ikr

Nifekalant hydrochloride is an IKr potassium channel blocker with an IC50 of 10 µM. It is a Class III antiarrhythmic compound and can be used in the study of tachyarrhythmias.

Plasma kallikrein-IN-1 is a PKK inhibitor with an IC50 value of 0.5 nM.

Plasma kallikrein-IN-3, a potent inhibitor ( IC 50 : 0.15 μM) of plasma kallikrein, finds application in research related to hereditary angioedema, diabetic macular edema, and diabetic retinopathy [1].

Kallikrein-IN-1 (Formula A) is an inhibitor of the kinin-releasing enzyme kallikrein.

Kallikrein-IN-2 (compound 1) is an inhibitor of the kinin-releasing enzyme Kallikrein.

Plasma kallikrein-IN-2, a potent inhibitor of plasma kallikrein (PKal) with an inhibitory concentration (IC) 50 value of 0.1 nM, is utilized in research targeting hereditary angioedema, diabetic macular edema, and diabetic retinopathy.

Kallikrein 5-IN-2 is a potent inhibitor of Kallikrein KLK5, exhibiting selectivity with a pIC50 value of 7.1. By inhibiting KLK5, it has the potential to normalize epidermal shedding, thereby reducing associated inflammation and itching.

Kallikrein is capable of forming the kallikrenase kalinin system (KKS) in plasma and tissues, producing bradykinin and kalin peptides , respectively [1] .

AZD-1305 is a novel anti-arrhythmic compound that primarily blocks the fast component of IKr, l-type calcium currents and intra-ward sodium currents in mammalian cells and ventricular cardiomyocytes and can be used in studies to reverse arrhythmias.

Dimethindene (Dimetindeno) is a selective antagonist of H1 receptor and blocks K+ current. Dimethindene exhibits antihistamine and anticholinergic effects.

Ranolazine dihydrochloride (Ranolazine 2HCl) , an antianginal agent, can treat arrhythmia via a novel mechanism of action (inhibition of the late phase of the inward sodium current), and do not affect blood pressure or heart rate.

Dofetilide (UK 68789) is a sulfonamide class III antiarrhythmic agent and potassium channel blocker. Dofetilide selectively blocks cardiac ion channels of the rapid component of the delayed rectifier potassium current Ikr. This antiarrhythmic agent prolongs cardiac action potential duration and effective refractory period due to delayed repolarization without affecting conduction velocity. This results in a normal sinus rhythm. Dofetilide is used in the treatment of atrial fibrillation and flutter.

Ranolazine (RS 43285-003) is a calcium uptake inhibitor via the sodium calcium channel, used to treat chronic angina. It affects the sodium-dependent calcium channels during myocardial ischemia in rabbits by altering the intracellular sodium level.

NS3623 is an activator of human ether-a-go-go-related gene (hERG) potassium channels with a dual mode of action, also acting as an inhibitor of hERG1 channels. It activates the IKr and Ito currents and exhibits an antiarrhythmic effect.

Sematilide hydrochloride (CK-1752) is a class III antiarrhythmic. It is a selectively delayed rectifier K+ current (IKr) channel blocker. It inhibits rapidly activating Ik in guinea pig atrial myocytes, resulting in the prolongation of refractoriness and action potential duration.

Sematilide is a blocker of selective IKr channel.

Almokalant is a class III antiarrhythmic drug, acts as a potassium channel blocker. And it inhibits a specific component (Ikr) of the time-dependent delayed rectifier K+ current.

Ersentilide, a benzamide derivative, functions as both a β1-adrenergic receptor antagonist and an Ikr blocker. It has demonstrated efficacy in animal models of cardiac arrhythmias.

Xamoterol hemifumarate is a potent and selective β1-adrenoceptor agonist.Xamoterol hemifumarate is a potential compound for the study of the relationship between cardiac arrhythmias and β1-adrenergic stimulation with IKr.

IDO1-IN-19 (Compound 17) is a potent IDO1 inhibitor with potential applications in cancer research.

Antiarrhythmic agent-1 (example I), functioning as an antiarrhythmic agent and an IKr potassium channel blocker (IC 50 <1 μM), effectively inhibits cardiac arrhythmias.

Azimilide Dihydrochloride (NE-10064 Dihydrochloride), a novel class III antiarrhythmic agent, blocks both the slowly activating (IKs) and rapidly activating (IKr) components of the delayed rectifier potassium current

PKCα (C2-4) inhibitor peptide is a specific antagonist to PKCα, preventing the α1A-adrenoreceptor agonist A-61603 [1] from inhibiting I_Kr.

Nifekalant (MS-551), a Class III antiarrhythmic agent, functions as an IKr potassium channel blocker with an IC50 of 10 μM. It is utilized in the research of rapid supraventricular arrhythmias.