Travoprost
(Synonyms: 曲伏前列素; Fluprostenol isopropyl ester; AL6221; Flu-Ipr) 目录号 : GC37822
A PGF2α analog and prodrug form of (+)-fluprostenol
Cas No.:157283-68-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Fluprostenol isopropyl ester is an analog of prostaglandin F2α and an isopropyl ester prodrug form of (+)-fluprostenol .1,2 Fluprostenol isopropyl ester is an FP receptor agonist, inducing phosphoinositide turnover in HEK293 cells expressing the human ocular FP receptor with an EC50 value of 40.2 nM.3 Topical application of fluprostenol isopropyl ester (0.01, 0.03, and 0.1 μg) induces miosis in conscious cats in a dose-dependent manner.2 It reduces intraocular pressure in a cynomolgus monkey model of ocular hypertension when administered topically at doses of 0.1 and 0.3 μg twice per day. Formulations containing fluprostenol isopropyl ester have been used in the treatment of open-angle glaucoma and ocular hypertension.
1.Sorbera, L.A., and Casta?er, J.TravoprostDrugs Future25(1)41-45(2000) 2.Hellberg, M.R., Sallee, V.L., McLaughlin, M.A., et al.Preclinical efficacy of travoprost, a potent and selective FP prostaglandin receptor agonistJ. Ocul. Pharmacol. Ther.17(5)421-432(2001) 3.Sharif, N.A., Kelly, C.R., Crider, J.Y., et al.Ocular hypotensive FP prostaglandin (PG) analogs: PG receptor subtype binding affinities and selectivities, and agonist potencies at FP and other PG receptors in cultured cellsJ. Ocul. Pharmacol. Ther.19(6)501-515(2003)
| 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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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 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 | 0.3996 mL | 1.9978 mL | 3.9956 mL |
| 10 mM | 0.1998 mL | 0.9989 mL | 1.9978 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Travoprost/timolol
Drugs Aging 2006;23(7):587-97; discussion 598-9.PMID:16930087DOI:10.2165/00002512-200623070-00005.
Travoprost 0.004%/timolol 0.5% fixed combination (Travoprost/timolol) is a once-daily eyedrops solution comprising the prostaglandin F(2alpha) analogue Travoprost and the beta-adrenoceptor antagonist timolol. It is indicated for the treatment of patients with open-angle glaucoma or ocular hypertension who are insufficiently responsive to topical beta-adrenoceptor antagonists or prostaglandin analogues. Once-daily Travoprost/timolol had generally similar efficacy to Travoprost plus timolol and was more effective than Travoprost or timolol monotherapy in reducing intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension in randomised, well designed studies. Both Travoprost/timolol and latanoprost plus timolol maintained IOP control, and Travoprost/timolol was shown to be noninferior to latanoprost/timolol in randomised, well designed studies. Travoprost/timolol was generally well tolerated, with a tolerability profile similar to those of Travoprost plus timolol, Travoprost or timolol monotherapy and latanoprost plus timolol. The majority of adverse events, such as ocular hyperaemia, were mild and resolved with or without treatment.
Travoprost
Drugs Aging 2002;19(6):465-71; discussion 472-3.PMID:12149052DOI:10.2165/00002512-200219060-00005.
Travoprost is a synthetic ester prodrug of a prostaglandin F(2alpha) analogue used in the treatment of open-angle glaucoma and ocular hypertension. Intraocular Travoprost 0.004% once daily was significantly more effective at reducing intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension than placebo or timolol 0.5% twice daily and was at least as effective as latanoprost 0.005% once daily in randomised, double-blind studies. When used as adjunctive therapy with timolol 0.5% twice daily in patients with elevated IOP not adequately controlled by timolol alone, Travoprost 0.004% showed significant additional IOP reduction in a randomised double-blind trial. Travoprost 0.004% was well tolerated in clinical trials. The majority of adverse events such as ocular hyperaemia and eyelash changes were mild and resolved without treatment.
Travoprost/timolol fixed combination
Expert Opin Pharmacother 2008 Apr;9(6):1059-65.PMID:18377347DOI:10.1517/14656566.9.6.1059.
Background: Travoprost and timolol are topical ocular hypotensive medications that have been used in the treatment of glaucoma. The fixed combination eye drop, Duotrav (Travoprost 0.004% and timolol maleate 0.5%), has recently been introduced into the market. Objective: In this paper, the results of clinical trials and existing data on the performance of Travoprost/timolol are discussed and analyzed. Methods: Appopriate studies for review were identified using PubMed. Studies selected for review compared efficacy and side-effect profile of fixed combination Travoprost/timolol with Travoprost and timolol used concomitantly, latanoprost and timolol used concomitantly, fixed combination latanoprost/timolol, Travoprost alone and timolol alone. Results/conclusion: Fixed combination eye drops such as Travoprost/timolol offer the potential benefits of increased patient adherence, reduced exposure to preservatives, and reduced cost.
Travoprost 0.004%/timolol 0.5% fixed combination
Drugs Today (Barc) 2007 Feb;43(2):77-83.PMID:17353945DOI:10.1358/dot.2007.43.2.1032058.
Fixed-combination Travoprost/timolol solution consists of Travoprost 0.004% and timolol 0.5%. Several studies have demonstrated the efficacy and safety of this medication used once daily for the treatment of open-angle glaucoma and ocular hypertension. This fixed combination has been compared to Travoprost and timolol used concomitantly, latanoprost and timolol used concomitantly, latanoprost/timolol fixed combination and Travoprost and timolol monotherapy. Fixed-combination medicines such as Travoprost/timolol offer the potential of maximizing patient adherence by decreasing the burden of using multiple topical agents that lower intraocular pressure, and by potentially decreasing the overall cost to both the patient and the health-care system. We discuss the benefits of fixed-dose medications, report on previous clinical trials and summarize the existing data on the performance of Travoprost/timolol.
Travoprost--a new prostaglandin analogue for the treatment of glaucoma
Expert Opin Pharmacother 2002 Jul;3(7):965-77.PMID:12083996DOI:10.1517/14656566.3.7.965.
Travoprost, a highly selective and potent analogue of the prostaglandin PGF(2)(alpha), has recently been approved and marketed as a topical ocular hypotensive agent for the treatment of ocular hypertension and glaucoma. Following absorption into the eye, the free acid form of Travoprost interacts with the endogenous FP prostanoid receptor to enhance aqueous humor outflow and lower intraocular pressure (IOP). Travoprost is distinguished from other marketed prostaglandin analogues in that it is a full agonist at the prostaglandin receptor. It is also highly selective with little or no affinity for other prostanoid or non-prostanoid receptors in the eye. Travoprost provides robust lowering of IOP with little diurnal fluctuation and results in low target pressures in a large percentage of patients. In controlled clinical trials, Travoprost 0.004% o.d. used as monotherapy produced greater IOP reduction than timolol 0.5% b.i.d. and equal or greater reduction than latanoprost 0.005%o.d. Travoprost 0.004% was also shown to be an effective adjunctive agent offering an additional 5 - 7 mmHg IOP reduction in patients inadequately controlled on timolol 0.5%. Subgroup analysis of a large Phase III trial revealed Travoprost 0.004% to be significantly more effective at lowering IOP in African American patients by almost 2 mmHg compared to non-African Americans. Moreover, a higher percentage of African American patients responded to Travoprost 0.004% and reached lower target pressures than with either latanoprost 0.005% or timolol 0.5%. Travoprost is a very stable compound, maintaining its efficacy following exposure to extremely low and high temperatures, repeated freezing and thawing and exposure to light. Throughout all clinical trials, Travoprost was found to be safe and well-tolerated with very few (< 5%) discontinuations due to adverse events. Travoprost 0.004% represents a clinically significant advance for the treatment of glaucoma and ocular hypertension, offering superior IOP reduction and diurnal control, especially among African American patients, in a safe, well-tolerated, stable formulation.