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Taprenepag

Cat. No. M9854
Taprenepag Structure
Synonym:

CP-544326

Size Price Availability Quantity
5mg USD 125  USD125 In stock
10mg USD 190  USD190 In stock
25mg USD 400  USD400 In stock
50mg USD 620  USD620 In stock
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Quality Control & Documentation
Biological Activity

Taprenepag (CP-544326) is a potent selective prostagenin EP(2) agonist with IC50 of 10 and 15 nM for human and rat EP2, respectively. Taprenepag has higher selectivity for EP2 than other EP receptors (IC50>3200 nM for EP1, EP3 and EP4) and a group of 37 G-protein-coupled receptors.

Chemical Information
Molecular Weight 478.52
Formula C24H22N4O5S
CAS Number 752187-80-7
Solubility (25°C) DMSO 90 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] Ganesh Prasanna, et al. Exp Eye Res. 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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