Travoprost是一种前列腺素F2α类似物的合成酯类前药，可抑制IKir6.2/Sur2a离子通道，IC50值为3μM。
Cas No.:157283-68-6
Sample solution is provided at 25 µL, 10mM.
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Travoprost is a synthetic ester prodrug of a prostaglandin F2α analogue that inhibits IKir6.2/Sur2a ion channel with an IC50 value of 3μM [1]. Travoprost is hydrolyzed into the active FP prostaglandin receptor agonist by the cornea and sclera, improving trabecular outflow facility[2].Travoprost has been widely used as an eye drop to reduce intraocular pressure in vivo experiments[3].
In vitro, Travoprost treatment at 20µg/ml for 20min significantly inhibited the viability of primary human limbal epithelial cells (LECs) and inhibited cell proliferation[4]. 35µg/ml Travoprost treatment for 72 hours significantly inhibited CD31 and CD54 expression in conjunctiva-derived epithelial cells[5]. Aniridia limbal stromal cells (AN-LSCs) were treated with 0.313μg/ml Travoprost for 20 minutes, resulting in an increase in the MMP-9 protein level of the cells, and an elevation in the mRNA levels of PTGFR and JNK[6].
References:
[1] Friesacher T, Houtman M J C, Chen X, et al. Development of IKatp ion channel blockers targeting sulfonylurea resitant mutant KIR6. 2 based channels for treating DEND syndrome[J]. Biophysical Journal, 2022, 121(3): 388a.
[2] Toris C B, Zhan G, Fan S, et al. Effects of travoprost on aqueous humor dynamics in patients with elevated intraocular pressure[J]. Journal of glaucoma, 2007, 16(2): 189-195.
[3] Lim K S, Nau C B, O'Byrne M M, et al. Mechanism of action of Bimatoprost, Latanoprost, and Travoprost in healthy subjects: a crossover study[J]. Ophthalmology, 2008, 115(5): 790-795. e4.
[4] Li S, Stachon T, Liu S, et al. The effect of travoprost on primary human limbal epithelial cells and the siRNA-based aniridia limbal epithelial cell model, in vitro[J]. Plos one, 2025, 20(8): e0330492.
[5] Guenoun J M, Baudouin C, Rat P, et al. In vitro study of inflammatory potential and toxicity profile of latanoprost, travoprost, and bimatoprost in conjunctiva-derived epithelial cells[J]. Investigative ophthalmology & visual science, 2005, 46(7): 2444-2450.
[6] Li S, Stachon T, Liu S, et al. Increased sensitivity of primary aniridia limbal stromal cells to travoprost, leading to elevated migration and MMP-9 protein levels, in vitro[J]. PloS one, 2025, 20(6): e0326967.
Travoprost是一种前列腺素F2α类似物的合成酯类前药，可抑制IKir6.2/Sur2a离子通道，IC50值为3μM[1]。Travoprost在角膜和巩膜中水解为具有活性的FP前列腺素受体激动剂，从而改善小梁网途径的房水流出易度[2]。Travoprost在体内实验中已被广泛用作滴眼剂以降低眼压[3]。
在体外，使用20µg/ml的Travoprost处理20分钟，显著抑制了原代人角膜缘上皮细胞（LECs）的活力并抑制了细胞增殖[4]。使用35µg/ml的Travoprost处理72小时，显著抑制了结膜来源上皮细胞中CD31和CD54的表达[5]。使用0.313µg/ml的Travoprost处理无虹膜角膜缘基质细胞（AN-LSCs）20分钟，导致细胞中MMP-9蛋白水平升高，以及PTGFR和JNK的mRNA水平上升[6]。
| Cell experiment [1]: | |
Cell lines | Human limbal epithelial cells (LECs) |
Preparation Method | Human limbal epithelial cells (LECs) were seeded into individual wells of six-well culture plates, and 2.5ml of KGM3 medium was added to each well. After the cells reached complete confluence, the cells were digested using trypsin-EDTA and subsequently reseeded into 96-well plates. LECs were cultured at 37°C, 95% humidity, and 5% CO2 under standard culture conditions. The cells were treated with various concentrations of Travoprost (0.078, 0.156, 0.313, 0.625, 1.25, 2.5, 5, 10, 20, 40μg/ml) for 20min and analyzed for viability. |
Reaction Conditions | 0.078, 0.156, 0.313, 0.625, 1.25, 2.5, 5, 10, 20, 40μg/ml; 20min |
Applications | Travoprost treatment decreased the cell viability of LECs in a dose-dependent manner. |
References: | |
| Cas No. | 157283-68-6 | SDF | |
| 别名 | 曲伏前列素; Fluprostenol isopropyl ester; AL6221; Flu-Ipr | ||
| Canonical SMILES | O=C(OC(C)C)CCC/C=C\C[C@@H]1[C@@H](/C=C/[C@@H](O)COC2=CC=CC(C(F)(F)F)=C2)[C@H](O)C[C@@H]1O | ||
| 分子式 | C26H35F3O6 | 分子量 | 500.55 |
| 溶解度 | Ethanol: 60 mg/mL (119.87 mM); DMSO: ≥ 41.67 mg/mL (83.25 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9978 mL | 9.989 mL | 19.978 mL |
| 5 mM | 399.6 μL | 1.9978 mL | 3.9956 mL |
| 10 mM | 199.8 μL | 998.9 μL | 1.9978 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
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体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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- Purity: >98.00% Appearance: An oil
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