| Identification | Back Directory | [Name]
PF-4217329 | [CAS]
1005549-94-9 | [Synonyms]
PF-4217329
Taprenepag isopropyl
PF-04217329 >=98% (HPLC)
Taprenepag isopropyl (PF-04217329)
isopropyl 2-(3-((N-(4-(1H-pyrazol-1-yl)benzyl)pyridine-3-sulfonamido)methyl)phenoxy)acetate(WXG02470)
Acetic acid, 2-[3-[[[[4-(1H-pyrazol-1-yl)phenyl]methyl](3-pyridinylsulfonyl)amino]methyl]phenoxy]-, 1-methylethyl ester | [Molecular Formula]
C27H28N4O5S | [MDL Number]
MFCD30532772 | [MOL File]
1005549-94-9.mol | [Molecular Weight]
520.6 |
| Chemical Properties | Back Directory | [Boiling point ]
690.0±65.0 °C(Predicted) | [density ]
1.26±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
2.30±0.11(Predicted) | [color ]
White to off-white | [InChI]
1S/C27H28N4O5S/c1-21(2)36-27(32)20-35-25-7-3-6-23(16-25)19-30(37(33,34)26-8-4-13-28-17-26)18-22-9-11-24(12-10-22)31-15-5-14-29-31/h3-17,21H,18-20H2,1-2H3 | [InChIKey]
NVPXUFQLKWKBHK-UHFFFAOYSA-N | [SMILES]
O=S(N(CC1=CC=C(N2N=CC=C2)C=C1)CC3=CC=CC(OCC(OC(C)C)=O)=C3)(C4=CC=CN=C4)=O |
| Hazard Information | Back Directory | [Uses]
Taprenepag isopropyl is a highly selective EP2 receptor agonist. | [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). | [in vivo]
Taprenepag isopropyl is a highly selective EP2 receptor agonist. Intraocular pressure (IOP) in the left, vehicle-dosed eye typically remains within the normal range. In the right (Taprenepag isopropyl-dosed) eye, IOP is reduced in all dose groups. In the high-dose group, IOP is reduced to the extent that it cannot be measured (<4mm Hg) on Days 22 and 29. There are no clinical signs or changes in body weight observed with any dose of Taprenepag isopropyl administration, and no
ocular findings occur for animals in the low-dose group (0.75 mg/day)[1]. | [IC 50]
EP2 | [References]
[1] Yanochko GM, et al. Investigation of ocular events associated with taprenepag isopropyl, a topical EP2 agonist in development for treatment of glaucoma. J Ocul Pharmacol Ther. 2014 Jun;30(5):429-39. DOI:10.1089/jop.2013.0222 |
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