SKF-96365 | TRPC channel blocker

SKF-96365 (130495-35-1) is an inhibitor of receptor-mediated calcium entry (RMCE) with IC₅₀'s of 8.5 μM for ADP stimulated platelets and 11.7 μM for thrombin stimulated platelets. Also inhibits Voltage-gated Ca²⁺ but not ATP-gated Ca²⁺ entry.¹ It has also been shown to block transient receptor potential canonical type (TRPC) channels², high-voltage-activated (HVA) L-type channels¹, K channels³, sarcoplasmic reticulum Ca-ATPase⁴ and voltage-gated sodium channels⁵. SKF-96365 is a potent blocker of LVA T-type Ca channels, in particular Ca(V)3.1 (IC₅₀ = 0.56 μM).⁶

References/Citations
1) Merritt et al.,(1990) SKF96365, a novel inhibitor of receptor-mediated calcium entry; Biochem. J. 271 515
2) Kiselyov et al., (1998) Functional interaction between InsP3 receptors and store-operated Htrp3 channels; Nature, 396 478
3) Schwarz et al., (1994) Multiple effects of SKF96365 on ionic currents and intracellular calcium in human endothelial cells; Cell Calcium, 15 45
4) Mason et al., (1993) Inhibition of Ca2+ transport pathways in thymic lymphocytes by econazole, miconazole and SKF96365; Am. J. Physiol., 264 C654
5) Hong et al. (1994) Inhibition of the sodium channel by SKF96365, an inhibitor of the receptor-operated calcium channel, in mouse diaphragm; J. Biomed. Sci., 1 172
6) Singh et al.,(2010) The transient receptor potential channel antagonist SKF96365 is a potent blocker of low-voltage-activated T-type calcium channels; Br. J. Pharmacol., 160 1464