PGN-9856 is a novel potent, selective prostaglandin EP2 receptor agonist. PGN-9856 exhibits high affinity for the EP₂ receptor, with a pKᵢ value of 8.6, and demonstrates full agonist activity, achieving a pEC₅₀ of 8.4 in functional assays. Notably, PGN-9856 shows exceptional selectivity, displaying minimal activity at other prostanoid receptors, including EP₄, and across a range of 45 receptors, 4 ion channels, 2 transporters, and 2 kinases. In vivo studies have highlighted PGN-9856's potent ocular hypotensive effects. Its isopropyl ester prodrug, JV-GL1, significantly reduces intraocular pressure (IOP) in Cynomolgus monkeys, with a single dose maintaining lowered IOP for an unprecedented duration of 5 to 10 days.
MedKoo Cat#: 414895
Name: PGN-9856
CAS#: 863704-91-0
Chemical Formula: C21H15F2NO4
Exact Mass: 383.0969
Molecular Weight: 383.35
Elemental Analysis: C, 65.80; H, 3.94; F, 9.91; N, 3.65; O, 16.69
The following data is based on the product molecular weight 383.35 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
