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Travoprost

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Chemical Structure| 157283-68-6 同义名 : Fluprostenol isopropyl ester;AL6221;Travoprost, AL-6221, Travatan, Travoprostin;Travoprostum;Flu-Ipr
CAS号 : 157283-68-6
货号 : A465015
分子式 : C26H35F3O6
纯度 : 99%+
分子量 : 500.548
MDL号 : MFCD03411995
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 40 mg/mL(79.91 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

无水乙醇: 60 mg/mL(119.87 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
动物实验配方：
生物活性
描述 Prostaglandin (PG) F(2α) is widely distributed in various organs and exhibits various biological functions, such as luteolysis, parturition, aqueous humor homeostasis, vasoconstriction, rennin secretion, pulmonary fibrosis[3]. Travoprost, a highly selective and potent analogue of the prostaglandin PGF(2α), has recently been approved and marketed as a topical ocular hypotensive agent for the treatment of ocular hypertension and glaucoma [4]. Travoprost produces a lower incidence of ocular irritation than PGF20 isopropyl ester at a dose of 1 μg in the New Zealand albino (NZA) rabbit. Topical ocular application of Travoprost produces a marked miotic effect in cats following doses of 0. 01, 0. 03 and 0.1 μg. In the ocular hypertensive monkey, b.i.d. application of 0.1 and 0.3 μg of travoprost afforded peak reduction in intraocular pressure (IOP) of 22.7% and 28.6%, respectively. Topical application of travoprost was well tolerated in rabbits, cats and monkeys, causing no ocular irritation or discomfort at doses up to 1 μg[5]. As assessed with YO-PRO-1 and Hoechst 33342 relative to cell viability determined with NR or AB, travoprost/timolol PQ produced significantly less apoptosis than travoprost/timolol BAK and latanoprost/timolol BAK and their respective BAK concentrations alone (P<0. 0001 for all) [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
NCT00767481 Glaucoma Ocul... 展开 >>ar Hypertension 收起 << Phase 3 Terminated(Project Cancelled) - Mexico ... 展开 >> Mexico City, Mexico, 6700 收起 <<
NCT01253902 Glaucoma, Open-Angle ... 展开 >> Ocular Hypertension 收起 << Phase 4 Completed - United States, Arkansas ... 展开 >> Rogers, Arkansas, United States Canada, Alberta Calgary, Alberta, Canada 收起 <<
NCT01253902 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.00mL

0.40mL

0.20mL

9.99mL

2.00mL

1.00mL

19.98mL

4.00mL

2.00mL
参考文献

[1]Berdahl J, Voskanyan L, et al. Implantation of two second-generation trabecular micro-bypass stents and topical travoprost in open-angle glaucoma not controlled on two preoperative medications: 18-month follow-up. Clin Exp Ophthalmol. 2017 Nov;45(8):797-802.

[2]Kiddee W, Atthavuttisilp S. The effects of selective laser trabeculoplasty and travoprost on circadian intraocular pressure fluctuations: A randomized clinical trial. Medicine (Baltimore). 2017 Feb;96(6):e6047.

[3]Kikuko Watanabe. Recent reports about enzymes related to the synthesis of prostaglandin (PG) F(2) (PGF(2α) and 9α, 11β-PGF(2)). J Biochem. 2011 Dec;150(6):593-6.

[4]Jess T Whitson. Travoprost--a new prostaglandin analogue for the treatment of glaucoma. Expert Opin Pharmacother. 2002 Jul;3(7):965-77.

[5] M R Hellberg, et al. Preclinical efficacy of travoprost, a potent and selective FP prostaglandin receptor agonist. J Ocul Pharmacol Ther. 2001 Oct;17(5):421-32.

[6]Françoise Brignole-Baudouin, Luisa Riancho,et al. In vitro comparative toxicology of polyquad-preserved and benzalkonium chloride-preserved travoprost/timolol fixed combination and latanoprost/timolol fixed combination. J Ocul Pharmacol Ther. 2011 Jun;27(3):273-80.