Activators & Inhibitors

Activity: TRP blocker . Function/Pharmacology: An IP3 receptor antagonist (IC50=42 μM).1 Inhibits store-operated Ca2+ channels at high concentrations (50 μM) but stimulates at low concs. (<10 μM).2 Modulates TRP channels, blocking TRPC1, TRPC3, TRPC5, TRPC6, TRPV6, TRPM3, TRPM7, TRPM8, TRPP2 and at higher concentrations, activating TRPV1, TRPV2, TRPV3.3,4 Also inhibits selected GAP junction subtypes.5 Chemical Name: 2-Aminoethoxydiphenyl borate

Activity: Herg channel blocker . Function/Pharmacology: Selective hERG potassium channel blocker. Inhibits the rapid delayed-rectifier K+ current (IKr). Class III antiarrhythmic agent. Cell permeable. Chemical Name: N-[4-[[1-[2-(6-Methyl-3-pyridinyl)ethyl]-4-piperidinyl]carbonyl]phenyl]methanesulfonamide dihydrochloride dihydrate

Activity: KATP channel opener . Function/Pharmacology: Minoxidil is a direct antihypertensive peripheral vasodilator acting via activation of KATP channels leading to relaxation of smooth muscle.1 Active metabolite is Minoxidil sulfate (IC50 = 0.14 µM). Mainly used as a treatment for alopecia because of its observed hair regrowth ability.2 Chemical Name: 6-Piperidine-1-ylpyrimidine-2,4-diamine 3-oxide

Activity: L-type Ca channel blocker . Function/Pharmacology: L-type calcium channel blocker (IC50 = 75 nM), which can also inhibit T-type calcium channels at higher concentrations (IC50 = 244 nM). Novel inhibitor of drug transport by p-glycoprotein. Chemical Name: null

Activity: L-type Ca channel blocker . Function/Pharmacology: Nitrendipine is a clinically useful L-type calcium blocker. Chemical Name: 2,6-Dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid ethyl methyl ester

Activity: TRPV1 blocker . Function/Pharmacology: SB-366791 is a potent (IC50 = 0.7 µM) and selective TRPV1 antagonist.1,2 Selective for TRPV1 in a panel of 47 different binding assays. Chemical Name: 3-(4-Chlorophenyl)-N-(3-methoxyphenyl)-2-propenamide

Activity: PDE2 inhibitor . Function/Pharmacology: Potent and selective phosphodiesterase (PDE3) inhibitor, IC50=36 nM).1 Inhibits platelet production by disrupting megakaryocyte maturation2 via a mechanism which is independent of PDE3 inhibition3. Clinically useful agent for conditions requiring platelet lowering therapy.4,5 Chemical Name: 6,7-dichloro-1,5-dihydroimidazo[2,1 –b]quinazolin-2(3H)-one hydrochloride

Activity: PDE5 inhibitor . Function/Pharmacology: Potent and selective phosphodiesterase (PDE5) inhibitor, IC50=4 nM).1-3 Clinically useful agent for male erectile disfunction4 and pulmonary hypertension5. Chemical Name: 1-[[3-(4,7-Dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-ethoxyphenyl]sulfonyl]-4-methylpiperazine citrate

Activity: HMG-CoA reductase inhibitor . Function/Pharmacology: Blocks cholesterol and isoprenoid biosynthesis via inhibition of HMG-CoA reductase (Ki=1nM for acid form).1,2 Induces apoptosis in various cell lines.3 Causes cell cycle arrest in early G1 phase.4 Clinically useful antihyperlipemic agent.5 Cell permeable Chemical Name: 2-Methyl-1,2,3,7,8,8a-hexahydro-3,7-dimethyl-8-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1-naphthalenyl ester butanoic acid