货号 | 9000843-25mg |
描述 | Tafluprost ethyl amide is derived from 17-phenyl trinor Prostaglandin F2α(17-phenyl trinor PGF2α). A number of 17-phenyl trinor PGF2α derivatives have been approved for the treatment of glaucoma.1,2,3,4 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.5 Alternatively, it was recently reported that analogs incorporating a 15-deoxy-15,15-difluoro modification also had a favorable ophthalmic activity profile.6 Tafluprost is a 2-series, 16-phenoxy analog of PGF2α with the 15,15-difluoro substitution. As a free acid, Tafluprost is a very potent FP receptor agonist (Ki = 0.4 nM).6 Ethyl amides of PGs tend to increase lipid solubility, to improve uptake into tissues and to further lower the effective concentration. |
别名 | Dechloro Dehydroxy Difluoro Ethylcloprostenolamide; |
供应商 | Cayman |
应用文献 | |
1.Woodward, D.F.,Krauss, A.H.P.,Chen, J., et al. The pharmacology of Bimatoprost (Lumigan™). Survey of Ophthalmology 45, S337-S345 (2001). 2.Abramovitz, M.,Adam, M.,Boie, Y., et al. The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs. Biochimica et Biophysica Acta 1483, 285-293 (2000). 3.Sorbera, L.A. and Castañer, J. Travoprost. Drugs of the Future 25, 41-45 (2000). 4.Maxey, K.M.,Johnson, J.,Camras, C.B., et al. The hydrolysis of bimatoprost in corneal tissue generates a potent prostanoid FP receptor agonist. Survey of Ophthalmology 47(4), 34-40 (2002). 5.Resul, B.,Stjernschantz, J.,No, K., et al. Phenyl-substituted prostaglandins: Potent and selective antiglaucoma agents. Journal of Medicinal Chemistry 36, 243-248 (1993). 6.Nakajima, T.,Matsugi, T.,Goto, W., et al. New fluoroprostaglandin F2α derivatives with prostanoid FP-receptor agonistic activity as potent ocular-hypotensive agents. Biological and Pharmaceutical Bullentin 26(12), 1691-1695 (2003). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 437.5 |
分子式 | C24H33F2NO4 |
CAS号 | 1185851-52-8 |
稳定性 | ≥ 1 year |
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