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Tafluprost

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Chemical Structure| 209860-87-7 同义名 : AFP-168;MK2452;AFP-168, AFP-168, AFP-168, MK-2452, MK2452, MK 2452, Saflutan, Taflotan, Tapros, Zioptan
CAS号 : 209860-87-7
货号 : A451878
分子式 : C25H34F2O5
纯度 : 97%
分子量 : 452.531
MDL号 : MFCD08062150
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(552.45 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Tafluprost is an anti-glaucoma prostaglandin (PG) analog. Tafluprost showed significant IOP(intraocular pressure)-lowering effects without any safety concerns in patients with various types of glaucoma and OH (ocular hypertension) in daily clinical practice and tafluprost is highly effective in any therapeutic patterns[3]. Tafluprost lowers IOP (intraocular pressure) through the prostanoid FP receptor. A part of ocular hypotensive effect of tafluprost is attributed to FP receptor-mediated prostaglandin production acting through the prostanoid EP3 receptor[4]. Tafluprost not only lowers IOP, but may also enhance retinal blood flow in POAG (Primary open-angle glaucoma) patients with a normal IOP[5]. A significant increase of MOPP (mean ocular perfusion pressure) and a decrease of VD (vessel density) in the ONH (inside disc) in patients with initial glaucoma occurred within a week under the topical tafluprost or its FC (fixed combination)[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01434888 Healthy Volunteers Phase 1 Completed - Finland ... 展开 >> Kuopio University Hospital Eye Clinic Kuopio, Finland, 70200 收起 <<
NCT01654484 Glaucoma and Ocular Hypertensi... 展开 >>on 收起 << Phase 1 Phase 2 Completed - United States, California ... 展开 >> Santen Investigational Site Newport Beach, California, United States, 92663 United States, Florida Santen Investigational Site Deerfield Beach, Florida, United States, 33064 Santen Investigational Site Largo, Florida, United States, 33773 United States, Georgia Santen Investigational Site Morrow, Georgia, United States, 30260 Santen Investigational Site Roswell, Georgia, United States, 30076 United States, New York Santen Investigational Site Rochester, New York, United States, 14618 United States, Ohio Santen Investigational Site Cleveland, Ohio, United States, 44115 United States, Texas Santen Investigational Site Austin, Texas, United States, 78731 Santen Investigational Site Fort Worth, Texas, United States, 76102 Santen Investigational Site San Antonio, Texas, United States, 78240 收起 <<
NCT01927406 Thyroid Eye Disease ... 展开 >> Ocular Hypertension Glaucoma 收起 << Phase 4 Withdrawn(Funding source unava... 展开 >>ilable) 收起 << December 2016 United States, California ... 展开 >> Stanford Hospital and Clinics Stanford, California, United States, 94304 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.21mL

0.44mL

0.22mL

11.05mL

2.21mL

1.10mL

22.10mL

4.42mL

2.21mL
参考文献

[1]Kuwayama Y, Nomura A. Prospective observational post-marketing study of tafluprost for glaucoma and ocular hypertension: short-term efficacy and safety. Adv Ther. 2014 Apr;31(4):461-71.

[2]Kumagami T, Wakiyama H, et al. Comparison of corneal safety and intraocular pressure-lowering effect of tafluprost ophthalmic solution with other prostaglandin ophthalmic solutions. J Ocul Pharmacol Ther. 2014 May;30(4):340-5.

[3]Kuwayama Y, Nomura A. Prospective observational post-marketing study of tafluprost for glaucoma and ocular hypertension: short-term efficacy and safety. Adv Ther. 2014 Apr;31(4):461-71

[4]Ota T, Aihara M, Saeki T, Narumiya S, Araie M. The IOP-lowering effects and mechanism of action of tafluprost in prostanoid receptor-deficient mice. Br J Ophthalmol. 2007 May;91(5):673-6

[5]Weindler H, Spitzer MS, Schultheiß M, Kromer R. OCT angiography analysis of retinal vessel density in primary open-angle glaucoma with and without Tafluprost therapy. BMC Ophthalmol. 2020 Nov 12;20(1):444

[6]Kurysheva NI. Assessment of the optic nerve head, peripapillary, and macular microcirculation in the newly diagnosed patients with primary open-angle glaucoma treated with topical tafluprost and tafluprost/timolol fixed combination. Taiwan J Ophthalmol. 2019 Apr-Jun;9(2):93-99