Size | Price | Stock | Qty |
---|---|---|---|
1mg |
|
||
2mg |
|
||
5mg |
|
||
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
Other Sizes |
|
Purity: ≥98%
Tafluprost (formerly MK-2452; MK2452; AFP-168; Taflotan; Zioptan) is a prostaglandin (PG) analog used as an anti-glaucoma drug. Tafluprost is applied topically (as eye drops) to treat ocular hypertension and regulate the advancement of glaucoma. It lowers intraocular pressure by causing the eyes to expel more aqueous fluid.
Targets |
PGF2α
|
---|---|
ln Vitro |
Tafluprost (3 μM, 48 h) causes RGC-5 cells to produce fewer cells[1]. Tafluprost (0.1-100 μM, 48 h) increases RGC-5 cell viability in a dose-dependent way[2].
|
ln Vivo |
Tafluprost (0.0015% AFP168 eye drops, used for 14 days) as a makeup Sprague-Dawley can decrease nerve cell apoptosis, raise RGC cell vitality, and lower intraocular pressure caused by optic nerve compression (ONC)[2].
|
Cell Assay |
Cell Line: RGC
Concentration: 0.1, 1, 3, 10, 100 μM Incubation Time: 48 h Result: Enhanced the viability of these cells in a dose-dependent fashion, with an optimal concentration of 3μM. Increased the relative fluorescence intensity (RFI). |
Animal Protocol |
Male Sprague rat model
0.0015% Via eye drops |
References |
|
Molecular Formula |
C25H34F2O5
|
---|---|
Molecular Weight |
452.5313
|
Exact Mass |
452.24
|
Elemental Analysis |
C, 66.35; H, 7.57; F, 8.40; O, 17.68
|
CAS # |
209860-87-7
|
Related CAS # |
209860-88-8 (Tafluprost acid); 157283-68-6 (Travoprost)
|
Appearance |
White solid powder
|
SMILES |
CC(C)OC(=O)CCC/C=C\C[C@H]1[C@H](C[C@H]([C@@H]1/C=C/C(COC2=CC=CC=C2)(F)F)O)O
|
InChi Key |
WSNODXPBBALQOF-VEJSHDCNSA-N
|
InChi Code |
InChI=1S/C25H34F2O5/c1-18(2)32-24(30)13-9-4-3-8-12-20-21(23(29)16-22(20)28)14-15-25(26,27)17-31-19-10-6-5-7-11-19/h3,5-8,10-11,14-15,18,20-23,28-29H,4,9,12-13,16-17H2,1-2H3/b8-3-,15-14+/t20-,21-,22+,23-/m1/s1
|
Chemical Name |
propan-2-yl (Z)-7-[(1R,2R,3R,5S)-2-[(E)-3,3-difluoro-4-phenoxybut-1-enyl]-3,5-dihydroxycyclopentyl]hept-5-enoate
|
Synonyms |
AFP-168; MK2452; AFP-168; MK-2452; AFP-168; MK 2452; Saflutan; Taflotan; Tapros; Zioptan
|
HS Tariff Code |
2934.99.9001
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
DMSO: ≥ 270 mg/mL (~596.7 mM)
|
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.25 mg/mL (4.97 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 22.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.25 mg/mL (4.97 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 22.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.25 mg/mL (4.97 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2098 mL | 11.0490 mL | 22.0980 mL | |
5 mM | 0.4420 mL | 2.2098 mL | 4.4196 mL | |
10 mM | 0.2210 mL | 1.1049 mL | 2.2098 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT05299593 | Recruiting | Drug: tafluprost/timolol | Glaucoma, Open-Angle Ocular Hypertension |
Fondazione G.B. Bietti, IRCCS | June 4, 2020 | Phase 4 |
NCT04737928 | Completed | Drug: Latanoprost Drug: tafluprost |
Glaucoma, Primary Open Angle | Santen Pharmaceutical (Taiwan) Co., LTD |
April 2, 2018 | Not Applicable |
NCT01369771 | Completed | Drug: Tafluprost 0.0015% | Ocular Hypertension Open-Angle Glaucoma |
FinnMedi Oy | August 2010 | Phase 4 |
NCT03204487 | Completed | Drug: Tafluprost 15µg/ml | Glaucoma, Open-Angle Ocular Hypertension |
Ordination Dr. Hommer | May 10, 2016 | Phase 4 |
NCT00918346 | Completed | Drug: Tafluprost 0.0015% | Open-Angle Glaucoma Ocular Hypertension |
Santen Oy | September 2005 | Phase 3 |
Effect of diclofenac Na (0.1%) on tafluprost‐induced intraocular pressure reduction in wild‐type and EP3 receptor knockout (EP3KO) mice at night. Br J Ophthalmol . 2007 May;91(5):673-6. td> |
(A) Mean deviation and (B) pattern standard deviation (SD) at baseline, 1 year, 2 years, and 3 years after treatment with tafluprost. Clin Ophthalmol . 2013:7:1411-6. td> |