Tafluprost ethyl amide is derived from 17-phenyl trinor Prostaglandin F2a(17-phenyl trinor PGF2a). A number of 17-phenyl trinor PGF2a derivatives have been approved for the treatment of glaucoma.{8941,8322,8839,9311} Of these, the ones wherein the 13,14-double bond has been hydrogenated retain relatively good potency, but show a significantly reduced incidence of local irritant side effects.{9736} Alternatively, it was recently reported that analogs incorporating a 15-deoxy-15,15-difluoro modification also had a favorable ophthalmic activity profile.{11598} Tafluprost is a 2-series, 16-phenoxy analog of PGF2a with the 15,15-difluoro substitution. As a free acid, Tafluprost is a very potent FP receptor agonist (Ki = 0.4 nM).{11598} Ethyl amides of PGs tend to increase lipid solubility, to improve uptake into tissues and to further lower the effective concentration.
25 mg
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Cayman Chemical
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