Taprenepag, also known as CP-544326, is a potent and selective EP(2) receptor agonist, with IC50 values of 10 and 15 nM for human and rat EP2, respectively. Taprenepag (CP-544326) increases cAMP levels in HEK293 cells expressing human EP2 (EC50=2.8 nM). Taprenepag is the active metabolite of PF-04217329.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO 90 mg/mL|
Effect of PF-04217329 a prodrug of a selective prostaglandin EP(2) agonist on intraocular pressure in preclinical models of glaucoma
Ganesh Prasanna, et al. Exp Eye Res. 2011 Sep;93(3):256-64. PMID: 21376717.
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