| Size | Price | Stock | Qty |
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| 1mg |
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| 10mg | |||
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| Targets |
F 16915 functions as a prodrug of docosahexaenoic acid (DHA), a long-chain omega-3 polyunsaturated fatty acid. Upon administration, F 16915 is metabolized to release DHA, which exerts its biological effects through multiple mechanisms including modulation of membrane fluidity, anti-inflammatory signaling, and regulation of cardiac ion channels. DHA is known to have cardioprotective effects and can prevent atrial fibrillation.
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| ln Vitro |
In vitro, F 16915 is evaluated for its ability to release DHA and its stability in biological matrices. As a prodrug, its in vitro activity is assessed by measuring the rate and extent of conversion to DHA in the presence of esterases or in plasma. The compound's ability to prevent heart failure-induced atrial fibrillation is linked to the biological activity of its active metabolite DHA.
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| ln Vivo |
F16915 (100 mg/kg; daily oral gavage for 2 months) decreases the fast deterioration in left ventricular (LV) systolic function and left atrial (LA) cavity dilation in rats two months after reperfusion and infarction[1]. F 16915 (1–5 g/day for 4 weeks) prevents left ventricular free wall thinning and dramatically lowers the extent of infarcts [1].
In vivo, F 16915 demonstrates cardioprotective effects in rat models of heart failure. In male Sprague-Dawley rats with heart failure induced by occlusion of the left descending coronary artery and reperfusion, oral administration of F 16915 at 100 mg/kg daily for 2 months reduced marked dilation of the left atrial cavity and the decline of left ventricular contractile function. F 16915 (1-5 g/day for 4 weeks) significantly reduces infarct size and prevents left ventricular free wall thinning. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for F 16915 are not typically performed, as the compound is a prodrug that exerts its effects through release of DHA. Instead, the compound's stability and conversion to DHA are assessed in plasma or tissue homogenates. DHA itself is known to interact with various receptors and ion channels, but F 16915 is primarily evaluated for its prodrug properties and DHA delivery efficiency.
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| Cell Assay |
In vitro cellular assays for F 16915 involve treating cells with the compound and measuring DHA release and subsequent biological effects. Cells such as cardiomyocytes or endothelial cells are treated with F 16915, and the levels of free DHA and its metabolites are quantified by LC-MS. Cellular effects of DHA, including changes in membrane composition, inflammatory marker expression, and ion channel function, are also assessed.
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rats (220-300 g), suffering from heart failure caused by occlusion of the left descending coronary artery and reperfusion for 2 months [1]
Doses: 100 mg/kg Route of Administration: Daily oral administration Results of intragastric (po) (po) Route of Administration: the infarct area was diminished. Prevents left ventricular free wall thinning. diminished dephosphorylation of connexin 43 in atrial tissue. In vivo animal experiments for F 16915 are conducted in rat models of heart failure. Male Sprague-Dawley rats (220-300 g) undergo occlusion of the left descending coronary artery followed by 2 months of reperfusion to induce heart failure. F 16915 is administered via daily oral gavage at 100 mg/kg for 2 months. Endpoints include measurement of infarct size, left ventricular function, atrial dilation, and phosphorylation status of connexin43. |
| ADME/Pharmacokinetics |
Pharmacokinetic studies of F 16915 in male rats following a single oral dose of 300 mg/kg show time-dependent changes in blood concentrations of total DHA and nicotinyl alcohol. As a DHA prodrug, F 16915 is designed to improve the oral bioavailability and pharmacokinetic profile of DHA. The compound has a molecular weight of 419.60 and molecular formula C28H37NO2. It appears as an oil with color ranging from colorless to light yellow.
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| Toxicity/Toxicokinetics |
Toxicological data for F 16915 are not extensively reported in the available literature. As a research compound, its safety profile has not been formally evaluated in comprehensive preclinical toxicology studies. The compound is intended for research purposes only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling this compound.
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| References |
[1]. Le Grand B, et al. F 16915 prevents heart failure-induced atrial fibrillation: a promising new drug as upstream therapy. Naunyn Schmiedebergs Arch Pharmacol. 2014 Jul;387(7):667-77.
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| Additional Infomation |
F 16915 is a synthetic DHA derivative and prodrug with CAS number 92510-91-3, molecular formula C28H37NO2, and molecular weight 419.60. It is also known as a docosahexaenoic acid derivative that can prevent heart failure-induced atrial fibrillation. The compound is supplied as an oil and should be stored appropriately. It is for research use only and is not intended for diagnostic or therapeutic applications.
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| Molecular Formula |
C28H37NO2
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| Molecular Weight |
419.598888158798
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| Exact Mass |
419.282
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| CAS # |
92510-91-3
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| PubChem CID |
14671646
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| Appearance |
Colorless to light yellow oil
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| LogP |
6.9
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
17
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| Heavy Atom Count |
31
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| Complexity |
611
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCC(=O)OCC1=CN=CC=C1
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| InChi Key |
BUWVEXMRBAWBPJ-KUBAVDMBSA-N
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| InChi Code |
InChI=1S/C28H37NO2/c1-2-3-4-5-6-7-8-9-10-11-12-13-14-15-16-17-18-19-20-23-28(30)31-26-27-22-21-24-29-25-27/h3-4,6-7,9-10,12-13,15-16,18-19,21-22,24-25H,2,5,8,11,14,17,20,23,26H2,1H3/b4-3-,7-6-,10-9-,13-12-,16-15-,19-18-
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| Chemical Name |
pyridin-3-ylmethyl (4Z,7Z,10Z,13Z,16Z,19Z)-docosa-4,7,10,13,16,19-hexaenoate
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
DMSO : ≥ 100 mg/mL (~238.32 mM)
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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 | 2.3832 mL | 11.9161 mL | 23.8322 mL | |
| 5 mM | 0.4766 mL | 2.3832 mL | 4.7664 mL | |
| 10 mM | 0.2383 mL | 1.1916 mL | 2.3832 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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