| Size | Price | |
|---|---|---|
| Other Sizes |
| Targets |
Interact with the air-liquid interface of the tear film and form a monolayer, preventing the evaporation of the aqueous phase of the tears.
|
|---|---|
| ln Vitro |
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.
|
| ln Vivo |
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.
PERFLUOROHEXYLOCTANE is a small molecule drug with a maximum clinical trial phase of IV (across all indications) that was first approved in 2023 and is indicated for dry eye syndrome and has 1 investigational indication. |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Perfluorohexane can penetrate the meibomian glands and has been reported to interact with and dissolve the denatured, viscous meibomian gland tissue. A pharmacokinetic study showed low systemic blood concentrations after topical ocular administration. In a rabbit model, perfluorohexane was detectable in tears 6 hours after ocular administration and in the meibomian glands 24 hours after administration, indicating extremely low systemic exposure. Metabolism/Metabolites In vitro studies have shown that perfluorohexane is not metabolized by human hepatic microsomes. |
| Toxicity/Toxicokinetics |
Effects during pregnancy and lactation
◉ Overview of medication use during lactation There is currently no information regarding the use of perfluorohexane during lactation. Because perfluorohexane is poorly absorbed, it is unlikely to enter the infant's bloodstream and will not cause any adverse effects on breastfed infants. No special precautions are required. ◉ Effects on breastfed infants As of the revision date, no relevant published information was found. ◉ Effects on lactation and breast milk As of the revision date, no relevant published information was found. |
| References |
[1]. Deciphering the Action of Perfluorohexyloctane Eye Drops to Reduce Ocular Discomfort and Pain. Front Med (Lausanne). 2021 Oct 26;8:709712.
[2]. https://pubchem.ncbi.nlm.nih.gov/compound/10477896 |
| Additional Infomation |
Perfluorohexyloctane is a fluoroalkane, a derivative of tetradecane, in which all hydrogen atoms at positions 1, 2, 3, 4, 5, and 6 are replaced by fluorine atoms. It is an ophthalmic solution used to treat symptoms of dry eye. It is both an ophthalmic drug and a nonionic surfactant. It is a fluorocarbon and a fluoroalkane. It is derived from the hydride of tetradecane. Perfluorohexyloctane is a semi-fluorinated alkane containing six perfluorinated carbon atoms and eight hydride carbon atoms. It is an inert, slightly amphiphilic compound. Because it is a completely non-aqueous liquid, microorganisms cannot grow; therefore, its pharmaceutical formulations do not require any preservatives. Perfluorohexyloctane has been used in ophthalmology as a vitreous substitute. This drug was approved by the U.S. Food and Drug Administration (FDA) on May 18, 2023, for the treatment of dry eye.
Drug Indications Perfluorohexyloctane ophthalmic preparations are indicated for the treatment of signs and symptoms of dry eye. Mechanism of Action Perfluorohexoctane exerts its effects by acting on the lipid layer and meibomian glands. Although its exact mechanism of action is not fully elucidated, it is generally believed that perfluorohexoctane interacts with the gas-liquid interface of the tear film to form a monolayer, thereby preventing the evaporation of the aqueous phase of the tear. Pharmacodynamics Perfluorohexoctane, when administered ocularly, can relieve dry eye symptoms, prolong tear film breakup time, and increase lipid layer thickness. Due to its low surface and interfacial tension, perfluorohexoctane can rapidly diffuse throughout the entire ocular surface. It has been reported that, due to its refractive index being similar to that of water, it causes minimal visual disturbance. |
| Molecular Formula |
C14H17F13
|
|---|---|
| Molecular Weight |
432.26
|
| Exact Mass |
432.112
|
| Elemental Analysis |
C, 38.90; H, 3.96; F, 57.14
|
| CAS # |
133331-77-8
|
| PubChem CID |
10477896
|
| Appearance |
Colorless to light yellow liquid（Density：1.331 g/cm3）
|
| LogP |
7.475
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
13
|
| Rotatable Bond Count |
11
|
| Heavy Atom Count |
27
|
| Complexity |
464
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
FC(F)(F)C(F)(F)C(F)(F)C(F)(F)C(F)(F)C(F)(F)CCCCCCCC
|
| InChi Key |
WRYIIOKOQSICTB-UHFFFAOYSA-N
|
| 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
|
| Chemical Name |
1,1,1,2,2,3,3,4,4,5,5,6,6-tridecafluorotetradecane
|
| Synonyms |
Miebo;
1-(Perfluorohexyl)octane; 133331-77-8; perfluorohexyloctane; 1,1,1,2,2,3,3,4,4,5,5,6,6-tridecafluorotetradecane; MIEBO;
|
| 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: ~100 mg/mL (~231 mM)
|
|---|---|
| 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.
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