Tafluprost
Based on 1 Customer Validation
Tafluprost (AFP-168) is an anti-glaucoma prostaglandin (PG) analog. Tafluprost can inhibit the apoptosis of retinal ganglion cells (RGCs) and rat RGCs cells. Tafluprost promotes axon regeneration by regulating Zn2+-mTORpathway, inhibits intracellular lipid accumulation in human preorbital adipocytes. Tafluprost can be used in the study of optic nerve injury in glaucoma.
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- Pureza: 99.69%
- No. CAS: 209860-87-7
- Fòrmula: C25H34F2O5
- Peso molecular:452.53
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Almacenamiento:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Tafluprost (3 μM, 48 h) decreases the number of apoptosis in RGC-5 cells[1].
Tafluprost (0.1-100 μM, 48 h) enhances cell viability in RGC-5 cells in a dose-dependent manner[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RGC
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Concentration:0.1, 1, 3, 10, 100 μM
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Incubation Time:48 h
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Result:Enhanced the viability of these cells in a dose-dependent fashion, with an optimal concentration of 3μM.
Increased the relative fluorescence intensity (RFI).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague rat model[2]
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Dosage:0.0015%
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Administration:Via eye drops
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Result:Increased the number of RGCs and reduced the number of TUNEL-positive cells.
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Animal Model:Prostaglandin receptor deletion C57BL/6 mice model[3]
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Dosage:3 μL (0.0015% Tafluprost)
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Administration:Instillation; Single dose
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Result:Reduced IOP in WT, EP1KO, EP2KO, EP3KO and FPKO mice, and the average IOP reduction rates were 25.8(2.1)%, 26.3(0.8)%, 24.2(1.4)%, 16.5(1.7)% and 20.9(1.5)%, respectively. (The decrease of IOP in EP3KO and FPKO mice was less than that in WT mice.)
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 209860-87-7
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Appearance Liquid (Density: 1.186 g/cm3)
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Peso molecular 452.53
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Fòrmula C25H34F2O5
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Color Colorless to light yellow
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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
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Synonyms
AFP-168; MK2452
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : ≥ 250 mg/mL (552.45 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.25 mg/mL (4.97 mM); Clear solution
This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.25 mg/mL (4.97 mM); Clear solution
This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (280 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Kuwayama, Y. and A. Nomura, Prospective observational post-marketing study of tafluprost for glaucoma and ocular hypertension: short-term efficacy and safety. Adv Ther, 2014. 31(4): p. 461-71. [Content Brief]
[2]. Kanamori A, et al. Tafluprost protects rat retinal ganglion cells from apoptosis in vitro and in vivo. Graefes Arch Clin Exp Ophthalmol. 2009 Oct;247(10):1353-60. [Content Brief]
[3]. Ota T, et al. The IOP-lowering effects and mechanism of action of tafluprost in prostanoid receptor-deficient mice. Br J Ophthalmol. 2007 May;91(5):673-6. [Content Brief]
[4]. Kumagami, T., et al., Comparison of corneal safety and intraocular pressure-lowering effect of tafluprost ophthalmic solution with other prostaglandin ophthalmic solutions. J Ocul Pharmacol Ther, 2014. 30(4): p. 340-5. [Content Brief]
[5]. Inoue, K., A. Tanaka, and G. Tomita, Effects of tafluprost treatment for 3 years in patients with normal-tension glaucoma. Clin Ophthalmol, 2013. 7: p. 1411-6. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2098 mL | 11.0490 mL | 22.0980 mL | 55.2450 mL |
| 5 mM | 0.4420 mL | 2.2098 mL | 4.4196 mL | 11.0490 mL | |
| 10 mM | 0.2210 mL | 1.1049 mL | 2.2098 mL | 5.5245 mL | |
| 15 mM | 0.1473 mL | 0.7366 mL | 1.4732 mL | 3.6830 mL | |
| 20 mM | 0.1105 mL | 0.5524 mL | 1.1049 mL | 2.7622 mL | |
| 25 mM | 0.0884 mL | 0.4420 mL | 0.8839 mL | 2.2098 mL | |
| 30 mM | 0.0737 mL | 0.3683 mL | 0.7366 mL | 1.8415 mL | |
| 40 mM | 0.0552 mL | 0.2762 mL | 0.5524 mL | 1.3811 mL | |
| 50 mM | 0.0442 mL | 0.2210 mL | 0.4420 mL | 1.1049 mL | |
| 60 mM | 0.0368 mL | 0.1841 mL | 0.3683 mL | 0.9207 mL | |
| 80 mM | 0.0276 mL | 0.1381 mL | 0.2762 mL | 0.6906 mL | |
| 100 mM | 0.0221 mL | 0.1105 mL | 0.2210 mL | 0.5524 mL |
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