Catalog No.
Product Name
Application
Product Information
Citations
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Potassium-Competitive Acid Blocker
Vonoprazan hydrochloride is a potassium-competitive acid blocker (P-CAB) that inhibits H+,K+-ATPase activity, exhibiting an IC50 of 19 nM at pH 6.5. Its potent antisecretory effects make it a valuable reagent in research related to acid-related conditions, including gastroesophageal reflux disease and peptic ulcer disease. Vonoprazan hydrochloride is also utilized for studies focusing on the eradication of Helicobacter pylori, contributing to advancements in gastrointestinal therapeutics. -
Potassium Channel Activator
Kaurenoic acid is a diterpene that acts as a potassium channel activator. It exhibits various biological activities, including antibacterial, anti-inflammatory, anticonvulsant, analgesic, and aortic vasodilating effects. This compound is primarily utilized in research related to neuroprotection, cardiovascular health, and the modulation of ion channel activity. -
TREK-1 Channel Blocker
Spadin is a potent TREK-1 channel blocker with an IC50 value of 10 nM. This natural peptide, derived from a propeptide released into the bloodstream, enhances 5-HT neurotransmission in the dorsal raphe nucleus of mice, promoting hippocampal CREB activation and neurogenesis. Spadin is valuable for research applications targeting antidepressant mechanisms and neuroplasticity. -
Stable Isotope
Chlorpromazine-d6 hydrochloride is a deuterated derivative of Chlorpromazine, primarily functioning as a dopamine receptor antagonist. This stable isotope is utilized in biochemical and pharmacological research to explore the interactions and mechanisms of action of antipsychotic agents. Its ability to inhibit serotonin receptors, potassium channels, and sodium channels makes it valuable for studying neuropharmacology and drug metabolism. -
Potassium Channel Inhibitor
Naluzotan hydrochloride is a selective potassium channel inhibitor that primarily functions as an amidosulfonamide 5-HT1A agonist, exhibiting an IC50 of approximately 20 nM and a Ki value of 5.1 nM. This compound demonstrates notable activity in modulating neurotransmitter pathways, making it a valuable tool for research into anxiety and depression treatments. Additionally, naluzotan hydrochloride acts as a weak hERG K+ channel blocker with an IC50 of 3800 nM, highlighting its potential relevance in cardiac safety assessments. -
ASK1 Inhibitor
ASK1-IN-10 is a selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1), exhibiting an IC50 value of less than 200 nM. In addition to its primary mechanism, ASK1-IN-10 exhibits inhibitory activity against hERG potassium channels. This compound serves as a valuable tool for investigating the role of ASK1 in inflammation-related research and its potential therapeutic implications. -
Potassium Channel Opener
Bimakalim is an ATP-sensitive potassium channel opener that induces vasodilation by enhancing potassium ion efflux. This compound has been shown to reduce transmural myeloperoxidase (MPO) activity and mimics ischemic preconditioning effects, leading to decreased infarct size and modulation of adenosine release and neutrophil function. Bimakalim is valuable for research applications focused on cardiovascular physiology and ischemia-reperfusion injury studies. -
hERG Inhibitor
GSK369796 is a selective inhibitor of the hERG potassium ion channel, demonstrating an IC50 value of 7.5 μM. This compound exhibits significant antimalarial activity, making it a valuable tool for research in both cardiac function and malaria therapeutics. Its potential implications in pharmacology and drug development provide a basis for further exploration in ion channel regulation and associated biological pathways. -
Anti-malaria Agent
Quinine hemisulfate hydrate, an alkaloid obtained from the bark of the cinchona tree, functions primarily as an anti-malaria agent. It acts as a potassium channel inhibitor, specifically targeting the Slo3 (KCa5.1) channel, and can effectively inhibit channel currents in wild-type mouse models. Its inhibitory activity is quantified with an IC50 value of 169 μM, making it a valuable compound for research into malaria treatment and the modulation of potassium channels. -
Stable Isotope
Endoxifen-d5 (Z-isomer) is the stable isotope-labeled derivative of the Z-isomer of Endoxifen. This metabolite of Tamoxifen exhibits significant anti-estrogenic activity in breast cancer cells that express the estrogen receptor alpha (ERα), contributing to its therapeutic efficacy in estrogen-sensitive tumors. Additionally, Endoxifen (Z-isomer) demonstrates a concentration-dependent inhibition of the hERG potassium channel, with an IC50 value of 1.6 μM, making it a valuable tool for research into breast cancer treatment and associated cardiotoxic effects. -
Antimalarial Agent
Halofantrine is an antimalarial agent that primarily targets Chloroquine-resistant strains of Plasmodium falciparum. This compound exhibits high lipophilicity and effectively blocks HERG potassium channels, contributing to its pharmacological profile. Halofantrine is utilized in research focused on malaria treatment and the mechanisms of drug resistance in parasitic infections. -
Parasite Inhibitor
Ep vinyl quinidine, an epi-vinyl stereoisomer of Quinidine, serves as a targeted inhibitor of parasitic activity. This compound exhibits significant potential in malaria research, leveraging its capabilities as a selective cytochrome P450db inhibitor. Additionally, it functions as a potassium channel blocker with an IC50 of 19.9 μM, positioning it as a valuable tool for investigating anti-parasitic mechanisms and therapeutic interventions. -
Anti-malarial Agent
Quinine sulfate hydrate (2:1:4) is an orally active alkaloid used primarily as an anti-malarial agent. This compound functions as a potassium channel inhibitor, specifically targeting the WT mouse Slo3 (KCa5.1) channel, with an IC50 of 169 μM observed in response to voltage pulses of +100 mV. It is valuable for research applications focused on malaria treatment and investigating ion channel physiology. -
Anti-malaria Agent
Quinine hydrochloride is an alkaloid extracted from the bark of the cinchona tree, primarily functioning as an anti-malarial agent. It acts as a potassium channel inhibitor, specifically targeting the WT mouse Slo3 (KCa5.1) channel and demonstrating inhibitory effects on channel currents evoked by voltage pulses to +100 mV, with an IC50 value of 169 μM. This compound is widely utilized in research applications related to malaria treatment and ion channel studies. -
Anti-malarial Agent
Quinine hemisulfate is an orally active alkaloid derived from cinchona bark, primarily recognized for its anti-malarial properties. This compound acts as a potassium channel inhibitor, specifically targeting the WT mouse Slo3 (KCa5.1) channel, with an IC50 value of 169 μM for channel currents induced by voltage pulses to +100 mV. Quinine hemisulfate serves as a valuable reagent for anti-malarial studies and relevant pharmacological investigations. -
Anti-malarial Agent
Quinine dihydrochloride is an orally active alkaloid extracted from cinchona bark, primarily used as an anti-malarial agent. It functions as a potassium channel inhibitor, specifically targeting the WT mouse Slo3 (KCa5.1) channel, with an IC50 of 169 μM. This compound is utilized in various research applications aimed at understanding malaria pathophysiology and exploring therapeutic strategies for its treatment. -
Stable Isotope
Quinine-d3 is a deuterium-labeled derivative of quinine, primarily used as a stable isotope in chemical research. Quinine is an alkaloid isolated from the cinchona tree, known for its efficacy as an antimalarial agent and its role as a potassium channel inhibitor. It specifically inhibits wild-type mouse Slo3 (KCa5.1) channel currents induced by voltage pulses, exhibiting an IC50 of 169 μM. This reagent facilitates studies in pharmacology and biochemistry, enabling precise tracking and quantification in various applications. -
CCR8 Antagonist
AZ760 is a potent antagonist of the CCR8 receptor, which plays a significant role in immune response modulation. This compound demonstrates excellent potency and favorable lipophilicity, resulting in a high free fraction in blood. However, it is important to note that AZ760 exhibits unacceptable inhibition of the hERG potassium channel, which may have implications for cardiovascular safety in therapeutic applications. -
CB1/2 Agonist
AB-FUBICA is a potent agonist for CB1 and CB2 receptors, serving as a valuable tool in cannabinoid research. It functions by activating G-protein coupled inwardly rectifying potassium channels (GIRK) through its binding to these receptors, demonstrating significant cannabinoid-like activity. With EC50 values of 21 nM for CB1 and 15 nM for CB2, AB-FUBICA is ideal for investigating pain management, neurodegenerative diseases, and inflammation-related pathways. -
Adrenergic Receptor Inhibitor
Besipirdine is an adrenergic receptor inhibitor that exhibits non-receptor-dependent cholinomimetic properties. This compound is known to inhibit voltage-dependent sodium and potassium channels, contributing to its pharmacological profile. Besipirdine's biological activity makes it relevant for research applications focused on neuropharmacology and the modulation of synaptic transmission. -
FTO Inhibitor
Meclofenamic acid sodium hydrate is a selective inhibitor of fat mass and obesity-associated enzyme (FTO). Its primary action involves competing with FTO for binding to m(6)A-containing nucleic acids, thereby influencing RNA metabolism. Additionally, it exhibits non-selective gap-junction blocking activity and inhibits potassium channels hKv2.1 and hKv1.1, with IC50 values of 56.0 μM and 155.9 μM, respectively. This compound is valuable in research focused on obesity, metabolic regulation, and the role of RNA modifications in cellular processes. -
μ-opioid Receptor Activator, hERG (Kv11.1) Potassium Channel Inhibitor
ERG-IN-6 is a potent μ-opioid receptor activator, exhibiting an EC50 of 0.12 nM, which makes it an effective tool for studies related to pain modulation. Additionally, ERG-IN-6 functions as a hERG (Kv11.1) potassium channel inhibitor with an IC50 of 0.681 μM. This compound is valuable for research applications investigating the interplay between opioid signaling and ion channel regulation. -
ORL1 Receptor Antagonist
MK-1925 is a selective ORL1 receptor antagonist, demonstrating human IC50 values of 8.2 nM and 4.6 nM. This compound exhibits oral bioavailability and the capability to penetrate the blood-brain barrier, making it a valuable tool for neuroscience research. MK-1925 specifically inhibits the ORL1 receptor without significant interaction with other opioid receptors or the hERG potassium channel, positioning it as a potential candidate for studies focused on pain modulation and opioid receptor mechanisms. -
Histamine H1 Receptor Antagonist
Terfenadine N-oxide is a histamine H1 receptor antagonist with an IC50 value of 2.73 μM, also exhibiting inhibition of the hERG potassium channel with an IC50 of 0.698 μM. This compound is valuable for investigating histamine-related allergic diseases and the role of hERG channels in arrhythmias. Its dual activity makes it a useful tool for research in pharmacology and toxicology related to allergic responses and cardiac rhythm disturbances. -
Antispasmodic Agent
Terodiline is an antispasmodic agent that primarily targets the hERG potassium channel, exhibiting an IC50 of 375 nM. It possesses both anticholinergic and calcium antagonist properties, making it effective in reducing abnormal bladder contractions associated with detrusor instability. Terodiline is suitable for research applications focused on urinary incontinence. -
Bupivacaine metabolite
Bupivacaine N-oxide hydrochloride is a metabolite of the local anesthetic Bupivacaine, which primarily acts as an NMDA receptor inhibitor. It also exhibits significant activity by blocking sodium, L-calcium, and potassium channels, particularly SCN5A channels with an IC50 of 69.5 μM. This compound is relevant for research into chronic pain mechanisms and provides insight into the pharmacological action of Bupivacaine and its derivatives. -
Drug Metabolite Control
Nicorandil pyridine oxide is a metabolite of Nicorandil, which acts as an activator of the sulfonylurea receptor 2B (SUR2B) and the ATP-sensitive potassium channel Kir6.2. This compound serves as a crucial tool for drug metabolite control, offering insights into the pharmacokinetics and therapeutic mechanisms of Nicorandil. Its biological activity is important for researchers studying cardiovascular effects and the modulation of ion channels in various biological systems. -
EBP Inhibitor
EBP-IN-1 is a selective inhibitor of emopamil binding protein (EBP) that effectively crosses the blood-brain barrier. This compound demonstrates an IC50 of 8.2 μM against human ERG potassium channels in CHO cells, leading to the inhibition of EBP's sterol isomerase activity and subsequent accumulation of Zymostenol. EBP-IN-1 has been shown to promote oligodendrocyte differentiation in human cortical organoids, making it a valuable tool for research into multiple sclerosis and related neurological disorders. -
Stable Isotope
Bupivacaine-d9 hydrochloride is a deuterium-labeled analog of Bupivacaine hydrochloride, primarily known for its role as an NMDA receptor inhibitor. This compound effectively blocks sodium, L-calcium, and potassium channels, demonstrating potent inhibition of SCN5A channels with an IC50 value of 69.5 μM. Bupivacaine-d9 hydrochloride is valuable for research focused on chronic pain modulation and neuronal signaling studies. -
TRPV4-KCa2.3 Protein Complex Enhancer
TRPV4-KCa2.3 modulator 1 is a modulator that enhances the TRPV4-KCa2.3 protein complex, exhibiting significant antihypertensive activity. This compound promotes hyperpolarization and vasodilation in endothelial cells. Its ability to influence vascular responses makes it a valuable tool for investigating hypertension and related cardiovascular disorders in research settings. -
Kv1.5 Inhibitor
MK-1832 is a selective inhibitor of the Kv1.5 potassium channel, exhibiting an IC50 value of 86 nM. As a P-glycoprotein substrate, MK-1832 is particularly relevant for studying atrial fibrillation and related cardiovascular disorders. Its specificity for Kv1.5 makes it a valuable tool for investigating the molecular mechanisms underlying cardiac arrhythmias and for evaluating potential therapeutic interventions. -
KV1.3 Inhibitor
KV1.3-IN-2 hydrochloride is a selective inhibitor of the KV1.3 potassium channel, with no impact on hERG channel activity. This compound is particularly valuable in the study of immune-related diseases, including psoriasis, rheumatoid arthritis, and systemic lupus erythematosus, due to its ability to modulate KV1.3-mediated cellular processes. Researchers can utilize KV1.3-IN-2 hydrochloride to explore mechanisms underlying these conditions and develop potential therapeutic strategies. -
Nav1.7 Inhibitor
Nav1.7-IN-19 is a selective inhibitor of the voltage-gated sodium channel Nav1.7, demonstrating a potent inhibitory activity with an IC50 of 0.49 μM. This compound exhibits significant selectivity for Nav1.7, with 312-fold and 662-fold selectivity over Nav1.1 and Nav1.5 in their inactivated states, respectively. Additionally, Nav1.7-IN-19 shows minimal inhibition of hERG potassium channels. Due to its analgesic properties, Nav1.7-IN-19 is valuable for research focused on neurological diseases. -
KCNQ2/3 Activator
Azetukalner is a selective Kv7.2/Kv7.3 potassium channel activator, demonstrating an EC50 of 27 nM. This compound exhibits approximately four-fold selectivity for the Kv7.2/7.3 combination over Kv7.3/7.5 and Kv7.4 channels, with EC50 values of 94 nM and 113 nM, respectively. Azetukalner's specificity exceeds 100-fold for Kv7 channels when compared to other ion channels and receptors. This reagent is valuable for research focused on focal epilepsy. -
CPS1 Inhibitor
H3B-120 is a selective inhibitor of carbamoyl phosphate synthetase 1 (CPS1) that functions through competitive allosteric modulation, exhibiting an IC50 of 1.5 μM and a Ki of 1.4 μM. This compound demonstrates anti-cancer activity, making it a valuable tool for research into metabolic and oncological pathways. H3B-120 can be utilized in studies investigating the role of CPS1 in cancer metabolism and therapeutic targeting. -
Complex II Inhibitor
Atpenin A5 is a highly selective inhibitor of complex II, with an IC50 of approximately 10 nM. This compound acts as a potent mKATP channel agonist, offering cardioprotective effects. It is valuable for research applications focused on mitochondrial function, cardiac physiology, and energy metabolism. -
TMEM175 Blocker
2-PPA is a selective blocker of the TMEM175 lysosomal potassium and proton channel, inhibiting the pore to occlude ion permeation pathways. This compound enhances lysosomal macromolecule degradation and accelerates macropinocytosis, making it a valuable tool in cellular and molecular research. 2-PPA's ability to covalently bind to hepatic proteins further supports its potential in investigating cellular processes. Its applications extend to the study of Parkinson's disease, providing insights into lysosomal function and related pathologies. -
ATP Analog
AMP-PNP tetralithium is a non-hydrolyzable ATP analog that serves as a potent inhibitor of ATP-dependent processes. It binds to ATP-binding sites without undergoing hydrolysis, thereby maintaining stable experimental conditions for the investigation of various biochemical pathways. This reagent is particularly valuable in studies of enzyme activity, kinase regulation, DNA and RNA metabolism, ion channel function, and protein complex assembly. -
Potassium Channel Activator
Pinacidil is a potent activator of ATP-sensitive potassium channels, primarily functioning as an antihypertensive agent. By facilitating K+ efflux in vascular smooth muscle, it induces hyperpolarization and promotes vasorelaxation, thereby inhibiting spontaneous tone and reducing contractions induced by agonists. Pinacidil is valuable for research applications in the study of cardiovascular diseases and vascular function. -
Kir6.2 Inhibitor
L-Palmitoylcarnitine chloride is a selective inhibitor of the Kir6.2 subunit of KATP channels. It disrupts membrane lipid homeostasis during ischemic conditions by accumulating in the sarcolemma while inhibiting channel activity without altering single-channel conductance. This compound is valuable for research into metabolic disturbances and the role of KATP channels in cardiac and skeletal muscle physiology. -
SK Channels Inhibitor
NS8593 hydrochloride is a selective inhibitor of small conductance Ca2+-activated K+ channels (SK channels). This compound demonstrates reversible inhibition of SK3-mediated currents with a Kd value of 77 nM, as well as inhibiting SK1-3 subtypes in a Ca2+-dependent manner (Kds of 0.42, 0.60, and 0.73 μM respectively at 0.5 μM Ca2+). Importantly, NS8593 hydrochloride does not affect intermediate and large conductance Ca2+-activated K+ channels, such as hIK and hBK channels. It is valuable for research applications exploring the role of SK channels in cellular signaling and excitability. -
TMEM175 Inhibitor
AP-6 is a selective inhibitor of TMEM175, targeting lysosomal function modulation. This compound enhances lysosomal macromolecular catabolism, promoting accelerated digestive processes in macrophages and other cell types. AP-6 is a valuable tool in research related to Parkinson's disease, providing insights into lysosomal dysregulation and its implications in neurodegeneration. -
KCNQ2/Q3 Opener
ICA-27243 is a selective and orally active opener of the KCNQ2/Q3 potassium channels, exhibiting an EC50 of 0.38 μM. This compound has demonstrated potent antiepileptic and anticonvulsant properties, making it valuable for neurological research. Additionally, it shows lower efficacy towards KCNQ4 and the KCNQ3/Q5 channels, highlighting its specificity. ICA-27243 is an important tool for investigating the role of KCNQ channels in neuronal excitability and related disorders. -
KCC2 Activator
CLP257 is a selective activator of the K+-Cl cotransporter KCC2, exhibiting an EC50 of 616 nM. It specifically enhances Cl transport in neurons with reduced KCC2 activity while showing no effects on NKCC1, GABAA receptors, KCC1, KCC3, or KCC4. This compound is shown to alleviate hypersensitivity in neuropathic pain models in rats and modulates KCC2 protein turnover at the plasmalemmal level post-translationally. CLP257 is valuable for research into neuron excitability and synaptic transmission. -
Ca2+-activated K+ Channel Inhibitor
Iberiotoxin is a potent inhibitor of Ca2+-activated K+ channels, derived from the venom of the Buthus tamulus scorpion. It demonstrates high specificity and selectivity, with an affinity (Kd) of approximately 1 nM, effectively blocking high conductance channels without affecting other voltage-dependent ion channels. This characteristic makes Iberiotoxin a valuable tool for investigating the physiological roles of Ca2+-activated K+ channels in various biological processes and for exploring their relevance in neurophysiological and cardiological research applications. -
TREK-1/2 Opener
BL-1249 is a selective opener of the TREK-1 (K2P2.1) and TREK-2 (K2P10.1) potassium channels, demonstrating potent activation with EC50 values of 5.5 μM and 8.0 μM, respectively. This compound effectively activates all members of the TREK subfamily while exhibiting no activity towards other K2P subfamilies. Notably, BL-1249 shows enhanced selectivity for bladder tissue, with an EC50 of 1.26 μM, compared to a higher EC50 of 21.0 μM in vascular tissue. The compound is valuable in research related to pain management and bladder function regulation. -
Kv12.2 (KCNH3) Inhibitor
ASP2905 is a potent inhibitor of the potassium channel Kv12.2 (KCNH3), encoded by the Kcnh3/BEC1 gene. This compound is orally active and capable of crossing the blood-brain barrier, exhibiting significant antipsychotic properties. ASP2905 is valuable for studying the roles of Kv12.2 in neuropsychiatric disorders and exploring therapeutic avenues for conditions such as schizophrenia. -
CHI3L1 Inhibitor
CHI3L1-IN-1 is a selective inhibitor of Chitinase-3-like protein 1 (CHI3L1), also known as YKL-40, with an IC50 of 50 nM. This compound exhibits additional effects by inhibiting the hERG channel with an IC50 of 2.3 μM. CHI3L1-IN-1 is valuable for research applications focused on the roles of CHI3L1 in inflammation and cancer, offering insights into its potential as a biomarker and therapeutic target. -
REK-1/TRAAK Agonist
2,2,2-Trichloroethanol functions as an agonist for the K2P potassium channels TREK-1 (KCNK2) and TRAAK (KCNK4). This compound is known to modulate neuronal excitability and plays a significant role in research related to pain, mood disorders, and neuroprotection. Its ability to enhance K2P channel activity makes it a valuable reagent for investigating the physiological and pharmacological properties of these ion channels. -
GIRK1/2 Activator
ML 297 is a potent and selective activator of GIRK1/2 channels, exhibiting an EC50 of 0.16 μM. This compound effectively crosses the blood-brain barrier, demonstrated by a brain-to-plasma ratio of 0.2 in murine models following intraperitoneal administration. ML 297 is under investigation for its potential therapeutic applications in the treatment of epilepsy.
