Activators & Inhibitors

Activity: Prostanoid EP antagonist . Function/Pharmacology: Selective PGE2 receptor (EP1) antagonist. At concentrations higher than 10 µM PGD2 and TXA2 receptors are also blocked. Chemical Name: 6-Isopropoxy-9-xanthone-2-carboxylic acid

Activity: DAG Lipase inhibitor . Function/Pharmacology: Inhibits DAG Lipase activity in a variety of cell types and tissues, including canine platelets, bovine adrenal chromaffin cells, human adrenal glomerulosa cells, rat thyroid lobes and pancreatic minilobules. IC50 in canine platelets is 4 µM1. Chemical Name: 1,6-bis(Cyclohexyloximinocarbonyl-amino)hexane

Activity: CysLT1 antagonist . Function/Pharmacology: LY-171883 is a selective and orally active leukotriene D4 (LTD4) antagonist (Ki = 0.63 µM).1 It is also an activator of peroxisome proliferator-activated receptors (PPAR’s).2,3 Chemical Name: 1-[2-Hydroxy-3-propyl-4-[4-1H-tetrazol-5-yl)butoxy]phenyl]ethanone

Activity: Glucocorticoid antagonist . Function/Pharmacology: Mifepristone is a cell-permeable steroid that is a potent antagonist at the progesterone and glucocorticoid receptors.1 It is used clinically as an abortifacient. KD progesterone receptor = 2.6 nM2 and KD glucocorticoid receptor = 0.4 nM3. Chemical Name: 11β-[4-(Dimethylamino)phenyl]-17β-hydroxy-17-(1-propynyl)estra-4,9-dien-3-one

Activity: IKK-2 inhibitor . Function/Pharmacology: Reversible, competitive inhibitor of IKK2 (IC50 = 11.2 µM). Has not been demonstrated to inhibit other IKK isoforms, or other kinases. Displays dose-dependent inhibition of the transcription of NK-κB dependent genes in cell culture1. Chemical Name: 5-(Thien-3-yl)-3-aminothiophene-2-carboxamide

Activity: TRPA1 blocker . Function/Pharmacology: TRPA1 antagonist. Active in rat models.1 Cell permeable Chemical Name: (1E,3E)-1-(4-Fluorophenyl)-2-methylpent-1-en-3-one oxime

Activity: PDE3 inhibitor . Function/Pharmacology: Ro 13-6438 is a selective inhibitor of phosphodiesterase III (PDE III, IC50 = 0.6 µM). Chemical Name: (R)-6-Chloro-1,5-dihydro-3-methylimidazo[2,1-b]quinazolin-2-one

Activity: Antioxidant/SIRT1 activator . Function/Pharmacology: Naturally occurring phenolic antioxidant. Displays antitumor and antiplatelet effects1. Activates SIRT1 and increases longevity in yeast2. Ameliorates ageing-related phenotypes by inhibition of cAMP phosphodiesterases3. Chemical Name: 3,4’,5-Trihydroxy-trans-stilbene

Activity: CB1 antagonist . Function/Pharmacology: Rimonabant is a selective CB1 receptor inverse agonist (Ki = 1.8 nM).1,2 It is an anorectic antiobesity drug originally approved for use in Europe but eventually withdrawn from the market because of potential severe psychiatric side effects. Chemical Name: 5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-piperidin-1-yl-1H-pyrazole-3-carboxamide