| Identification | Back Directory | [Name]
Omidenepag Isopropyl | [CAS]
1187451-19-9 | [Synonyms]
OMDI
Omidenepag Isopropyl
Isopropyl (6-((N-(4-(1H-pyrazol-1-yl)benzyl)pyridine-3-sulfonamido)methyl)pyridin-2-yl)glycinate
Glycine, N-[6-[[[[4-(1H-pyrazol-1-yl)phenyl]methyl](3-pyridinylsulfonyl)amino]methyl]-2-pyridinyl]-, 1-methylethyl ester | [Molecular Formula]
C26H28N6O4S | [MDL Number]
MFCD32204454 | [MOL File]
1187451-19-9.mol | [Molecular Weight]
520.6 |
| Chemical Properties | Back Directory | [solubility ]
DMSO: Sparingly soluble: 1-10 mg/ml | [form ]
Solid | [color ]
White to off-white | [InChIKey]
VIQCWEGEHRBLAC-UHFFFAOYSA-N | [SMILES]
C(OC(C)C)(=O)CNC1=NC(CN(CC2=CC=C(N3C=CC=N3)C=C2)S(C2=CC=CN=C2)(=O)=O)=CC=C1 |
| Hazard Information | Back Directory | [Uses]
Omidenepag Isopropyl is a derivative of Omidenepag (O635205) which is a novel selective, non-prostanoid EP2 receptor agonist for the treatment of Glaucoma: | [in vivo]
Omidenepag isopropyl at 0.0001%, 0.001%, or 0.01%, Xalatan, or vehicle was topically administered to one eye in ocular normotensive monkeys. IOP change after drug administration was compared to the predosing baseline value established on day 1. Omidenepag isopropyl also shows significant and dose-dependent IOP-lowering effects at doses of 0.0001%, 0.001%, and 0.01% in ocular normotensive monkeys, with mean maximal IOP reductions of 2.4 ± 0.6, 7.6 ± 1.7, and 13.3 ± 1.2 mm Hg at each tested concentration, respectively. The significant decreases in IOP for 0.001% and 0.01% OMDI at time 0 of day 7. Omidenepag isopropyl is hydrolyzed in the eye to Omidenepag (OMD), an EP2 receptor agonist , with a significant ocular hypotensive effect in both ocular normotensive and hypertensive animal models[1].
In ocular hypertensive monkeys finds that Omidenepag isopropyl lowers IOP by increasing both trabecular outflow facility and uveoscleral outflow[2]. | [IC 50]
EP2 | [References]
[1] RYO IWAMURA*. Identification of a Selective, Non-Prostanoid EP2 Receptor Agonist for the Treatment of Glaucoma: Omidenepag and its Prodrug Omidenepag Isopropyl[J]. Journal of Medicinal Chemistry, 2018, 61 15: 6869-6891. DOI: 10.1021/acs.jmedchem.8b00808
[2] TOMOKO KIRIHARA. Pharmacologic Characterization of Omidenepag Isopropyl, a Novel Selective EP2 Receptor Agonist, as an Ocular Hypotensive Agent.[J]. Investigative ophthalmology & visual science, 2018, 59 1: 145-153. DOI: 10.1167/iovs.17-22745 |
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