Tafluprost
(Synonyms: 他氟前列素; AFP-168; MK2452) 目录号 : GC37721
A 15,15-
Cas No.:209860-87-7
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
A number of 17-
1.Woodward, D.F., Krauss, A.H., Chen, J., et al.The pharmacology of bimatoprost (LumiganTM)Surv. Ophthalmol.45(Suppl 4)S337-S345(2001) 2.Abramovitz, M., Adam, M., Boie, Y., et al.The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogsBiochim. Biophys. Acta1483(2)285-293(2000) 3.Sorbera, L.A., and Casta?er, J.TravoprostDrugs Future25(1)41-45(2000) 4.Maxey, K.M., Johnson, J., and LaBrecque, J.The hydrolysis of bimatoprost in corneal tissue generates a potent prostanoid FP receptor agonistSurv. Ophthalmol.47(Suppl 1)S34-S40(2002) 5.Resul, B., Stjernschantz, J., No, K., et al.Phenyl-substituted prostaglandins: Potent and selective antiglaucoma agentsJ. Med. Chem.36243-248(1993) 6.Nakajima, T., Matsugi, T., Goto, W., et al.New fluoroprostaglandin F2α derivatives with prostanoid FP-receptor agonistic activity as potent ocular-hypotensive agentsBiol. Pharm. Bull.26(12)1691-1695(2003)
| Cas No. | 209860-87-7 | SDF | |
| 别名 | 他氟前列素; AFP-168; MK2452 | ||
| Canonical SMILES | O=C(OC(C)C)CCC/C=C\C[C@@H]1[C@@H](/C=C/C(F)(F)COC2=CC=CC=C2)[C@H](O)C[C@@H]1O | ||
| 分子式 | C25H34F2O5 | 分子量 | 452.53 |
| 溶解度 | DMSO: ≥ 270 mg/mL (596.65 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 | 2.2098 mL | 11.049 mL | 22.098 mL |
| 5 mM | 0.442 mL | 2.2098 mL | 4.4196 mL |
| 10 mM | 0.221 mL | 1.1049 mL | 2.2098 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。
Effects of Tafluprost on Ocular Blood Flow
Ophthalmol Ther 2022 Dec;11(6):1991-2003.PMID:36109465DOI:10.1007/s40123-022-00566-z.
Increasing evidence indicates that improving ocular blood flow (OBF) can be a therapeutic direction for glaucoma therapy. Tafluprost, a prostaglandin analogue which lowers the intraocular pressure (IOP), has been shown to improve OBF in animals and humans. Several animal experiments showed that topical Tafluprost significantly increased optic nerve head and retinal blood flow. Clinical trials also showed a beneficial effect of Tafluprost on optic nerve head and macula blood flow, and a good ocular pulse amplitude-lowering effect. But, there are still a few conflicting results. Overall, Tafluprost seems to have a beneficial effect on OBF, and the positive effect is probably independent from its IOP-lowering effect, which also is expected to improve OBF. Moreover, reducing the intracellular free Ca2+ concentration may be a possible mechanism of Tafluprost's effect on OBF. More well-designed studies are required to reveal the truth.
Tafluprost for glaucoma
Expert Opin Pharmacother 2011 Oct;12(15):2393-401.PMID:21916788DOI:10.1517/14656566.2011.606810.
Introduction: Lowering intraocular pressure (IOP) is, at present, the only therapeutic approach to the treatment of glaucoma. Good compliance is essential in every chronic therapy; therefore, the development of IOP-lowering eye drops that are well tolerated and have an easy administration schedule is essential for the treatment of glaucoma. Prostaglandins are a first-choice drug class for the treatment of glaucoma. Areas covered: This review provides a background on Tafluprost, a newly synthesized prostaglandin analogue, and summarizes the existing data on its efficacy and safety, including comparative data with the other prostaglandin derivatives now available on the market. A review of the literature was performed. Expert opinion: Current research focuses not only on the efficacy of the drugs but also on their tolerability. The importance of obtaining good compliance by the patient is increasingly relevant; therefore, new formulations are studied to provide fewer side effects and an easier schedule. Tafluprost is a new prostaglandin analogue that has been marketed in some European countries and in Japan for more than 2 years and was recently (July 2009) approved in 21 countries. Besides a well-demonstrated IOP-lowering effect, Tafluprost is the first topical prostaglandin available as a preservative-free formulation.
Tafluprost/Timolol: A Review in Open-Angle Glaucoma or Ocular Hypertension
Drugs 2015 Oct;75(15):1807-13.PMID:26431840DOI:10.1007/s40265-015-0476-9.
A once-daily preservative-free fixed combination ophthalmic solution containing Tafluprost 0.0015 % and timolol 0.5 % (hereafter referred to as Tafluprost/timolol) [Taptiqom(®)] has been developed to lower intraocular pressure (IOP) whilst avoiding damage to the ocular surface associated with preservatives such as benzalkonium chloride. Tafluprost/timolol is available in various EU countries for the reduction of IOP in adults with open-angle glaucoma or ocular hypertension who are insufficiently responsive to topical monotherapy with β-adrenergic receptor antagonists or prostaglandin analogues and require a combination therapy, and who would benefit from preservative-free eye drops. In two multinational, phase III studies, Tafluprost/timolol was superior to monotherapy with either preservative-free Tafluprost 0.0015 % once daily or preservative-free timolol 0.5 % twice daily, and noninferior to concomitant therapy with preservative-free Tafluprost 0.0015 % once daily plus preservative-free timolol 0.5 % twice daily in lowering IOP in adults with open-angle glaucoma or ocular hypertension. Tafluprost/timolol was well tolerated in these studies, with a tolerability profile consistent with that of its individual components and with no new adverse reactions observed. Thus, preservative-free fixed combination Tafluprost/timolol is an effective treatment option for the reduction of IOP in adults with open-angle glaucoma or ocular hypertension, providing a useful alternative for those patients who would benefit from preservative-free eye drops.
Tafluprost: the first preservative-free prostaglandin to treat open-angle glaucoma and ocular hypertension
Ann Pharmacother 2012 Nov;46(11):1506-10.PMID:23092867DOI:10.1345/aph.1R229.
Objective: To review the pharmacology, pharmacokinetics, clinical trial data, efficacy data, and adverse effect incidence of Tafluprost. Data sources: A literature search was completed using PubMed, Web of Science, and Google Scholar. Tafluprost was the primary search term. Articles published between January 2008 and April 2012 were included in this review. Additional limits placed on the searches were "human" and "English." Citations in which Tafluprost appeared in the title were 36, 29, and more than 300 in PubMed, Web of Science, and Google Scholar, respectively. Study selection and data extraction: Three clinical trials were included in this review. One trial enrolled more than 500 subjects in a randomized fashion. Another also enrolled more than 500 subjects, although the study design was not randomized. The third trial evaluated the effects of Tafluprost on subjects who had recently discontinued use of latanoprost, another prostaglandin that is approved to treat glaucoma and ocular hypertension. The duration of all 3 trials was 12 weeks. Data synthesis: Tafluprost 0.0015% is the first topical prostaglandin approved by the Food and Drug Administration for treatment of open-angle glaucoma and ocular hypertension that does not contain the widely used preservative, benzalkonium chloride (BAK). Although some controversy surrounds the long-term safety of exposure to BAK, clinical trial data are inconclusive. Tafluprost, like other prostaglandin analogues, exerts its effects on prostaglandin F receptors to reduce intraocular pressure (IOP). Results from 1 trial demonstrated significant reductions in IOP when monotherapy was switched to Tafluprost monotherapy. Reductions in IOP with Tafluprost use were compared with those seen with use of timolol and latanoprost in 2 trials, and noninferiority was observed. Significant reductions in tear osmolarity were noted in subjects who changed from latanoprost, another prostaglandin analogue, to Tafluprost therapy. Conjunctival hyperemia is the most common adverse effect seen in patients receiving drugs from this class. Many have also reported stinging, ocular pruritus, increased darkening or growth of eyelashes, and darkening of eyelids, as well as irreversible brown pigmentation of the iris. Conclusions: Clinical trial data suggest that Tafluprost is as efficacious as other agents used in the management of ocular hypertension and glaucoma. Its use may be especially advantageous in people with allergies, sensitivities to preservatives, or dry or sensitive eyes.
Tafluprost Ophthalmic Solution 0.0015 %: A Review in Glaucoma and Ocular Hypertension
Clin Drug Investig 2016 Jun;36(6):499-508.PMID:27225879DOI:10.1007/s40261-016-0413-z.
Tafluprost ophthalmic solution 0.0015 % preserved with benzalkonium chloride (BAK) 0.001 % is available in several Asian countries, including Japan. In pivotal trials, BAK-preserved Tafluprost ophthalmic solution 0.0015 % lowered intraocular pressure (IOP) more effectively than placebo in Asian patients with normal-tension glaucoma and was at least as effective as latanoprost ophthalmic solution 0.005 % in Asian patients with primary open-angle glaucoma or ocular hypertension. In other prospective studies in Asian patients with glaucoma or ocular hypertension, Tafluprost ophthalmic solution 0.0015 % was at least as effective as latanoprost ophthalmic solution 0.005 % or travoprost ophthalmic solution 0.004 % in terms of IOP lowering, and was considered easier to use and/or store. The efficacy of Tafluprost ophthalmic solution 0.0015 % was maintained in the longer term. Tafluprost ophthalmic solution 0.0015 % was generally well tolerated. In conclusion, BAK-preserved Tafluprost ophthalmic solution 0.0015 % remains a useful option for the treatment of Asian patients with glaucoma and ocular hypertension.