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o-3M3FBS is the negative control of m-3M3FBS. o-3M3FBS inhibits inward and outward currents via mechanisms independent of PLC acting in an antagonistic manner. In contrast, o-3M3FBS also causes an increase in [Ca 2+]i in an agonistic manner .
Cholesterol myristate is a natural steroid present in traditional Chinese medicine. Cholesterol myristate binds to several ion channels such as the nicotinic acetylcholine receptor, GABAA receptor, and the inward-rectifier potassium ion channel.
Lotusine is a pure alkaloid extracted from the green seed embryo of Nelumbo nucifera Gaertn. Lotusine shows effects on the action potentials in myocardium and slow inward current in cardiac Purkinje fibers .
Lotusine (hydroxide) is a pure alkaloid extracted from the green seed embryo of Nelumbo nucifera Gaertn. Lotusine (hydroxide) shows effects on the action potentials in myocardium and slow inward current in cardiac Purkinje fibers .
Dimethyl lithospermate B (dmLSB) is a selective Na + channel agonist. Dimethyl lithospermate B slows inactivation of sodium current (INa), leading to increased inward current during the early phases of the action potential (AP) .
Antiarrhythmic agent-2 is a nonspecific Ca 2+inward current blocker that inhibits ionic currents in sensory neuron membranes. Antiarrhythmic agent-2 can be used in the study of cardiovascular diseases, such as arrhythmias .
NP-313 is a potent antithrombotic agent that inhibits platelet aggregation and activation. NP-313 has dual inhibition of thromboxane A 2 synthesis and selective inhibition of SOCC-mediated Ca 2+inward flow .
GMQ is a ASIC (acid-sensing ion) channel activator with an EC50 value of 1.83 mM for ASIC3 at pH 7.4. GMQ opens only ASIC3 but no other ASICs at pH 7.4. GMQ can be used for neurological disease research .
NPBA, a potassium K2P channel TASK-3 (KCNK9) agonist, is a tandem pore domain weak inward rectifying K + channel (TWIK2) channel blocker. NPBA suppresses NLRP3 inflammasome activation in macrophages .
(R)-IDHP is an isomer of IDHP, a salvia metabolite that exerts vasorelaxant effects by inhibiting Ca 2+ release and Ca 2+inward flow in voltage-dependent and receptor-operated calcium channels in vascular smooth muscle cells. IDHP is used in studies of cardiovascular disease .
G907 is a selective antagonist of ATP-binding cassette (ABC) transporter MsbA with anti-microbial activity. G907 inhibits E. coli MsbA with an IC50 value of 18 nM. G907 traps MsbA in an inward-facing, lipopolysaccharide-bound conformation by wedging into an architecturally conserved transmembrane pocket .
Ranolazine dihydrochloride (CVT 303 dihydrochloride) is an anti-angina agent that achieves its effects by inhibiting the late phase of inwardsodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP) . Ranolazine dihydrochloride is also a partial fatty acid oxidation inhibitor .
Flecainide hydrochloride is a potent and orally active antiarrhythmic agent. Flecainide hydrochloride blocks the cardiac fast inward Na + current (INa) and the rapid component of the delayed rectifier K + current. Flecainide hydrochloride prolongs the action potential duration (APD) in ventricular and atrial muscle fibres. Flecainide hydrochloride has the potential for the research of fetal tachycardias .
Flecainide is a potent and orally active antiarrhythmic agent. Flecainide blocks the cardiac fast inward Na + current (INa) and the rapid component of the delayed rectifier K + current. Flecainide prolongs the action potential duration (APD) in ventricular and atrial muscle fibres. Flecainide has the potential for the research of fetal tachycardias .
Disopyramide (Dicorantil) is a class IA antiarrhythmic agent with efficacy in ventricular and atrial arrhythmias. Disopyramide blocks the fast inwardsodium current of cardiac muscle and prolongs the duration of cardiac action potentials. Disopyramide inhibits HERG encoded potassium channels. Disopyramide also exhibits complex protein binding, and has a potent negative inotropic action .
Disopyramide phosphate is a class IA antiarrhythmic agent with efficacy in ventricular and atrial arrhythmias. Disopyramide phosphate blocks the fast inwardsodium current of cardiac muscle and prolongs the duration of cardiac action potentials. Disopyramide phosphate inhibits HERG encoded potassium channels. Disopyramide phosphate also exhibits complex protein binding, and has a potent negative inotropic action .
Ranolazine (CVT 303) is an anti-angina drug that achieves its effects by inhibiting the late phase of inwardsodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP) . Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor . Antianginal agent.
Proflavine hemisulfate, an acridine dye, is a known DNA intercalating agent. Anti-microbial agent . Proflavine hemisulfate behaves as a pore blocker for Kir3.2. Proflavine hemisulfate is a potential lead compound for Kir3.2-associated neurological diseases .
Ranolazine-d8 (dihydrochloride) is the deuterium labeled Ranolazine dihydrochloride. Ranolazine dihydrochloride (CVT 303 dihydrochloride) is an anti-angina agent that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)[1][2]. Ranolazine dihydrochloride is also a partial fatty acid oxidation inhibitor[3].
VU0529331 is a modestly selective non-GIRK1-containing G protein-gated, inwardly-rectifying, potassium channel (non-GIRK1/X) activator, with EC50s of 5.1 µM and 5.2 µM for GIRK2 and GIRK1/2 in HEK293 cells, respectively, also effective on GIRK4 homomeric channel .
Ranolazine-d3 is the deuterium labeled Ranolazine. Ranolazine (CVT 303) is an anti-angina agent that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)[1][2]. Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor[3]. Antianginal agent.
Ranolazine-d8 is the deuterium labeled Ranolazine. Ranolazine (CVT 303) is an anti-angina agent that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)[1][2]. Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor[3]. Antianginal agent.
Ranolazine-d5 is the deuterium labeled Ranolazine. Ranolazine (CVT 303) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)[1][2]. Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor[3]. Antianginal agent.
Zatebradine (UL-FS-49 (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 values 1.96 µM. Zatebradine blocks the slow inward current through human HCN1, HCN2, HCN3 and HCN4 channels, with IC50 values of 1.83 µM, 2.21 µM, 1.90 µM and 1.88 µM, respectively .
Proflavine (3,6-Diaminoacridine) dihydrochloride, an acridine dye, is a DNA intercalating agent and Anti-microbial agent. Proflavine dihydrochloride behaves as a pore blocker for Kir3.2. Proflavine dihydrochloride is a potential lead compound for Kir3.2-associated neurological diseases .
Zatebradine (UL-FS-49 (free base); UL-FS-49CL (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 value of 1.96 µM. Zatebradine blocks the slow inward current through human HCN1, HCN2, HCN3 and HCN4 channels, with IC50 values of 1.83 µM, 2.21 µM, 1.90 µM and 1.88 µM, respectively .
Trovafloxacin is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1inward current. Trovafloxacin does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1 .
Trovafloxacin mesylate is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin mesylate blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin mesylate is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1inward current. Trovafloxacin mesylate does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin mesylate leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1 .
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 .
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 .
Ifenprodil tartrate is a typical noncompetitive NMDA receptor antagonist. Ifenprodil tartrate exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM) . Ifenprodil tartrate inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil tartrate has the potential to be a cerebral vasodilator .
VU041 is a first submicromolar-affinity inhibitor of Anopheles (An.) gambiae and Aedes (Ae.) aegyptiinward rectifier potassium 1 (Kir1) channels with IC50 values of 2.5 μM and 1.7 μM, respectively. VU041 inhibits appreciably is mammalian Kir2.1 (IC50 of 12.7 μM), and has less inhibitory effect on mammalian Kir1.1, Kir4.1, Kir6.2/SUR1, and Kir7.1. VU041 also induces impaired Malpighian tubule function .
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 .
IK1 inhibitor PA-6 (PA-6), a pentamidine analogue, is a selective and potent IK1 (KIR2.x ion-channel-carried inward rectifier current) inhibitor, with IC50 values of 12-15 nM for human and mouse KIR2.x currents. IK1 inhibitor PA-6 (PA-6) elevates KIR2.1 protein expression and induces intracellular KIR2.1 accumulation. IK1 inhibitor PA-6 (PA-6) has the potential to treat atrial fibrillation and arrhythmia .
SCH-23390 maleate (R-(+)-SCH-23390 maleate) 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 maleate is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 maleate also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 maleate inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM .
VU590 is a potent and moderately selective ROMK (Kir1.1) inhibitor, with an IC50 of 290 nM. VU590 also inhibits Kir7.1, with an IC50 of 8 μM. VU590 is not a good probe of ROMK function in the kidney .
VU590 dihydrochloride is a potent and moderately selective ROMK (Kir1.1) inhibitor, with an IC50 of 290 nM. VU590 also inhibits Kir7.1, with an IC50 of 8 μM. VU590 dihydrochloride is not a good probe of ROMK function in the kidney .
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 212 potassium channel inhibitor and activators, which is a useful tool to discover drugs for cardiovascular diseases and potassium channel research.
Proflavine hemisulfate, an acridine dye, is a known DNA intercalating agent. Anti-microbial agent . Proflavine hemisulfate behaves as a pore blocker for Kir3.2. Proflavine hemisulfate is a potential lead compound for Kir3.2-associated neurological diseases .
Cholesterol myristate is a natural steroid present in traditional Chinese medicine. Cholesterol myristate binds to several ion channels such as the nicotinic acetylcholine receptor, GABAA receptor, and the inward-rectifier potassium ion channel.
Egg Laying Hormone, aplysia is a neuropeptide synthesized by the bag cell neurons, which contains 36 amino acids and can stimulate egglaying and ovulation in Aplysia via electrical discharge triggering of neurons. Egg-laying hormone of Aplysia induces a voltage-dependent slow inward current carried by Na' in an identified motoneuron .
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 .
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 .
Cholesterol myristate is a natural steroid present in traditional Chinese medicine. Cholesterol myristate binds to several ion channels such as the nicotinic acetylcholine receptor, GABAA receptor, and the inward-rectifier potassium ion channel.
Lotusine (hydroxide) is a pure alkaloid extracted from the green seed embryo of Nelumbo nucifera Gaertn. Lotusine (hydroxide) shows effects on the action potentials in myocardium and slow inward current in cardiac Purkinje fibers .
Dimethyl lithospermate B (dmLSB) is a selective Na + channel agonist. Dimethyl lithospermate B slows inactivation of sodium current (INa), leading to increased inward current during the early phases of the action potential (AP) .
Lotusine is a pure alkaloid extracted from the green seed embryo of Nelumbo nucifera Gaertn. Lotusine shows effects on the action potentials in myocardium and slow inward current in cardiac Purkinje fibers .
(R)-IDHP is an isomer of IDHP, a salvia metabolite that exerts vasorelaxant effects by inhibiting Ca 2+ release and Ca 2+inward flow in voltage-dependent and receptor-operated calcium channels in vascular smooth muscle cells. IDHP is used in studies of cardiovascular disease .
Ifenprodil tartrate is a typical noncompetitive NMDA receptor antagonist. Ifenprodil tartrate exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM) . Ifenprodil tartrate inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil tartrate has the potential to be a cerebral vasodilator .
The KCNJ16 protein is a member of inwardly rectifying potassium channels, which facilitates the influx of potassium into cells. Extracellular potassium concentration modulates voltage dependence, resulting in a positive voltage shift. KCNJ16 Protein, Human (Cell-Free, His) is the recombinant human-derived KCNJ16 protein, expressed by E. coli Cell-free , with N-10*His labeled tag. The total length of KCNJ16 Protein, Human (Cell-Free, His) is 418 a.a., with molecular weight of 50.8 kDa.
The KCNJ10 protein regulates potassium buffering in brain glial cells, favoring potassium influx due to its inward rectifying properties. Extracellular potassium concentration modulates its voltage dependence, and internal magnesium induces inward rectification by blocking outward current. KCNJ10 Protein, Mouse (Cell-Free, His) is the recombinant mouse-derived KCNJ10 protein, expressed by E. coli Cell-free , with N-10*His labeled tag. The total length of KCNJ10 Protein, Mouse (Cell-Free, His) is 379 a.a., with molecular weight of 48.5 kDa.
KCNJ16 is a member of the inwardly rectifying potassium channel, which facilitates potassium influx and is regulated by extracellular potassium concentration. Its inward rectification involves the suppression of outward current by internal magnesium. KCNJ16 Protein, Rat (Cell-Free, His) is the recombinant rat-derived KCNJ16 protein, expressed by E. coli Cell-free , with N-10*His labeled tag. The total length of KCNJ16 Protein, Rat (Cell-Free, His) is 419 a.a., with molecular weight of 54.0 kDa.
The KCNJ10 protein is an inwardly rectifying potassium channel that plays a critical buffering role in potassium in brain glial cells. It facilitates the influx of potassium and is regulated at extracellular levels. KCNJ10 Protein, Rat (Cell-Free, His) is the recombinant rat-derived KCNJ10 protein, expressed by E. coli Cell-free , with N-6*His labeled tag. The total length of KCNJ10 Protein, Rat (Cell-Free, His) is 379 a.a., with molecular weight of 46.6 kDa.
The KCNJ10 protein is an inwardly rectifying potassium channel that is essential for potassium buffering by glial cells in the brain. It favors potassium influx rather than efflux, and the voltage dependence is regulated by extracellular potassium levels. KCNJ10 Protein, Human (Cell-Free, His) is the recombinant human-derived KCNJ10 protein, expressed by E. coli Cell-free , with N-10*His labeled tag. The total length of KCNJ10 Protein, Human (Cell-Free, His) is 379 a.a., with molecular weight of 48.6 kDa.
The KCNJ10 protein is an inwardly rectifying potassium channel that is essential for potassium buffering by glial cells in the brain. It favors potassium influx rather than efflux, and the voltage dependence is regulated by extracellular potassium levels. KCNJ10 Protein, Human (Cell-Free, His, SUMO) is the recombinant human-derived KCNJ10 protein, expressed by E. coli Cell-free , with N-6*His, N-SUMO labeled tag. The total length of KCNJ10 Protein, Human (Cell-Free, His, SUMO) is 379 a.a., with molecular weight of 58.5 kDa.
Ranolazine-d8 (dihydrochloride) is the deuterium labeled Ranolazine dihydrochloride. Ranolazine dihydrochloride (CVT 303 dihydrochloride) is an anti-angina agent that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)[1][2]. Ranolazine dihydrochloride is also a partial fatty acid oxidation inhibitor[3].
Ranolazine-d3 is the deuterium labeled Ranolazine. Ranolazine (CVT 303) is an anti-angina agent that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)[1][2]. Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor[3]. Antianginal agent.
Ranolazine-d8 is the deuterium labeled Ranolazine. Ranolazine (CVT 303) is an anti-angina agent that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)[1][2]. Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor[3]. Antianginal agent.
Ranolazine-d5 is the deuterium labeled Ranolazine. Ranolazine (CVT 303) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)[1][2]. Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor[3]. Antianginal agent.
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