Fluorometholone
(Synonyms: 氟米龙) 目录号 : GC40771
A synthetic glucocorticoid
Cas No.:426-13-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Fluorometholone is a synthetic glucocorticoid that binds to glucocorticoid receptors (IC50 = 1.5 nM; Kd = 2.8 nM in a radioligand binding assay). Fluorometholone (0.01%) decreases survival of cultured corneal epithelial cells and inhibits their migration in a scratch assay following 12 hours of treatment. Formulations containing fluorometholone have been used for the treatment of eye inflammation.
| Cas No. | 426-13-1 | SDF | |
| 别名 | 氟米龙 | ||
| Canonical SMILES | O=C1C=C[C@@]2(C)C([C@@H](C)C[C@]3([H])[C@]2(F)[C@@H](O)C[C@@]4(C)[C@@]3([H])CC[C@]4(O)C(C)=O)=C1 | ||
| 分子式 | C22H29FO4 | 分子量 | 376.5 |
| 溶解度 | DMSO : 50 mg/mL (132.82 mM; Need ultrasonic) | 储存条件 | 4°C, away from moisture and light |
| 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 | 2.656 mL | 13.2802 mL | 26.5604 mL |
| 5 mM | 0.5312 mL | 2.656 mL | 5.3121 mL |
| 10 mM | 0.2656 mL | 1.328 mL | 2.656 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。
Fluorometholone inhibits high glucose-induced cellular senescence in human retinal endothelial cells
Hum Exp Toxicol 2022 Jan-Dec;41:9603271221076107.PMID:35264022DOI:10.1177/09603271221076107.
Diabetic retinopathy (DR) is a common diabetic complication that severely impacts the life quality of diabetic patients. Recently, cellular senescence in human retinal endothelial cells (HRECs) induced by high glucose has been linked to the pathogenesis of DR. Fluorometholone (FML) is a glucocorticoid drug applied in the treatment of inflammatory and allergic disorders of the eye. The objective of the present study is to investigate the protective function of FML on high glucose-induced cellular senescence in HRECs. The in vitro injury model was established by stimulating HRECs with 30 mm glucose. After evaluating the cytotoxicity of FML in HRECs, 0.05% and 0.1% FML were used as the optimal concentration in the entire experiment. It was found that the excessive released inflammatory factors including tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), and interleukin-8 (IL-8) in HRECs induced by high glucose were significantly suppressed by FML, accompanied by the inhibitory effects on the expression levels of vascular endothelial growth factor (VEGF) and tissue factor (TF). Declined telomerase activity and enhanced senescence-associated β-galactosidase (SA-β-gal) activity were found in high glucose-challenged HRECs, which were dramatically alleviated by FML, accompanied by the inactivation of the p53/p21 and retinoblastoma (Rb) signaling. Interestingly, FML ameliorated high glucose-induced dephosphorylation of Akt. Lastly, the protective effects of FML against high glucose-induced cellular senescence in HRECs were abolished by the co-treatment of the PI3K/Akt signaling inhibitor LY294002, suggesting the involvement of this pathway. Taken together, these data revealed that FML-inhibited high glucose-induced cellular senescence mediated by Akt in HERCs, suggesting a novel molecular mechanism of FML.
Fluorometholone modulates gene expression of ocular surface mucins
Acta Ophthalmol 2019 Dec;97(8):e1082-e1088.PMID:30963711DOI:10.1111/aos.14113.
Purpose: Mucins are vital to keep the ocular surface hydrated. Genes encoding for mucins contain a glucocorticoid response element. The purpose of this study was to evaluate the effect of Fluorometholone, a glucocorticoid receptor agonist used in the management of dry eye, on the gene expression of conjunctival and corneal epithelial cell mucins. Methods: Stratified cultures of human conjunctival and corneal epithelial cells were exposed to 25, 50 and 100 nM of Fluorometholone alone or in presence of mifepristone, a glucocorticoid receptor antagonist. The mRNA was isolated from the cells and reverse transcribed to cDNA. The cDNA was used for quantification of gene expression of mucin (MUC) 1, 4, 16 and 19 using real-time PCR. Results: Fluorometholone caused a dose- and time-dependent increase in the gene expression of MUC1, MUC4, MUC16 and MUC19 in the conjunctival as well as corneal epithelial cells. Mifepristone, a glucocorticoid receptor antagonist, inhibited fluorometholone-mediated increase in the gene expression of conjunctival and corneal mucins. At the tested concentration, neither Fluorometholone nor mifepristone caused any notable changes in the cellular phenotype or viability of conjunctival and corneal epithelial cells. Conclusion: Fluorometholone increases the gene expression of MUC1, MUC4, MUC16 and MUC19 in the conjunctival and corneal epithelial cells through activation of glucocorticoid receptors. The increased expression of mucins can be an additional possible mechanism contributing to the beneficial effects of Fluorometholone in dry eye in addition to its well-known anti-inflammatory effects.
Do reducing regimens of Fluorometholone for paediatric ocular surface disease cause glaucoma?
Br J Ophthalmol 2011 Nov;95(11):1531-3.PMID:21296793DOI:10.1136/bjo.2010.192773.
Background/aims: Although Fluorometholone (FML) is considered a steroid of minimal ocular penetration, reports in children have shown dose-dependent intraocular pressure (IOP) rise. The authors aimed to assess whether reducing regimens of FML for paediatric ocular surface disease have sustained clinically significant ocular hypertensive effects. Methods: Retrospective case-note review. Glaucoma was defined as an IOP of ≥ 21 mm Hg on at least two occasions or, in young children, moderate/firm digital IOP with one of the following: myopic shift, increased cup:disc ratio or corneal oedema. Exclusion criteria were other concurrent steroids or pre-existing optic nerve disease. Results: 107 cases were included. The median age was 6 years (range 3 months to 17 years). The commonest indication for FML was blepharo-kerato-conjunctivitis. The maximal frequency prescribed was four times a day, gradually reduced to once weekly in cases of long-term treatment. The mean total number of eye-drop applications was 228 over a mean time span of 9 months. Post-FML IOP was formally documented in 51/107 casenotes (median age 6.85 years, range 4 months to 16 years) and it was <19 mm Hg in all cases. 56 cases did not allow IOP measurement (median age 5.9 years, range 3 months to 17 years), but none met the glaucoma definition. Conclusions: In this cohort, reducing regimens of FML proved to be a safe anti-inflammatory treatment in terms of avoiding steroid-induced glaucoma.
A topical Fluorometholone nanoformulation fabricated under aqueous condition for the treatment of dry eye
Colloids Surf B Biointerfaces 2022 Apr;212:112351.PMID:35091382DOI:10.1016/j.colsurfb.2022.112351.
Fluorometholone (FMT) is a frequently prescribed drug for the alleviation of dry eye. However, due to low aqueous solubility, it has been routinely used as an ophthalmic suspension, which is characterized by low bioavailability, inconvenience of administration, and difficulty in delivering accurate dose. Furthermore, the opaque appearance of the ophthalmic suspension is not desirable for optical purpose. In the present study, a transparent FMT nanoformulation (FMT-CD NPs) was fabricated by the cyclodextrin (CD) nanoparticle technology without organic solvents. It was demonstrated that FMT was encapsulated in an amorphous form, which was associated with increased release rate and enhanced corneal penetration efficiency. The biocompatibility of FMT-CD NPs was confirmed by the Live/Dead assay, CCK-8 assay and the wound healing assay. Most importantly, FMT-CD NPs alleviated dry eye signs more efficiently than the commercial eye drop, with one-fifth the dosage of FMT in the latter. Collectively, our study provides a promising FMT formulation for improved management of dry eye while reducing drug related side effects.
Fluorometholone 0.1% as Ancillary Therapy for Trachomatous Trichiasis Surgery: Randomized Clinical Trial
Am J Ophthalmol 2019 Jan;197:145-155.PMID:30267699DOI:10.1016/j.ajo.2018.09.017.
Purpose: To assess the hypothesis that Fluorometholone 0.1% eye drops are safe and effective as adjunctive therapy for trachomatous trichiasis (TT) surgery; determining the most promising dose. Design: Randomized, placebo-controlled, double-masked parallel dose-ranging clinical trial. Methods: Patients undergoing upper lid TT surgery at a rural Ethiopian hospital were randomized to Fluorometholone 0.1% twice daily for 4 weeks, 4 times daily for 4 weeks, 4 times daily for 8 weeks, or matching frequency placebo in a 3:1:3:1:3:1 ratio for 1 eye. Randomization was stratified by TT severity (1-4 vs ≥5 lashes touching the globe). Safety outcomes (intraocular pressure [IOP] elevation, cataract, and other dose-limiting toxicities) and postoperative TT incidence were assessed over 1 year. Results: Subjects randomized were 39:13:39:13:38:13 in the respective groups, and 1 subject in the 8-weeks Fluorometholone group was withdrawn. Of 154 subjects, 148 (96.1%) completed 1 year's follow-up. Among 76 eyes receiving Fluorometholone 4 times daily, 1 developed IOP elevation ≥ 30 mm Hg (to 37 mm Hg) and 1 had an allergic reaction attributed to the study drug; each resolved upon drug cessation without sequelae. No cataract or other dose-limiting toxicity events occurred. Postoperative TT within 1 year occurred in 29.3% of placebo eyes vs 17.7%, 19.6%, and 23.2% among the respective Fluorometholone groups (P = .29 comparing placebo vs all active treatments combined). Conclusions: The results suggest Fluorometholone 0.1% is likely to be safe and efficacious to reduce postoperative TT following TT surgery, and 1 drop twice daily for 4 weeks is the most promising dose. Confirmation in a full-scale clinical trial is needed before programmatic implementation.