| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 250mg | |||
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| Targets |
FFPM targets phosphodiesterase 4 (PDE4), a key enzyme that hydrolyzes cyclic AMP (cAMP). It acts as a selective PDE4 inhibitor with an IC50 of 26.2 nM against the human PDE4 core catalytic domain. Some sources report an IC50 of 6 nM with good selectivity over other PDEs. The compound has oral bioavailability and blood-brain barrier permeability.
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| ln Vitro |
In vitro, FFPM inhibits PDE4 with an IC50 of 26.2 nM against the human PDE4 core catalytic domain, with some sources reporting 6 nM. It suppresses inflammasome activation in microglial cells by enhancing autophagy. The compound demonstrates good selectivity over other phosphodiesterase subtypes and reduces pro-inflammatory cytokine production in cultured cells.
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| ln Vivo |
In vivo, FFPM is orally bioactive and blood-brain barrier permeable. It reverses cognitive deficits in animal models and suppresses pro-inflammatory factor production. The compound's anti-inflammatory effects in the central nervous system make it a potential candidate for neuroinflammatory and cognitive disorders.
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| Enzyme Assay |
The in vitro enzyme assay for FFPM involves measuring its inhibitory effect on phosphodiesterase 4 (PDE4) activity. Recombinant human PDE4 enzyme is incubated with varying concentrations of FFPM and a fluorescent or radiometric substrate (e.g., cAMP). The extent of cAMP hydrolysis is measured, and the IC50 is calculated from dose-response curves. FFPM inhibits human PDE4 with an IC50 of 26.2 nM.
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| Cell Assay |
In vitro cellular assays for FFPM involve treating cultured microglial cells or other immune cells with varying concentrations of the compound. Inflammasome activation is induced using LPS and ATP or other stimuli. Autophagy markers (e.g., LC3-II) are measured by Western blotting. Pro-inflammatory cytokine levels (e.g., IL-1β, TNF-α) in the culture medium are measured by ELISA. FFPM suppresses inflammasome activation by enhancing autophagy.
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| Animal Protocol |
In vivo animal experiments for FFPM typically use rodent models of cognitive impairment or neuroinflammation. The compound is administered orally at various doses. Cognitive function is assessed using behavioral tests such as the Morris water maze or novel object recognition. Brain tissue is analyzed for cytokine levels, autophagy markers, and PDE4 activity. FFPM reverses cognitive deficits and suppresses pro-inflammatory factor production.
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| ADME/Pharmacokinetics |
FFPM (Roflupram) has oral bioavailability and blood-brain barrier permeability. It is a selective PDE4 inhibitor with molecular weight of 284.34 (C16H20F2O4). The compound's ability to penetrate the blood-brain barrier is a key feature for its central nervous system activity. Specific PK parameters (e.g., half-life, Cmax) would be available from preclinical studies.
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| Toxicity/Toxicokinetics |
Foxicological data for FFPM are limited in publicly available sources. As a PDE4 inhibitor, potential adverse effects may include nausea, vomiting, and gastrointestinal disturbances, which are class effects of PDE4 inhibitors. The compound's central nervous system penetration may also result in neurological effects. Complete toxicology data would be available from preclinical development studies.
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| References |
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| Additional Infomation |
A PDE4 inhibitor; inhibits the activation of inflammasomes in microglia.
FFPM (CAS#: 1093412-18-0) is a selective, orally bioavailable, and blood-brain barrier permeable PDE4 inhibitor also known as Roflupram. It suppresses inflammasome activation in microglial cells by enhancing autophagy and reverses cognitive deficits in animal models. FFPM is not approved for clinical use and remains an investigational compound for neuroinflammatory and cognitive disorders. |
| Molecular Formula |
C16H20F2O4
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|---|---|
| Molecular Weight |
314.32
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| Exact Mass |
314.132
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| CAS # |
1093412-18-0
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| PubChem CID |
25147798
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| Appearance |
Colorless to light yellow liquid
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| LogP |
3.8
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
22
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| Complexity |
362
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C)CC(=O)C1=CC(=C(C=C1)OC(F)F)OC2CCOC2
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| InChi Key |
IXURVUHDDXFYDR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H20F2O4/c1-10(2)7-13(19)11-3-4-14(22-16(17)18)15(8-11)21-12-5-6-20-9-12/h3-4,8,10,12,16H,5-7,9H2,1-2H3
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| Chemical Name |
1-[4-(difluoromethoxy)-3-(oxolan-3-yloxy)phenyl]-3-methylbutan-1-one
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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) |
DMSO : ~100 mg/mL (~318.15 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.95 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 25.0 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: ≥ 2.5 mg/mL (7.95 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 25.0 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: ≥ 2.5 mg/mL (7.95 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 | 3.1815 mL | 15.9074 mL | 31.8147 mL | |
| 5 mM | 0.6363 mL | 3.1815 mL | 6.3629 mL | |
| 10 mM | 0.3181 mL | 1.5907 mL | 3.1815 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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