9-keto Fluprostenol isopropyl ester
(Synonyms: 9-酮氟前列醇异丙酯) 目录号 : GC42647
A potential EP agonist in prodrug form
Cas No.:1219032-18-4
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 is a well-studied, potent analog of prostaglandin F2α (PGF2α) and acts primarily through the FP receptor. Oxidation at C-9 of fluprostenol yields 9-keto fluprostenol. Prostaglandin esters are known to be hydrolyzed in the eye to the corresponding free acids. However, the use of prostaglandin esters as prodrugs outside the eye is relatively unexplored. 9-keto Fluprostenol is an analog of PGE2 with structural modifications intended to give it a prolonged half-life and greater potency. 9-keto Fluprostenol isopropyl ester has the potential to act as an EP agonist in prodrug form. However, no studies on the pharmacology of this compound have been published to date. In addition 9-keto fluprostenol isopropyl ester is a potential metabolite of Travoprost, which is the Alcon trade name for fluprostenol isopropyl ester. In monkey cornea, this transformation was observed as a product of NADP+-dependent 15-hydroxyprostaglandin dehydrogenase when the closely related analog Latanoprost was used as a substrate. Certain F-series prostaglandins have been shown to be converted to the corresponding E-series compounds in rabbit liver and human platelet preparations.
| Cas No. | 1219032-18-4 | SDF | |
| 别名 | 9-酮氟前列醇异丙酯 | ||
| Canonical SMILES | O[C@H]1[C@H](/C=C/[C@@H](O)COC2=CC(C(F)(F)F)=CC=C2)[C@@H](C/C=C\CCCC(OC(C)C)=O)C(C1)=O | ||
| 分子式 | C26H33F3O6 | 分子量 | 498.5 |
| 溶解度 | DMF: 30 mg/ml,DMF:PBS (1:1): 500 µ g/ml,DMSO: 20 mg/ml,Ethanol: 25 mg/ml | 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 | 2.006 mL | 10.0301 mL | 20.0602 mL |
| 5 mM | 0.4012 mL | 2.006 mL | 4.012 mL |
| 10 mM | 0.2006 mL | 1.003 mL | 2.006 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。
Effect of femto to nano molar concentrations of prostaglandin analogues on pregnant rat uterine contractility
Eur J Pharmacol 2008 Feb 26;581(1-2):185-90.PMID:18177857DOI:10.1016/j.ejphar.2007.11.041
Prostaglandins are bioactive lipids and important mediators of uterine relaxation as well as contraction during pregnancy and labour. E series prostaglandins may directly contract or relax myometrium in a dose-dependent manner, with the relaxatory effects mediated through the prostanoid receptors EP(2) and EP(4). The aim of this study was to evaluate the pharmacological effects of prostaglandin analogues on isolated pregnant rat uterine contractility, at 10(-15) to 10(-9) M concentrations. Uterine strips from rats at 19 days of gestation were set up in organ baths at 37 degrees C, bathed in Krebs buffer and gassed with 95% O(2)/5% CO(2). Spontaneous contractions were recorded via a force transducer. Concentration ranges of 10(-15)-10(-9) M of PGE(2), PGF(2alpha) and a range of prostaglandin analogues were applied non-cumulatively to the tissues. Spontaneous contractions were recorded for 12 min post dose. Amplitude, frequency, baseline tone and percent contractility over 10 min periods were analysed. PGE(2), butaprost, 9-keto fluprostenol, 11-keto fluprostenol, 9-keto Fluprostenol isopropyl ester, AL8810 and 15(S)-15-methyl PGE(2) all caused a decrease in percent contractility (P<0.05). These agents, plus Delta(12)PGJ(2) and 9-deoxy-9-methylene-16,16-dimethyl PGE(2), also decreased frequency of contraction (P<0.05). Only PGE(2), PGF(2alpha) and 11-keto fluprostenol decreased baseline tone (P<0.05). The lower concentrations of prostaglandins used here mediated inhibition of spontaneous contractility of pregnant rat myometrium. Use of selective agonists suggested that the prostanoid receptors EP(2) and DP(2) are responsible for this relaxatory effect.