Potassium Channel Inhibitor

BAPTA-AM is a well-known membrane permeable Ca²⁺ chelator. BAPTA-AM inhibits hERG channels, hKv1.3 and hKv1.5 channels in HEK 293 cells with IC₅₀s of 1.3 μM, 1.45 μM and 1.23 μM, respectively.

ShK toxin TFA (Stichodactyla helianthus neurotoxin TFA) is a neurotoxin. ShK toxin TFA blocks voltage-dependent potassium channel (K_v1.3 channel). ShK toxin TFA can be isolated from the whole body extract of the Caribbean sea anemone (Stichodactylu helianthus). ShK toxin TFA competes with dendrotoxin I and α-dendrotoxin for binding to synaptosomal membranes of rat brain, facilitates acetylcholine release. ShK toxin TFA suppresses K⁺ currents in cultured rat dorsal root ganglion neurons. ShK toxin TFA also inhibits T lymphocyte proliferation.

CPL500036 is an orally active, blood-brain barrier permeable phosphodiesterase 10A (PDE10A) inhibitor with IC₅₀ values of 1 nM (Reference 1) and 35 nM (Reference 2). CPL500036 acts as a negative allosteric modulator of the M2 muscarinic receptor with an IC₅₀ of 9.2 μM. CPL500036 alters cyclic nucleotide levels in basal ganglia circuits, inhibits the hydrolysis of cAMP and cGMP, and suppresses hERG potassium channel tail currents. CPL500036 induces catalepsy in rats and reverses injury-induced contralateral forelimb use impairment. CPL500036 can be used in research related to schizophrenia, Parkinson's disease, and levodopa-induced dyskinesia.

Rosuvastatin Calcium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC₅₀ of 11 nM. Rosuvastatin Calcium potently blocks hERG current with an IC₅₀ of 195 nM. Rosuvastatin Calcium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Calcium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.

Ac4ManNAz can be taken up by cells and is an azide-containing metabolic glycoprotein labeling reagent that selectively modifies proteins. Commonly used for cell labeling, tracking and proteomic analysis. Ac4ManNAz contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Ac4ManNAz can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.

SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) is a potent and selective dopamine D₁-like receptor antagonist with K_is 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-HT_2C receptor agonist with a K_i of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the 5-HT₂ and 5-HT_1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC₅₀ of 268 nM.

Glibenclamide (Glyburide) is an orally active ATP-sensitive K⁺ channel (K_ATP) inhibitor and can be used for the research of diabetes and obesity. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of K_ATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR). Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability. Glibenclamide can induce autophagy.

Carbamazepine is an orally active pressure-sensitive sodium ion channel blocker with an IC₅₀ of 131 μM. Carbamazepine blocks voltage gated Na⁺, Ca²⁺, and K⁺ channels, and is also a HDAC inhibitor (IC₅₀: 2 μM). Carbamazepine is an anticonvulsant and can be used for research of epilepsy and neuropathic pain.

Branaplam (LMI070; NVS-SM1) is a highly potent, selective and orally active survival motor neuron-2 (SMN2) splicing modulator with an EC₅₀ of 20 nM for SMN. Branaplam inhibits human-ether-a-go-go-related gene (hERG) with an IC₅₀ of 6.3 μM. Branaplam elevates full-length SMN protein and extends survival in a severe spinal muscular atrophy (SMA) mouse model.

20(S)-Ginsenoside Rg3 is the main component of Panax ginseng C. A. Meyer. Ginsenoside Rg3 inhibits Na⁺ and hKv1.4 channel with IC₅₀s of 32.2±4.5 and 32.6±2.2 μM, respectively. 20(S)-Ginsenoside Rg3 also inhibits Aβ levels, NF-κB activity, and COX-2 expression.

Tetrandrine (NSC-77037; d-Tetrandrine) is a bis-benzyl-isoquinoline alkaloid, which inhibits voltage-gated Ca²⁺ current (ICa) and Ca²⁺-activated K⁺ current.

E-4031 is a selective hERG potassium channel blocker for use in class III anti-arrhythmic studies.

Tannic acid is a novel hERG channel blocker with IC₅₀ of 3.4 μM.

W-7 hydrochloride is a selective calmodulin antagonist. W-7 hydrochloride inhibits the Ca²⁺-calmodulin-dependent phosphodiesterase and myosin light chain kinase with IC₅₀ values of 28 μM and 51 μM, respectively. W-7 hydrochloride induces apoptosis and has antitumor and vascular relaxing activity. W-7 hydrochloride is a blocker of Kv4.3 and can be used for research of arrhythmias.

Dofetilide (UK 68789), as a class III antiarrhythmic agent, is an orally active, potent and specific IKr blocker. Dofetilide can be used for the research of cardiovascular disease.

Quinidine (15% dihydroquinidine) is an antiarrhythmic agent. Quinidine is a potent, orally active, selective cytochrome P450db inhibitor. Quinidine is also a K⁺ channel blocker with an IC₅₀ of 19.9 μM, and can induce apoptosis. Quinidine can be used for malaria research.

Amiodarone, a benzofuran-based Class III antiarrhythmic agent, inhibits WT outward ionic current (IhERG) tails with an IC₅₀ of ∼45 nM. Amiodarone induces cell proliferation and myofibroblast differentiation via ERK1/2 and p38 MAPK signaling in fibroblasts. Amiodarone can be used in the research of both supraventricular and ventricular arrhythmias.

Amiodarone hydrochloride, a benzofuran-based Class III antiarrhythmic agent, inhibits WT outward ionic current (IhERG) tails with an IC₅₀ of ∼45 nM. Amiodarone hydrochloride induces cell proliferation and myofibroblast differentiation via ERK1/2 and p38 MAPK signaling in fibroblasts. Amiodarone hydrochloride can be used in the research of both supraventricular and ventricular arrhythmias.

TRAM-34 is a highly selective blocker of intermediate-conductance calcium-activated K⁺ channel (IKCa1) (K_d=20 nM).

Ketanserin is a selective 5-HT2 receptor antagonist. Ketanserin also blocks hERG current (I_hERG) in a concentration-dependent manner (IC₅₀=0.11 μM).