Bioactivity | Taprenepag (CP-544326) is a potent and selective prostaglandin EP(2) agonist with IC50s of 10 and 15 nM for human and rat EP2, respectively. Taprenepag shows selectivity for EP2 over other EP receptors (IC50s>3200 nM for EP1, EP3, and EP4) and a panel of 37 G protein-coupled receptors[1]. | ||||||||||||
Invitro | Taprenepag (CP-544326) (0.01-1000 nM) increases cAMP levels in HEK293 cells expressing human EP2 (EC50=2.8 nM). Taprenepag has poor corneal permeability in an ex vivo rabbit corneal model[1]. | ||||||||||||
Name | Taprenepag | ||||||||||||
CAS | 752187-80-7 | ||||||||||||
Formula | C24H22N4O5S | ||||||||||||
Molar Mass | 478.52 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Prasanna G, et al. Effect of PF-04217329 a prodrug of a selective prostaglandin EP(2) agonist on intraocular pressure inpreclinical models of glaucoma. Exp Eye Res. 2011 Sep;93(3):256-64. |