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VK-II-86 is a carvedilol analogue lacking antagonist activity at β-adrenoceptors, effectively suppresses SOICR by directly reducing the open duration of the cardiac ryanodine receptor (RyR2).VK-II-86 exhibited >2,000-fold lower beta-AR binding affinity than carvedilol.VK-II-86 prevented stress-induced ventricular tachyarrhythmias in RyR2-mutant mice and did so more effectively when combined with either of the selective beta blockers metoprolol or bisoprolol.VK-II-86 prevented hypokalaemia-induced AP prolongation and depolarization but did not alter AP parameters in normokalaemia.
T-Type calcium channel inhibitor is a potent inhibitor of T-Type calcium channel. T-Type calcium channel inhibitor penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished both for wild-type and mutant Cav3.1 channels. T-Type calcium channel inhibitor has the potential for the research of neurology disease.
MCU-i4 is a negative modulator of the mitochondrial calcium uniporter (MCU) complex that directly binds a specific cleft in MICU1 and decreases mitochondrial Ca2+ influx.,MCU-i4 decreases mitochondrial Ca2+ influx. Docking simulations reveal that MCU-i4 directly binds a specific cleft in MICU1, a key element of the MCU complex that controls channel gating. Accordingly, in MICU1-silenced or deleted cells, the inhibitory effect of MCU-i4 is lost. Moreover, MCU-i4 fails to inhibit mitochondrial Ca2+ uptake in cells expressing a MICU1 mutated in the critical amino acids that forge the predicted binding cleft.[1]
Azumolene (EU4093 free base), a Dantrolene analog, is a muscle relaxant. Azumolene is a ryanodine receptor (RyR) modulator and inhibits the calcium-release through ryanodine receptor. Azumolene can be used for malignant hyperthermia research.
SR33805 is a potent Ca2+ channel antagonist, with EC50s of 4.1 nM and 33 nM in depolarized and polarized conditions, respectively. SR33805 blocks L-type but not T-type Ca2+ channels. SR33805 can be used for the research of acute or chronic failing hearts.
NSC-609249 hydrochloride is an impurity of Verapamil. Verapamil is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor.
CDN1163 (CDN-1163) is a small molecule, allosteric activator of SERCA2, dose-dependently increases the Vmax of SERCA2 Ca2+-ATPase activity in ER microsomes; increases Ca2+-ATPase activity and significantly enhances Ca2+ uptake into the ER, attenuates H2O2-stimulated cell death in HEK cells; improves glucose homeostasis and metabolic parameters, increases glucose tolerance in ob/ob mice; CDN1163 reduces lipid accumulation and decreases lipogenesis in obese mice livers.
TTA-Q6 is a potent, selective T-type Ca2+ channel antagonist with IC50 of 14 nM and 590 nM in FLIPR depolarized assaay and FLIPR hyperpolarized assay, respectively.
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