Catalog No.
Product Name
Application
Product Information
Citations
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P-glycoprotein Agonist
MCI826 is a P-glycoprotein (P-gp) agonist that enhances the efflux of various substrates across cell membranes. Its primary biological activity focuses on modulating drug transport and influencing cellular drug accumulation. This compound is valuable in research applications related to pharmacokinetics, multidrug resistance, and therapeutic strategies involving P-gp. -
Piezo1 Channel Activator
Jedi2 is a selective activator of the Piezo1 ion channel, facilitating mechanotransduction in various physiological processes. It demonstrates a binding affinity (Kd) of 2770 μM for mouse Piezo1 proteins, enabling the study of Piezo1's role in cellular responses to mechanical stimuli. This compound is suitable for research applications investigating the physiological and pathological implications of Piezo1 activation in multiple biological systems. -
Piezo1 Agonist
Yaddle1 is a potent agonist of the mechano-activated ion channel Piezo1, exhibiting a half-maximal effective concentration (MEC50) of 0.40 μM. This compound effectively promotes Ca2+ influx in T cells, leading to significant T cell activation. Yaddle1 serves as a valuable tool in research applications focused on vaccine adjuvants and the modulation of immune responses. -
Piezo1 Agonist
Yoda2 (KC289) functions as a Piezo1 agonist with an EC50 of 150 nM, facilitating calcium ion elevation and nitric oxide-dependent relaxation. This compound induces vasodilation in mouse arterial and cavernous tissues. Additionally, Yoda2 is implicated in inhibiting glucocorticoid-induced osteoclast formation and bone resorptive activity, effectively reversing glucocorticoid-mediated bone density loss and structural deterioration. Its applications extend to research in areas such as hypertension and osteoporosis. -
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. -
Antiarrhythmic Agent
Flecainide is an orally active antiarrhythmic agent that primarily targets sodium channels to modulate cardiac excitability. By inhibiting calcium ion release mediated by the ryanodine receptor (RyR2), it plays a critical role in the study of arrhythmias. Research applications include the investigation of diseases such as catecholaminergic polymorphic ventricular tachycardia (CPVT), where it may help elucidate underlying mechanisms and therapeutic strategies. -
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. -
M-type K+ current Inhibitor
Linopirdine is a selective inhibitor of the M-type potassium current (IM; Kv7; KCNQ channels) with an IC50 of 2.4 μM. This compound exhibits potential as a cognition-enhancing agent by promoting acetylcholine release in rat brain tissue. Linopirdine is primarily utilized in research focused on understanding cognitive function and the modulation of neurotransmitter release. Additionally, its role as a TRPV1 agonist provides further avenues for investigation in neurobiology and pharmacology. -
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. -
Potassium Channel Opener
Rimtuzalcap is a selective positive allosteric modulator targeting small-conductance calcium-activated potassium channels (SK channels). This compound exhibits key biological activity as a potassium channel opener, which may facilitate neuronal hyperpolarization and reduce excitability. Rimtuzalcap is primarily utilized in research focused on movement disorders, such as essential tremor (ET) and spinocerebellar ataxia (SCA), providing insights into potential therapeutic avenues for these conditions. -
Cationic Amphiphilic Lytic Peptide
L17E is an attenuated cationic amphiphilic lytic peptide that facilitates the delivery of macromolecules, including proteins, antibodies, and DNA nanostructures. Its mechanism involves membrane insertion and cleavage via electrostatic interactions, promoting intracellular escape. The effectiveness of L17E is closely linked to the expression of KCNN4, encoding the calcium-activated potassium channel KCa3.1, and it enhances cellular uptake through the induction of micropinocytosis. Additionally, L17E can be optimized through dimerization and combined with other delivery systems, such as nuclear localization signal peptides and cell membrane-coated nanoparticles, for improved performance in research applications. -
KCNQ Channel Blocker
XE991 is a potent blocker of KCNQ (Kv7) channels, effectively inhibiting Kv7.1 (KCNQ1), Kv7.2 (KCNQ2), Kv7.3 (KCNQ3), and the M-current with IC50 values of 0.75 µM, 0.71 µM, 0.6 µM, and 0.98 µM, respectively. This selective inhibition makes XE991 a valuable tool for studying the physiological and pathophysiological roles of KCNQ channels in cells. It has applications in neurological research and the exploration of conditions related to ion channel dysfunction. -
Kv1.3 Inhibitor
Margatoxin is a highly selective inhibitor of the voltage-gated potassium channel Kv1.3, with a binding affinity (Kd) of 11.7 pM. It also exhibits inhibitory effects on Kv1.2 (Kd = 6.4 pM) and Kv1.1 (Kd = 4.2 nM). This 39-amino-acid peptide, derived from the venom of Centruroides margaritatus, is extensively utilized in ion channel research to study the role of Kv1.3 in various physiological and pathophysiological processes. -
KATP Channel Blocker
5-Hydroxydecanoate sodium is a selective blocker of ATP-sensitive K+ (KATP) channels, exhibiting an IC50 of approximately 30 μM. This compound serves as a substrate for mitochondrial outer membrane acyl-CoA synthetase and possesses antioxidant properties. It is primarily utilized in research to study the physiological and pathophysiological roles of KATP channels in various cellular processes. -
KCNQ1/mink Activator
L-364,373 is a selective activator of the voltage-gated Kv7.1 (KCNQ1) channels. It enhances the Iks (slow delayed rectifier potassium current) and significantly shortens action potential duration in guinea pig cardiac myocytes, while also suppressing early afterdepolarizations in rabbit ventricular myocytes. This compound is valuable for research on cardiac electrophysiology and the mechanisms underlying cardiac arrhythmias. -
hERG Channel Activator
ICA-105574 is a potent hERG channel activator that primarily functions by inhibiting the inactivation of hERG channels. It significantly increases current amplitudes by more than 10-fold, demonstrating an EC50 of 0.5 ± 0.1 μM and a Hill slope of 3.3 ± 0.2. This compound has been shown to prevent arrhythmias resulting from cardiac delayed repolarization and can concentration-dependently shorten action potential duration in ventricular myocytes, making it valuable for cardiovascular research applications. -
Kv1.3 Inhibitor
Dalazatide is a potent inhibitor of the Kv1.3 potassium channel, specifically designed for research applications in autoimmune diseases. This peptide has shown efficacy in the modulation of immune responses, making it a valuable tool for studying conditions such as multiple sclerosis, lupus erythematosus, psoriasis, rheumatoid arthritis, type 1 diabetes, and inflammatory bowel disease. Its role in Kv1.3 inhibition provides insights into the pathophysiology of these diseases and potential therapeutic avenues. -
Kv7.2/7.3 Activator
Opakalim is a selective activator of Kv7.2 and Kv7.3 potassium channels, exhibiting an EC50 of 0.6 μM. It demonstrates minimal activation of GABAA receptors while offering potent anti-seizure efficacy in the maximal electroshock seizure (MES) model. Opakalim is suitable for research applications focused on seizure mechanisms and the modulation of neuronal excitability. -
Anti-arrhythmic Agent
Ibutilide is a potent anti-arrhythmic agent primarily targeting the rapidly activating delayed rectifier K+ current (IKr). By prolonging action potentials, it effectively manages cardiac arrhythmias. This compound is commonly utilized in electrophysiology research to study cardiac action potentials and the mechanisms underlying arrhythmogenesis. -
Kir4.1 Blocker
VU0134992 hydrochloride is a selective blocker of the Kir4.1 potassium channel, exhibiting an IC50 of 0.97 µM. This compound demonstrates a nine-fold selectivity for homomeric Kir4.1 channels compared to Kir4.1/5.1 concatemeric channels, with an IC50 of 9 µM at -120 mV. Its unique profile makes it a valuable tool for investigating the physiological roles of Kir4.1 channels in various biological processes and potential therapeutic applications. -
KATP Channel Opener
Tifenazoxide (NN414) is a potent, orally active opener of KATP channels, specifically targeting the SUR1/Kir6.2 subunits. This compound demonstrates antidiabetic properties by inhibiting glucose-stimulated insulin release both in vitro and in vivo, thereby contributing to enhanced glucose homeostasis. Tifenazoxide is valuable for research applications focused on diabetes and metabolic disorders. -
PKG Activator
Dibutyryl-cGMP sodium is a cell-permeable analogue of cyclic guanosine monophosphate (cGMP) that primarily activates cGMP-dependent protein kinase (PKG). This compound has been shown to inhibit the release of [3H]-arachidonic acid from γ-thrombin-stimulated human platelets, demonstrating its role in modulating platelet activity. Additionally, Dibutyryl-cGMP sodium induces peripheral antinociception through the activation of ATP-sensitive potassium channels, making it a valuable tool for research in pain modulation and cardiovascular physiology. -
TASK-3 Agonist/TWIK2 Blocker
NPBA is a potassium K2P channel TASK-3 (KCNK9) agonist and TWIK2 (KCNK1) channel blocker. This compound plays a crucial role in inhibiting NLRP3 inflammasome activation in macrophages, making it valuable for research into inflammatory pathways and potassium channel function. Its unique mechanism provides insights into potential therapeutic applications in inflammatory diseases. -
SK2/3 Positive Modulator
CyPPA is a positive modulator of human small conductance potassium channels hSK2 and hSK3, exhibiting EC50 values of 14 μM and 5.6 μM, respectively. This compound does not activate hSK1 or hIK channels, making it selective for its target. CyPPA is utilized in research to investigate the physiological roles and therapeutic potential of small conductance potassium channels in various biological processes. -
Sodium Current Inhibitor
Eleclazine hydrochloride is a selective inhibitor of the cardiac late sodium current, exhibiting an IC50 value of less than 1 μM, along with a weaker inhibitory effect on potassium current (IC50 approximately 14.2 μM). This compound demonstrates therapeutic potential by providing protection against autonomically induced atrial premature beats, repolarization alternans, heterogeneity, and atrial fibrillation in porcine models. Eleclazine hydrochloride is applicable in the study of cardiac arrhythmias and their underlying mechanisms. -
TREK1/2 Channels Opener
GI-530159 is a selective opener of TREK1 and TREK2 potassium channels, exhibiting an EC50 of 0.76 μM for TREK1. This compound demonstrates a significant ability to reduce excitability in rat dorsal root ganglion neurons, indicating potential analgesic effects. GI-530159 is valuable for research applications focused on pain modulation and the physiological roles of TREK channels in neuronal activity. -
Antiarrhythmic Agent
Flecainide hydrochloride is a potent antiarrhythmic agent that primarily targets sodium channels in cardiac tissues. By inhibiting the release of calcium ions mediated by the cardiac ryanodine receptor (RyR2), it effectively stabilizes cardiac membrane excitability. This compound is utilized in research studies focusing on cardiac arrhythmias, including catecholaminergic polymorphic ventricular tachycardia (CPVT) and other related cardiovascular diseases. -
Sodium Channel Inhibitor
Ropivacaine hydrochloride monohydrate is a potent sodium channel inhibitor that reversibly blocks sodium ion influx, thereby disrupting impulse conduction in nerve fibers. Additionally, it inhibits the K2P potassium channel TREK-1 with an IC50 of 402.7 μM in COS-7 cell membranes. This compound is widely utilized for regional anesthesia and in the management of neuropathic pain in vivo, making it a valuable reagent in pain research and therapeutic applications. -
Kv7 Potassium Channels Opener
ICA-105665 is a potent opener of neuronal Kv7.2/7.3 and Kv7.3/7.5 potassium channels. It effectively enhances potassium ion flow, making it relevant for research in neurological disorders, particularly in the context of seizure activity. Additionally, ICA-105665 inhibits liver mitochondrial function and bile salt export protein (BSEP) transport with an IC50 of 311 μM, positioning it as a valuable tool for studying both central nervous system and hepatic physiological processes. Its ability to penetrate the blood-brain barrier further supports its utility in investigating antiseizure mechanisms. -
K(v)7 Channels Modulator
QO 58 is a potent modulator of K(v)7 channels, specifically enhancing current amplitudes and shifting the voltage-dependent activation curve in a more negative direction. Additionally, it effectively slows the deactivation of K(v)7.2/K(v)7.3 currents. This compound is valuable for studying diseases linked to neuronal hyperexcitability, providing insights for potential therapeutic applications. -
Potassium Channel Modulator
Flindokalner is a potassium channel modulator that positively influences all neuronal Kv7 channel subtypes expressed in HEK293 cells, alongside acting as a positive modulator of large conductance calcium-activated potassium channels (BKca). It exhibits negative modulatory activity at Kv7.1 channels with a Ki of 3.7 μM and also negatively modulates GABAA receptors. In vivo studies demonstrate its anxiolytic efficacy, making it a valuable reagent for research in neuropharmacology and the study of ion channel function. -
Potassium Channel Opener
Cromakalim functions as a potassium channel opener, facilitating relaxation of smooth muscle tissue. It exhibits bronchodilator activity in asthma by inhibiting the spontaneous tone of human isolated bronchi in a concentration-dependent manner. Its effectiveness is comparable to that of isoprenaline or theophylline, making it a valuable tool for research in respiratory physiology and pharmacology. -
KCNQ2 Inhibitor
ML252 is a selective inhibitor of the KCNQ2 (Kv7.2) ion channel, exhibiting an IC50 of 69 nM for KCNQ2, along with lower inhibitory effects on KCNQ1, KCNQ2/Q3, and KCNQ4. This compound also demonstrates inhibition of key Cytochrome P450 enzymes, including CYP1A2, CYP2C9, CYP3A4, and CYP2D6, with IC50 values ranging from 3.9 nM to 19.9 nM. ML252 is notable for its ability to penetrate the blood-brain barrier, making it a valuable tool for investigating neuronal function and related disorders. -
TREK Activator
ONO-2920632 is an orally active TREK activator that effectively penetrates the central nervous system, exhibiting EC50 values of 0.3 µM for TREK-1 and 2.8 µM for TREK-2. This compound demonstrates significant selectivity for TREK channels over other K2P channels, showing more than 91-fold selectivity versus TASK1, TASK2, TASK3, TRAAK, and TWIK2, as well as 31-fold selectivity for TRESK. ONO-2920632 is recognized for its analgesic properties and is suitable for research applications in pain management, migraine, and various neurological disorders.
