxin-I (DTX-I) is a potent inhibitor of voltage-gated potassium channels, specifically targeting the KV1.1, KV1.2, and KV1.6 subunits with IC50 values ranging from 0.13 to 50 nM. This neurotoxin exhibits significant biological activity that can influence neuronal excitability and synaptic transmission. Dendrotoxin-I is primarily utilized in research applications related to cancer and neurobiology, providing insights into ion channel function and their roles in disease mechanisms. -
hERG Channel Blocker
Tannic acid is identified as a novel hERG channel blocker, exhibiting an IC50 of 3.4 μM. This compound has significant implications in cardiovascular research, particularly in studying drug-induced long QT syndrome and cardiac arrhythmias. Its capacity to modulate ion channel activity makes it a valuable tool in pharmacological studies focused on cardiac safety and ion channel function. -
TASK-1 Inhibitor
Doxapram hydrochloride hydrate is a TASK-1 inhibitor that enhances respiratory function by stimulating the brain's respiratory centers and peripheral chemoreceptors. This compound effectively increases both the rate and depth of breathing, while demonstrating inhibitory effects on TASK-1, TASK-3, and their heterodimeric channels with EC50 values of 410 nM, 37 μM, and 9 μM, respectively. Additionally, it inhibits Ca²⁺-activated and Ca²⁺-independent potassium currents in type I cells of the carotid body, with IC50 values of approximately 13 μM and 20 μM, respectively. Doxapram hydrochloride hydrate serves as a useful reagent for research on respiratory depression conditions, including post-anesthesia recovery, chronic obstructive pulmonary disease, and apnea of prematurity. -
Potassium Channel Inhibitor
Cloperastine hydrochloride is a potassium channel inhibitor primarily targeting hERG K+ currents. It demonstrates concentration-dependent inhibition, with an IC50 value of 27 nM. This reagent is employed in research applications focused on cardiac ion channel function and drug interactions, providing valuable insights into cardiovascular safety and pharmacology. -
Potassium Channel Inhibitor
Cloperastine fendizoate is a potent inhibitor of the hERG potassium channels, exhibiting concentration-dependent inhibition with an IC50 value of 27 nM. This compound is primarily utilized in research applications focusing on cardiac ion channel function and related arrhythmia studies. Its effects on potassium currents make it valuable for investigating the electrophysiological properties of cardiac tissues and potential therapeutic interventions. -
Potassium Channel Inhibitor
Tetraethylammonium chloride is a non-selective inhibitor of potassium channels, effectively blocking their function. This compound is recognized as a substrate for organic cation transporter 1 (OCTN1), which may be relevant in transport-related studies. Additionally, tetraethylammonium chloride exhibits potential antitumor properties, making it a valuable tool in cancer research and investigations into ion channel dynamics. -
FTO Inhibitor
Meclofenamic acid is a highly selective inhibitor of the fat mass and obesity-associated (FTO) enzyme, which plays a crucial role in the regulation of m(6)A RNA methylation. By competing with FTO for binding to m(6)A-containing nucleic acids, it modulates RNA metabolism and influences cellular processes related to metabolism and obesity. Additionally, Meclofenamic acid exhibits non-selective blockade of gap junctions and inhibits the potassium channels hKv2.1 and hKv1.1, with IC50 values of 56.0 µM and 155.9 µM, respectively. This compound is valuable for research applications focused on obesity, metabolic regulation, and ion channel physiology. -
Vasodilator
SCA-40 is a potent vasodilator targeting bronchial smooth muscle. It induces biphasic relaxation in bronchi exhibiting spontaneous tension, with its relaxation effects remaining unaffected by various potassium channel blockers. This compound is suitable for research applications focused on bronchial conditions and related pathophysiological studies. -
Antipsychotic Agent
Chlorpromazine is an orally active antipsychotic agent that primarily antagonizes D2 dopamine and 5-HT2A serotonin receptors, making it effective in the treatment of schizophrenia and other psychiatric conditions. Additionally, chlorpromazine exhibits anti-cancer properties through mechanisms such as inhibition of tumor proliferation, induction of autophagy, cell cycle arrest at the G2-M phase, and suppression of tumor growth and metastasis. It also blocks hNav1.7 and HERG potassium channels, which has implications for analgesic and cardiac arrhythmia research. Furthermore, chlorpromazine inhibits clathrin-mediated endocytosis, expanding its potential applications in biomedical research.
