Potassium Channel Inhibitor

Quinidine sulfate dihydrate is an orally active antiarrhythmic agent. Quinidine sulfate dihydrate reduces the expression level of P-gp, inhibits P-gp-mediated efflux, increases the intracellular accumulation of P-gp substrates, induces PARP cleavage and Caspase-3 activation, and elevates the proportion of Apoptotic cells at the sub-G1 phase. Quinidine sulfate dihydrate exerts sustained block and open-channel block effects on I_K(f). Quinidine sulfate dihydrate alters the urinary metabolic ratio of Amphetamine, modulates the Pentylenetetrazol-induced seizure threshold, and regulates the anticonvulsant effect of Dextromethorphan. Quinidine sulfate dihydrate can be used in studies related to uterine sarcoma and seizures.

Amsacrine isethionate (m-AMSA isethionate) is a Topoisomerase II inhibitor. Amsacrine isethionate intercalates into DNA. Amsacrine isethionate induces Ca²⁺-mediated inactivation of ERK, and also downregulates AKT, promoting MCL1 downregulation mediated by GSK3β via reducing the phosphorylation level of GSK3β. Amsacrine isethionate induces Apoptosis by activating Caspase-9 and Caspase-3. Amsacrine isethionate blocks HERG potassium channels in the open/inactivated state. Amsacrine isethionate induces chromosomal aberrations and sister chromatid exchanges, and inhibits the synthesis of RNA and DNA. Amsacrine isethionate exhibits anti-leukemic activity. Amsacrine isethionate causes cardiac repolarization disorders, QT interval prolongation, ventricular arrhythmias, and increases the risk of sudden cardiac death. Amsacrine isethionate can be used in research related to acute myeloid leukemia, lymphoma and progressive malignancies.

NNRT-IN-10 is a potent, selective and orally active non-nucleoside HIV-1 reverse transcriptase (NNRTI) inhibitor with with an EC₅₀ values ranging from 1.16 to 18.3 nM for HIV and its mutant strains. NNRT-IN-10 exhibits good pharmacokinetic properties and favorable safety profiles. NNRT-IN-10 can be used for the study of AIDS, caused by HIV-1.

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

ML133 is a selective K_ir2 family channels inhibitor, with an IC₅₀ of 1.8 μM at pH 7.4 and 290 nM at pH 8.5.

Domiphen bromide (Standard) is the analytical standard of Domiphen bromide (HY-B1467). This product is intended for research and analytical applications. Domiphen bromide is a cationic active quaternary ammonium salt and also an inhibitor of HERG channels (IC₅₀: 9 nM), aminopeptidase-like enzymes, Escherichia coli alkaline phosphatase, and α-chymotrypsin. Domiphen bromide has multiple activities such as antibacterial, antimalarial, and disinfectant properties, and it is also a synergist of Colistin (HY-113678). Domiphen bromide can be used as a chemical preservative and a cationic surfactant, and it can also be used in the research of bacterial infectious diseases such as pharyngitis, thrush, and oral ulcers.

Quinine dihydrochloride is an orally active alkaloid extracted from cinchona bark, possessing various biological activities including antimalarial, antidengue virus (DENV), and anticancer properties. Quinine dihydrochloride is a potassium channel inhibitor that inhibits WT mouse Slo3 (K_Ca5.1) channel currents evoked by voltage pulses to +100 mV with an IC₅₀ of 169 μM.

IKs124 is KCNE2/KCNQ1 potassium channel blocker with the with an IC₅₀ of 8 nM. IKs124 can be used for study of peptic ulcers.

APD668 (Standard) is the analytical standard of APD668. This product is intended for research and analytical applications. APD668 is a potent, selective and orally active agonist of G-protein coupled receptor GPR119, with EC50s of 2.7 nM and 33 nM for hGPR119 and rGPR119, respectively. APD668 shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (Ki=0.1 μM). APD668 can be used for the research of steatohepatitis and diabetes.

Aprindine hydrochloride (Standard) is the analytical reference standard of Aprindine hydrochloride (HY-A0236A). This product is used for research and analytical applications. Aprindine hydrochloride is an Ib-class anti-arrhythmic agent. Aprindine hydrochloride mainly exerts its effect by blocking sodium channels (I_Na), thereby reducing the excitability and conduction velocity of cardiac muscle cells. Aprindine hydrochloride significantly inhibits delayed potassium currents, which helps to prolong the atrial effective refractory period (AERP) and inhibit the occurrence of atrial fibrillation. Aprindine hydrochloride can also regulate intracellular calcium ion concentration by inhibiting Na⁺/Ca²⁺ exchange current (INCX), thereby further stabilizing cardiac electrical activity. Aprindine hydrochloride can be used for the study of atrial fibrillation (AF) and ventricular arrhythmias.

Rosuvastatin Sodium (Standard) (ZD 4522 Sodium (Standard)) is the analytical standard of Rosuvastatin Sodium (HY-17504B). This product is intended for research and analytical applications. Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC₅₀ of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC₅₀ of 195 nM. Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.

BMS-394136 (compound 1) is a potent inhibitor of Kv 1.5, with an IC₅₀ of 0.05 μM. BMS-394136 is a selective IKur inhibitor. BMS-394136 dose-dependently prolongs atrial effective refractory period (AERP) and action potential duration (APD) without effecting ventricular effective refractory period (VERP). BMS-394136 can be used for acute atrial ischemia research.

SCH-23390 hydrochloride (Standard) is the analytical standard of SCH-23390 hydrochloride (HY-19545A). This product is intended for research and analytical applications. 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.

BRD7929 is an orally active phenylalanyl-tRNA synthetase (PheRS) inhibitor and parasiticide, with an IC₅₀ value of 0.023 μM against Plasmodium falciparum PheRS. BRD7929 inhibits the aminoacylation activity of the target enzyme, blocking protein synthesis, DNA replication and parasite nuclear division. BRD7929 clears the asexual blood stage, liver stage and mature gametocyte stage of malaria parasite species, and prevents parasite transmission to mosquitoes. BRD7929 shows moderate cytotoxicity against mammalian cells and inhibits hERG ion channels. BRD7929 achieves cure of malaria in animal models. BRD7929 can be used in research related to cryptosporidiosis and malaria.

Ketanserin (tartrate) (Standard) is the analytical standard of Ketanserin (tartrate). This product is intended for research and analytical applications. Ketanserin (R41468) tartrate is a selective 5-HT2 receptor antagonist. Ketanserin tartrate also blocks hERG current (IhERG) in a concentration-dependent manner (IC50=0.11 μM).

Norfluoxetine oxalate is the active metabolite of the antidepressant Fluoxetine (HY-B0102); it is also a TREK-2 K₂P potassium channel inhibitor. Norfluoxetine oxalate exhibits neuroimmunological activity, induces apoptosis in primary microglial cells, and inhibits the release of pro-inflammatory factors. Norfluoxetine oxalate inhibits high-threshold voltage-gated Ca²⁺ currents in neurons with an EC₅₀ of 20.4 μM. Norfluoxetine oxalate can be used in research related to depression, ischemic stroke, and epilepsy.

(2-Fluorophenyl) diphenylmethanol is a IKCa1 channel blocker with a K_d value of 700 nM. (2-Fluorophenyl) diphenylmethanol is used in the research of graft-versus-host disease and inflammatory diseases.

Quinine (hydrochloride dihydrate) (Standard) is the analytical standard of Quinine (hydrochloride dihydrate). This product is intended for research and analytical applications. Quinine hydrochloride dihydrate (Qualaquin) is an orally active and can be used in anti-malarial studies. Quinine hydrochloride dihydrate is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100?mV with an IC₅₀ of 169 μM.

UCL-1848 TFA is a hSK1 blocker with an IC₅₀ value of 1.1 nM. hSK1 is a small conductance calcium-activated potassium channel.

Ipravacaine (IQB-9302) is a long-acting amide-based local anesthetic. Ipravacaine blocks open-state hKv1.5, with stereoselective, time-dependent and voltage-dependent inhibitory effects, and exerts stronger activity on the R (+) enantiomer. Ipravacaine blocks Kv2.1, Kv4.3 and HERG potassium channels. Ipravacaine induces negative chronotropic effects, increases mean arterial pressure, and exhibits vasodilatory effects at high concentrations.