sk channel

Upacicalcet (AJT-240) is an intraventricular calcium mimetic, a SHPT available for human hemodialysis, that inhibits excessive parathyroid hormone (PTH) secretion by directly acting on parathyroid cell membrane calcium-sensitive receptors, thereby lowering blood levels of PTH.Upacicalcet is an orthosteric modulator of calcium-sensitive receptors and prevents adenine-induced secondary vascular calcification and bone disease in a rat model of adenine-induced secondary hyperparathyroidism.

ICA (N-[4-(2-Pyridinyl)-2-thiazolyl]-2-pyridinamine) is a SK channel inhibitor and exhibits antileishmanial activity (IC50: 2.1 µM).

Bisoprolol, a selective beta-1 adrenergic receptor antagonist, selectively and competitively binds to and blocks beta-1 adrenergic receptors in the heart, thereby with antihypertensive activity and devoid of intrinsic sympathomimetic activity.

NS8593 hydrochloride (NS8593 HCl) is a potent and selective inhibitor of small conductance Ca2+-activated K+ channels (SK channels) .

Bisoprolol is a cardioselective β1-adrenergic blocker used for secondary prevention of heart failure, myocardial, angina pectorisinfarction (MI) and mild to moderate hypertension.

UCL-1848 trifluoroacetate salt is a selective Ca2+-activated, SK potassium channel blocker.

AP14145 hydrochloride is a potent negative allosteric modulator of K Ca 2 (SK) channels, specifically targeting K Ca 2.2 (SK2) and K Ca 2.3 (SK3) channels with an IC 50 of 1.1 μM. Inhibition of AP14145 hydrochloride is highly influenced by S508 and A533 amino acids present in the channel. This compound effectively extends the atrial effective refractory period (AERP) in rats and exhibits antiarrhythmic properties in a Vernakalant-resistant porcine model of atrial fibrillation (AF).

Bupivacaine is a BK SK, Kv1, Kv3, TASK-2 K Channel and voltage-gated Na channel blocker used as an anesthetic. It maybe neurotoxic at high does, inducing apoptosis in neuroblastoma cells. It acts by binding to the intracellular portion of voltage-gated sodium channels and blocking sodium influx into nerve cells.

Tamapin, a venom peptide isolated from the Indian red scorpion (Mesobuthus tamulus) [1], selectively targets and blocks small-conductance Ca(2+)-activated K(+) (SK) channels, particularily SK2 (Potassium Channel). It inhibits SK channel-mediated currents in the pyramidal neurons of the hippocampus.

Tamapin TFA, a venom peptide isolated from the Indian red scorpion (Mesobuthus tamulus) [1], selectively targets and blocks small conductance Ca(2+)-activated K(+) (SK) channels, particularly the SK2 subtype (Potassium Channel). It is known to inhibit SK channel-mediated currents in the hippocampal pyramidal neurons.

Rimtuzalcap (CAD-1883) (CAD-1883), a pioneering selective positive allosteric modulator of small-conductance calcium-activated potassium channels (SK channels), is employed in the study of movement disorders such as spinocerebellar ataxia (SCA) and essential tremor (ET).