Inwardly rectifying potassium channel Inhibitor

Talatisamine is an orally active cyclophilin D activator isolated from the roots of Aconitum carmichaeli Debx. Talatisamine exerts biological functions by activating cyclophilin D, inhibiting Ca²⁺-dependent opening of the mitochondrial permeability transition pore (mPTP) (IC₅₀=78 μM), and blocking delayed rectifier K⁺ channels (IC₅₀=146 μM). Talatisamine possesses both antioxidant and membrane-stabilizing properties, effectively inhibits lipid peroxidation and protects mitochondrial membrane function. Talatisamine exhibits multiple activities including antiarrhythmic, hypotensive, anti-inflammatory, anticancer and neuroprotective effects. Talatisamine finds applications in the research of ischemic diseases, rheumatoid arthritis, inflammation-related diseases and Alzheimer's disease.

Azimilide (NE-10064) dihydrochloride is a class III antiarrhythmic agent, which works by blocking potassium channels in the heart. Azimilide dihydrochloride is a dual blocker of I_Ks (IC₅₀ = 2.6 μM (2mM [K⁺]ₑ)) and I_Kr (IC₅₀ = 1 μM (4 mM [K⁺])). Azimilide dihydrochloride blocked HERG channel at 0.1 and 1 Hz with IC₅₀s of 1.4 μM and 5.2 μM respectively. Azimilide dihydrochloride also inhibits L-type calcium current (I_Ca) (IC₅₀ = 17.8 μM) and sodium current (I_Na) (IC₅₀ = 19 μM). Azimilide dihydrochloride can be used for the study of atrial fibrillation and ventricular fibrillation.

Azimilide (NE-10064) is a class III antiarrhythmic agent, which works by blocking potassium channels in the heart. Azimilide is a dual blocker of I_Ks (IC₅₀ = 2.6 μM (2mM [K⁺]ₑ)) and I_Kr (IC₅₀ = 1 μM (4 mM [K⁺])). Azimilide blocked HERG channel at 0.1 and 1 Hz with IC₅₀s of 1.4 μM and 5.2 μM respectively. Azimilide also inhibits L-type calcium current (I_Ca) (IC₅₀ = 17.8 μM) and sodium current (I_Na) (IC₅₀ = 19 μM). Azimilide can be used for the study of atrial fibrillation and ventricular fibrillation.

CPU-228 is a complex class III antiarrhythmic agent. CPU-228 concentration-dependently blocks the activities of the rapid component 50 of the delayed rectifier potassium channel (I_Kr) and the L-type calcium channel (I_Ca,L), with an IC₅₀ value of 0.909 μM for I_Ca,L current. CPU-228 produces negative inotropic effects and induces mild, non-frequency-dependent prolongation of the effective refractory period (ERP) in isolated left atria. CPU-228 reduces the incidence of torsades de pointes (TDP) in anesthetized rabbits and inhibits ischemia/reperfusion-induced arrhythmias in rats. CPU-228 can be used in studies related to torsades de pointes.

IDO1-IN-19 (Compound 17) is an orally active IDO1 inhibitor with an IC₅₀ of CYP2C9 of 8.64 μM. IDO1-IN-19 also acts funciton on cardiac channels, with IC₅₀s of 12 μM (IKr), 40 μM (INa), 8.3 μM (ICa), respectively. IDO1-IN-19 has the potential to study cancer diseases.

VU6080824 (Compound 5s), a derivative of ML-133 (HY-100230), is an inward-rectifier potassium channel (K_ir2.1) inhibitor with an IC₅₀ of 0.35  μM. VU6080824 has superior thallium flux and manual patch clamp (MPC) functional potency.

ROMK-IN-1 is an orally active inhibitor of ROMK (Kir1.1) with an IC₅₀ of 0.073 μM. ROMK-IN-1 exhibits no activity against Kir2.1, Kir4.1, Kir7.1, Nav1.5, Cav1.2, as well as the enzymes CYP3A4, CYP2D6, and CYP2C9. ROMK-IN-1 can be used in research related to hypertension.