62 products were found matching "K04259"!

Receptor for prostaglandin E2 (PGE2). The activity of this receptor is mediated by G(s) proteins that stimulate adenylate cyclase. The subsequent raise in intracellular cAMP is responsible for the relaxing effect of this receptor on smooth muscle.

Prostaglandin (PG) E2 exerts its actions by acting on a group of G-protein-coupled receptors (GPCRs). There are four GPCRs responding to PGE2 designated subtypes EP1, EP2, EP3, and EP4 and multiple splicing isoforms of the subtype EP3. The EP subtypes exhibit differences in signal transduction, tissue localization,...

Prostaglandin E2 (PGE2) evokes distinct responses through four different 'E prostanoid' (EP) receptors. EP2 is a G protein-coupled receptor which signals preferentially through Gs proteins. PF-04418948 is an orally active, potent, and selective EP2 receptor antagonist (IC50 = 16 nM). It is over a thousand-fold less...

Evatanepag is an agonist of prostaglandin E2 (PGE2) receptor subtype EP2. It induces cAMP accumulation in cells expressing rat EP2 (EC50 = 0. nM). Evatanepag (3 mg/kg) increases total bone area, mineral content, and mineral density in rat tibia.. Solulibility: DMSO: Sparingly soluble: 0.1-1 mg/ml: .

The biological effects of prostaglandin E2 (PGE2) are mediated through interaction with four distinct membrane-bound G-protein coupled EP receptors: EP1, EP2, EP3, and EP4. Binding of PGE2 to the EP2 receptor results in an increase in adenylate cyclase activity with a subsequent increase in cAMP. Pharmacologicially,...

TG6-10-1 is a potent antagonist of E prostanoid receptor 2 (EP2, Kb = 17.8 nM in C6 glioma cells overexpressing human EP2). It is 300-, 25-, and 10-fold selective for EP2 over other prostanoid receptors, including human EP3-4, FP and TP, and DP1 receptors, respectively. TG6-10-1 is also selective for EP2 over a...

CP 544,326 is a potent agonist of E prostanoid (EP) receptor 2 (IC50s = 10 and 15 nM for human and rat EP2, respectively). It is selective for EP2 over other EP receptors (IC50s = >3,200 nM for EP1, EP3, and EP4) and a panel of 37 G protein-coupled receptors (=30% inhibition at a concentration of 10 µM). CP 544,326...

Prostaglandin E2 (PGE2) evokes distinct responses through four different 'E prostanoid' (EP) receptors. EP2 is a G protein-coupled receptor that has diverse roles, including those in cancer, inflammation, and neuroprotection. TG4-155 is a brain penetrant EP2 antagonist (KB = 2.4 nM) that is over 1000-fold less...

tetranor-Misoprostol is a metabolite of misoprostol (Cay-13820). It is formed when misoprostol undergoes rapid de-esterification to form misoprostol (free acid) (Cay-13821), which is further metabolized to form the more polar tetranor-misoprostol in rats, dogs, and monkeys.Formal Name:...

Prostaglandin E2 (PGE2, Cay-14010) evokes distinct responses through four different 'E prostanoid' (EP) receptors. EP2 is a G protein-coupled receptor that has diverse roles, including those in cancer, inflammation, and neuroprotection. TG6-129 is an antagonist of the EP2 receptor, suppressing PGE2-induced elevation...

TG11-77 is a brain-permeable antagonist of the prostaglandin E2 (PGE2) receptor subtype EP2 (KB = 9.7 nM). It is selective for EP2 over DP1, EP4, and IP receptors (KBs = 7,320, 5,300, and >10,000 nM, respectively). TG11-77 (0.3 and 1 µM) inhibits the expression of genes encoding COX-2, IL-1beta, and IL-6 induced by...