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1g |
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5g |
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Other Sizes |
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ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Perfluorohexyloctane penetrates meibomian glands, where it has been reported to interact with and dissolve the altered, viscous meibum in the glands. A single pharmacokinetic study showed low systemic perfluorohexyloctane blood levels after topical ocular administration. In rabbits, perfluorohexyloctane was detected in tears at six hours and in meibomian glands at 24 hours following ophthalmic administration, with minimal systemic exposure. Metabolism / Metabolites Perfluorohexyloctane was not metabolized by human liver microsomes _in vitro_. |
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References |
[1]. Delicado-Miralles M, et al. Deciphering the Action of Perfluorohexyloctane Eye Drops to Reduce Ocular Discomfort and Pain. Front Med (Lausanne). 2021 Oct 26;8:709712.
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Additional Infomation |
Perfluorohexyloctane is a fluoroalkane that is tetradecane in which all of the hydrogen atoms at positions 1, 2, 3, 4, 5, and 6 have been replaced by fluorine atoms. It is an ophthalmic solution used to treat the signs and symptoms of dry eye disease. It has a role as an ophthalmology drug and a nonionic surfactant. It is a fluorohydrocarbon and a fluoroalkane. It derives from a hydride of a tetradecane.
Perfluorohexyloctane is a semifluorinated alkane that contains six perfluorinated carbon atoms and eight hydrogenated carbon atoms. It is an inert, slightly amphiphilic compound. Because it is a completely non-aqueous liquid, microbial growth is not possible; therefore, its drug products do not need to be combined with any preservative. Perfluorohexyloctane has been used in the field of ophthalmology as a vitreous substitute. It was approved by the FDA on May 18, 2023 for the treatment of dry eye disease. Drug Indication Perfluorohexyloctane ophthalmic formulation is indicated for the treatment of the signs and symptoms of dry eye disease. Mechanism of Action Perfluorohexyloctane mediates its actions in the lipid layer and meibomian glands. While the exact mechanism of action is not fully understood, perfluorohexyloctane is believed to interact with the air-liquid interface of the tear film and form a monolayer, preventing the evaporation of the aqueous phase of the tears. Pharmacodynamics Perfluorohexyloctane is administered ophthalmically to alleviate symptoms of dry eye disease, increase tear film breakup time, and increase lipid layer thickness. Having low surface and interface tensions, perfluorohexyloctane spreads rapidly across the ocular surface. It is reported to cause minimal visual disturbances, attributed to its refractive index being similar to that of water. |
Molecular Formula |
C14H17F13
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Molecular Weight |
432.26
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Exact Mass |
432.112
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CAS # |
133331-77-8
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PubChem CID |
10477896
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Appearance |
Typically exists as solid at room temperature
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LogP |
7.475
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Hydrogen Bond Donor Count |
0
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Hydrogen Bond Acceptor Count |
13
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Rotatable Bond Count |
11
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Heavy Atom Count |
27
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Complexity |
464
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Defined Atom Stereocenter Count |
0
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SMILES |
FC(F)(F)C(F)(F)C(F)(F)C(F)(F)C(F)(F)C(F)(F)CCCCCCCC
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InChi Key |
WRYIIOKOQSICTB-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C14H17F13/c1-2-3-4-5-6-7-8-9(15,16)10(17,18)11(19,20)12(21,22)13(23,24)14(25,26)27/h2-8H2,1H3
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Chemical Name |
1,1,1,2,2,3,3,4,4,5,5,6,6-tridecafluorotetradecane
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Synonyms |
Miebo
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HS Tariff Code |
2934.99.9001
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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)
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Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.3134 mL | 11.5671 mL | 23.1342 mL | |
5 mM | 0.4627 mL | 2.3134 mL | 4.6268 mL | |
10 mM | 0.2313 mL | 1.1567 mL | 2.3134 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.