Taprenepag (formerly known as CP-544326) is a potent and selective agonist of EP2 (prostaglandin EP receptor 2) with IC50 of 10 nM and EC50 of 2.8 nM. The compound, when dosed as the isopropyl ester prodrug PF-04217329, significantly increased both its ocular bioavailability and corneal permeability. In a clinical study involving patients with primary open angle glaucoma, PF-04217329 (Taprenepag isopropyl), a prodrug of CP-544326 (active acid metabolite), a potent and selective EP(2) receptor agonist, was successfully evaluated for its ocular hypotensive activity. In preclinical species, topical ocular dosing of PF-04217329 resulted in an elevation of cAMP in aqueous humor/iris-ciliary body, indicating in vivo activation of EP(2) target receptors. The treatment was well tolerated. CP-544326 was exposed to the eyes at doses higher than the EC(50) for the EP(2) receptor when PF-04217329 was applied topically. After administering PF-04217329 once daily, normotensive Dutch-belted rabbits, normotensive dogs, and laser-induced ocular hypertensive cynomolgus monkeys showed reductions in IOP of between 30 and 50% in single-day studies, and between 20 and 40% in multiple-day studies when compared to eyes that were dosed with a vehicle. One topical dose resulted in an IOP reduction that lasted for six to twenty-four hours straight. Finally, preclinical data collected thus far seem to favor PF-04217329's clinical development as a novel glaucoma treatment drug.

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.