| 货号 | 516821-480Well |
| 描述 | 17-phenyl trinor Prostaglandin F2α (17-phenyl trinor PGF2α) is a metabolically stable analog of PGF2α and is a potent agonist for the FP receptor. It binds to the FP receptor on ovine luteal cells with a relative potency of 756% compared to that of PGF2α.1 At the rat recombinant FP receptor expressed in CHO cells, 17-phenyl trinor PGF2α inhibits PGF2α binding with a Ki value of 1.1 nM.2 In human and animal models of glaucoma, FP receptor agonist activity corresponds very closely with intraocular hypotensive activity. 17-phenyl trinor PGF2α ethyl amide is an F-series prostaglandin analog which has been approved for use as an ocular hypotensive drug, sold under the Allergan trade name Bimatoprost.3 Whether 17-phenyl trinor PGF2α ethyl amide is a prodrug analogous to prostaglandin ester prodrugs such as latanoprost is currently controversial. There is some evidence that unmetabolized 17-phenyl trinor PGF2α is a weak FP receptor agonist.4 17-phenyl trinor PGF2α is converted by an amidase enzymatic activity in the bovine and human cornea to yield the corresponding free acid, with a conversion rate of about 40 µg/g corneal tissue/24 hours.5 Cayman’s 17-phenyl trinor PGF2α ELISA is a sensitive detection method for measuring both the free acid and ethyl amide forms of 17-phenyl trinor PGF2α. The assay is most appropriate for use when only one of the two forms is present. Samples containing mixtures of both the ethyl amide and free acid should be purified and the two compounds separated prior to ELISA analysis. |
| 别名 | Bimatoprost (free acid);17-phenyl trinor Prostaglandin F2α EIA Kit; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Balapure, A.K.,Rexroad, C.E., Jr.,Kawada, K., et al. Structural requirements for prostaglandin analog interaction with the ovine corpus luteum prostaglandin F2α receptor. Biochemical Pharmacology 38, 2375-2381 (1989). 2.Lake, S.,Gullberg, H.,Wahlqvist, J., et al. Cloning of the rat and human prostaglandin F2α receptors and the expression of the rat prostaglandin F2α receptor. FEBS Letters 355, 317-325 (1994). 3.Woodward, D.F.,Krauss, A.H.P.,Chen, J., et al. The pharmacology of Bimatoprost (Lumigan™). Survey of Ophthalmology 45, S337-S345 (2001). 4.Sharif, N.A.,Williams, G.W., and Kelly, C.R. Bimatoprost and its free acid are prostaglandin FP receptor agonists. European Journal of Pharmacology 432, 211-213 (2001). 5.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). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 稳定性 | ≥ 6 months |
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