产品描述
Omidenepag isopropyl is converted to the active product Omidenepag during corneal penetration. Omidenepag isopropyl is a selective EP2 receptor agonist. Omidenepag isopropyl displays only a weak affinity for EP1, EP2, and FP receptors. Omidenepag isopropyl is under development for the treatment of glaucoma as intraocular pressure (IOP)-lowering drug.
体内活性
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]. Omidenepag isopropyl also displays 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. Omidenepag isopropyl at 0.0001%, 0.001%, or 0.01%, Xalatan, or vehicle was topically administered to one eye in ocular normotensive monkeys. IOP changes after drug administration were compared to the predosing baseline value established on day 1.?The significant decreases in IOP for 0.001% and 0.01% OMDI at time 0 of day 7. In ocular hypertensive monkeys finds that Omidenepag isopropyl lowers IOP by increasing both trabecular outflow facility and uveoscleral outflow[2].
Cas No.
1187451-19-9
分子式
C26H28N6O4S
分子量
520.6
别名
Omidenepag isopropyl
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years