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PF-04217329

Cat. No. M8120
PF-04217329 Structure
Synonym:

PF-04217329

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Quality Control & Documentation
Biological Activity

PF-04217329 is a selective and potent prostaglandin EP2 receptor agonist. PF-04217329 is an ocular bioavailable isopropyl ester prodrug of CP-544326 (active acid metabolite).

Chemical Information
Molecular Weight 520.6
Formula C27H28N4O5S
CAS Number 1005549-94-9
Solubility (25°C) DMSO: 2 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

References

[1] Gina M Yanochko, et al. Investigation of ocular events associated with taprenepag isopropyl, a topical EP2 agonist in development for treatment of glaucoma

[2] Ronald A Schachar, et al. Subclinical increased anterior stromal reflectivity with topical taprenepag isopropyl

[3] Ronald A Schachar, et al. A phase 2, randomized, dose-response trial of taprenepag isopropyl (PF-04217329) versus latanoprost 0.005% in open-angle glaucoma and ocular hypertension

[4] Ganesh Prasanna, et al. Effect of PF-04217329 a prodrug of a selective prostaglandin EP(2) agonist on intraocular pressure in preclinical models of glaucoma

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