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DS16570511 is a cell-permeable inhibitor of the mitochondrial calcium uniporter (MCU) that inhibits serum-induced mitochondrial Ca2+ influx in HEK293A cells with IC50 of 7 uM; blocks the MCU- or MICU1-dependent increases of Ca2+ influx, blocks the Ca2+ uptake activity of the pig heart mitochondria with IC50 of 15 uM; also blocks mitochondrial Ca2+ overload in a Langendorff perfused beating rat heart, increases cardiac contractility without affecting heart rate in the perfused heart.




MK-8998 (CX-8998) is a potent and selective antagonist of the T-type calcium channel for the treatment of schizophrenia.; does not block D2, 5HT2a, muscarinic, or histaminic receptors; has the potential for a substantially improved side effect profile compared with currently available atypical antipsychotics.


Phase 2 Clinical



1256269-87-0 SAK3 (T-VGCC enhancer SAK3) is a potent, orally acitve enhancer of T-type voltage-gated Ca2+ channel (T-VGCC), enhances CaV3.1 and CaV3.3, but not CaV3.2 activity at concentrations of 0.01-10 nM in neuro2A cells in vitro; significantly enhanced acetylcholine (ACh) release in the hippocampal CA1 region of naïve mice (0.5 mg/kg, p.o.); significantly enhanced hippocampal ACh levels in olfactory-bulbectomized (OBX) mice, rescuing impaired memory-related behaviors.


BTT-369 (BTT369) is a voltage-gated CaV2.2 calcium channel inhibitor that disrupts the CaVα·CaVβ3 protein-protein interaction with Ki of 2.0 uM in FP assays; decreases trafficking of CaV2.2 channels to the plasma membrane and modulates the functions of the channel, suppresses pain responses in rodent neuropathic pain models; BTT-369 (BTT369) is a cell-permeable derivative of BTT-266.


BTT-266 (BTT266) is a voltage-gated CaV2.2 calcium channel inhibitor that disrupts the CaVα·CaVβ3 protein-protein interaction, directly binds to CaVβ3 with Kd of 3.6 uM; decreases surface presentation of the CaV2.2α1 subunit, significantly reduces trafficking of CaV2.2 to the plasma membrane at 50 uM, does not affect CaV2.2 currents in either in HEK-CaV2.2 cells or rat dorsal root ganglion (DRG) neurons.


892711-75-0 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.


120934-96-5 FPL64176 (ARC-64176) is a potent L-type Ca++ channel activator with EC50 of 16 nM; prolongs action potential duration and enhances contractility in guinea pig papillary muscle, induces contractile response with EC50 of 0.2 uM; produces biexponential tail current decays at -50 mV with fast and slow time constants of 4.30 +/- 0.30 and 44.52 +/- 4.56 msec, respectively; produces large increases in cardiac contractile force and diastolic blood pressure in anesthetized dogs (100 mg/kg, i.v.).

Heart Failure


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