Activators & Inhibitors

Activity: TAAR1 antagonist . Function/Pharmacology: A novel selective trace amine associated receptor 1 (TAAR1) antagonist (IC50=28 nM at mouse TAAR1). A useful tool for probing the physiologic role of TAAR1. Chemical Name: N-(3-Ethoxy-phenyl)-4-pyrrolidin-1-yl-3-trifluoromethyl-benzamide

Activity: GPR18 agonist . Function/Pharmacology: Endogenous anti-inflammatory lipo-aminoacid1. Full agonist at GPR182,3. Induces macrophage apoptosis via GPR184 which may be a mechanism for its resolution of inflammation activity5. Chemical Name: N-(5Z,8Z,11Z,14Z-eicosatetraenoyl)glycine

Activity: L-type Ca channel blocker / MDR inhibitor . Function/Pharmacology: Nicardipine is a clinically useful L-type calcium blocker. Inhibitor of MDR.2 Chemical Name: 1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)methyl-2-[methyl(phenylmethyl)amino]-3,5-pyridinedicarboxylic acid methyl ester hydrochloride

Activity: L-type Ca channel blocker . Function/Pharmacology: L-type calcium channel blocker. Displays antiatherosclerotic effects and improves endothelium-mediated nitric oxide-dependent vasodilation. Displays neuroprotective activity in rat models. Orally active and cell permeable Chemical Name: 4-(4-Benzofurazanyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic acid, methyl, 1-methylester diester

Activity: cellular calcium sponge . Function/Pharmacology: BAPTA-AM is a selective cell permeable Ca2+ chelator. It is a widely used intracellular calcium sponge1,2. Rapidly taken up by cells where it is irreversibly hydrolyzed to BAPTA by intracellular esterases. Pretreatment of cells with BAPTA-AM inhibits thapsigargin-induced responses3. Chemical Name: 1,2-bis-(2-Aminophenoxy)ethane-N,N,N’,N’-tetraacetic acid, tetraacetoxymethyl ester

Activity: Extracellular calcium sponge . Function/Pharmacology: BAPTA is a selective extracellular Ca2+ chelator. It is a widely used calcium sponge for chelating Ca2+outside of intact cells.1 It’s a useful tool to probe the involvement of extracellular Ca2+ in cellular signaling.2,3 Non-cell-permeable. Chemical Name: 1,2-bis-(2-Aminophenoxy)ethane-N,N,N’,N,-tetraacetic acid

Activity: Inhibits IP3-mediated Ca2+ release . Function/Pharmacology: A potent and reversible inhibitor of IP3-mediated Ca2+ release, IC50 = 358 nM1. Experiments with guinea-pig ileum permeabilized with alpha toxin revealed that Xestospongin C inhibits the IP3 receptor but not the ryanodine receptor in SR membranes. In intact smooth muscle cells it inhibits voltage-dependent Ca2+ and K+ currents at a concentration range similar to that at which it inhibits the IP3 receptor. It is a useful tool for probing the involvement of IP3 receptors in cellular signaling3. Cell permeable. Chemical Name: Natural product isolated from the marine sponge Xestospongia sp.

Activity: L-type Ca channel blocker . Function/Pharmacology: Anti-hypertensive L-type calcium channel blocker, which also benefits the cardiovascular system by stimulating nitric oxide synthase, inhibiting angiotension-induced oxidative stress and cardiovascular injury, and inhibiting monocyte/endothelial adhesion. Amlodipine also has a longer duration of action as compared to other similar calcium channel blockers. Chemical Name: null

Activity: Soluble guanylyl cyclase inhibitor . Function/Pharmacology: A potent and selective inhibitor of soluble guanylyl cyclase (sGC), IC50 = 20 nM).1 ODQ acts via competition with NO for the heme site of sGC where it binds irreversibly.2 ODQ does not inhibit NO-mediated macrophage toxicity, an activity that is unrelated to cGMP nor does it inhibit particulate GC.1 ODQ is an extremely useful tool to explore the involvement of the NO-cGMP pathway in cellular signaling and physiologic processes.3-5 Chemical Name: 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one