Potassium Channel Antagonist

VU0463271 is a selective KCC2 antagonist, with an IC₅₀ of 61 nM.

Mefloquine hydrochloride (Mefloquin hydrochloride), a quinoline antimalarial agent, is an anti-SARS-CoV-2 entry inhibitor. Mefloquine hydrochloride is also a K⁺ channel (KvQT1/minK) antagonist with an IC₅₀ of ~1 μM. Mefloquine hydrochloride can be used for malaria, systemic lupus erythematosus and cancer research.

Repaglinide is an insulin secretagogue for the treatment of type-2 diabetes mellitus.

Mefloquine (Mefloquin), an orally active and potent quinoline antimalarial agent, is an anti-SARS-CoV-2 entry inhibitor. Mefloquine is also a K⁺ channel (KvQT1/minK) antagonist with an IC₅₀ of ~1 μM. Mefloquine can be used for malaria, systemic lupus erythematosus and cancer research.

Amifampridine (3,4-Diaminopyridine) is an orally active, potent and cell permeable voltage-gated potassium (K_v) channel blocker (PCB). Amifampridine is efficacy in the reversal of BoNT/A (HY-P79153) intoxication. Amifampridine increases transmitter release from neuromuscular junctions (NMJs). Amifampridine can be used for Lambert-Eaton myasthenic syndrome (LEMS) research.

ML418 is a potent, selective and CNS penetrating Kir7.1 potassium channel blocker. ML418 inhibits Kir7.1 with an IC₅₀ value of 0.31 μM. ML418 can be used for the research of neurological, cardiovascular, endocrine and muscle disorders.

Mitiglinide Calcium (KAD-1229 anhydrous), an insulinotropic agent, is an ATP-sensitive K⁺ (K_ATP) channel antagonist. Mitiglinide Calcium is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell K_ATP channel). Mitiglinide Calcium can be used for the research of type 2 diabetes.

Penitrem A is an indole diterpene neurotoxic alkaloid produced by Penicillium, acts as a selective BK channel antagonist with antiproliferative and anti-invasive activities against multiple malignancies. Penitrem A increases the spontaneous release of endogenous glutamate, gamma-aminobutyric acid (GABA) and aspartate from cerebrocortical synaptosomes, and induces tremorgenic syndromes in animals.

Mitiglinide calcium hydrate (KAD-1229), an insulinotropic agent, is an ATP-sensitive K⁺ (K_ATP) channel antagonist. Mitiglinide calcium hydrate is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell K_ATP channel). Mitiglinide Calcium hydrate can be used for the research of type 2 diabetes.

Repaglinide (Standard) is the analytical standard of Repaglinide. This product is intended for research and analytical applications. Repaglinide is an insulin secretagogue for the treatment of type-2 diabetes mellitus.

PNU 37883 hydrochloride (PNU 37883A) is a selective vascular ATP-sensitive potassium (Kir6, K_ATP) channels blocker. PNU 37883 hydrochloride has diuretic effects with specific binding in kidney and vascular smooth muscle rather than in brain or pancreatic beta cells.

Tamapin TFA is a venom peptide, targeting to small conductance Ca(2+)-activated K(+) (SK) channels. Tamapin TFA is a selctive blocker of SK2 (Potassium Channel). Tamapin TFA inhibits SK channel-mediated currents in pyramidal neurons of the hippocampus. Tamapin TFA can be isolated from the Indian red scorpion (Mesobuthus tamulus).

VU0463271 quarterhydrate is a potent KCC2 antagonist, with an IC₅₀ of 61 nM.

KCNK13-IN-1 (example 71), a KCNK13 antagonist, is an anti-inflammatory agent, with an IC₅₀ of <200 nM for IL-1 β.

Amifampridine-d₃ (3,4-Diaminopyridine-d₃) is deuterium labeled Amifampridine. Amifampridine (3,4-Diaminopyridine) is an orally active, potent and cell permeable voltage-gated potassium (K_v) channel blocker (PCB). Amifampridine is efficacy in the reversal of BoNT/A (HY-P79153) intoxication. Amifampridine increases transmitter release from neuromuscular junctions (NMJs). Amifampridine can be used for Lambert-Eaton myasthenic syndrome (LEMS) research.

LY3972406 is an orally active, selective Kv1.3 antagonist. LY3972406 acts on chronically stimulated effector memory T cells without affecting naive central memory T cells. LY3972406 induces mild, non-adverse skin irritation in Rattus norvegicus. LY3972406 is applicable for the research of autoimmune diseases.

Mitiglinide (KAD-1229), an insulinotropic agent, is an ATP-sensitive K⁺ (K_ATP) channel antagonist. Mitiglinide is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell K_ATP channel). Mitiglinide can be used for the research of type 2 diabetes.

Amifampridine (3,4-Diaminopyridine) phosphate is an orally active, potent and cell permeable voltage-gated potassium (K_v) channel blocker (PCB). Amifampridine phosphate is efficacy in the reversal of BoNT/A (HY-P79153) intoxication. Amifampridine phosphate increases transmitter release from neuromuscular junctions (NMJs). Amifampridine phosphate can be used for Lambert-Eaton myasthenic syndrome (LEMS) research.

Prenylamine (lactate) (Standard) is the analytical standard of Prenylamine (lactate). This product is intended for research and analytical applications. Prenylamine lactate is a calcium-modulating protein (CaM) antagonist that inhibits CaM-dependent enzymes and can slowly relax smooth muscle preparations. The effect of Prenylamine lactate on smooth muscle is not inhibited by the calcium agonist Bay K 8644 (HY-10588). Reports suggest that under low heart rate conditions, Prenylamine seems to enhance voltage-dependent transmembrane calcium currents.

KNa1.1-IN-2 (Compound Z05) is a selective KNa1.1 channel inhibitor with blood-brain barrier penetration, particularly effective against the hERG channel. KNa1.1-IN-2 works by binding to the KNa1.1 channel and blocking the channel activity induced by Gain-of-function (GOF) mutations, effectively intervening in KCNT1-related epilepsy. Additionally, KNa1.1-IN-2 inhibits the GOF mutant Y796H. KNa1.1-IN-2 holds promise for research into KCNT1-related epilepsy disorders.