Roflupram
Based on 1 publication(s) in Google Scholar
Roflupram is a selective, orally active and brain-penetrant PDE4 inhibitor, with an IC50 of 26.2 nM for core catalytic domains of human PDE4. Roflupram can reverse cognitive deficits and reduce the production of pro-inflammatory factors.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.45%
- No. CAS: 1093412-18-0
- Fòrmula: C16H20F2O4
- Peso molecular:314.32
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Almacenamiento:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Immunology/Inflammation Compound Library
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Publications Citing Use of MedChemExpress (MCE) Roflupram
More
Actividad biológica
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PDE4 26.2 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PBMC | IC50 |
40 nM
Compound: 5v
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Inhibition of LPS-induced TNFalpha production in human PBMC
Inhibition of LPS-induced TNFalpha production in human PBMC
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[PMID: 19049349] |
Chemical Information
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No. CAS 1093412-18-0
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Appearance Liquid (Density: 1.181±0.06 g/cm3)
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Peso molecular 314.32
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Fòrmula C16H20F2O4
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Color Colorless to light yellow
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SMILES
CC(CC(C1=CC=C(C(OC2COCC2)=C1)OC(F)F)=O)C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Toxicology
Upregulation of postsynaptic cAMP/PKA/CREB signaling alleviates copper(Ⅱ)-induced oxidative stress and pyroptosis in MN9D cells. [Abstract]2023 Aug 1:494:153582. PMID: 37353053
Solvente y solubilidad
DMSO : 100 mg/mL (318.15 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.95 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.95 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Li D, et, al. Roflupram, a novel phosphodiesterase 4 inhibitor, inhibits lipopolysaccharide-induced neuroinflammatory responses through activation of the AMPK/Sirt1 pathway. Int Immunopharmacol. 2021 Jan;90:107176. [Content Brief]
[2]. You T, et, al. Roflupram, a Phosphodiesterase 4 Inhibitior, Suppresses Inflammasome Activation through Autophagy in Microglial Cells. ACS Chem Neurosci. 2017 Nov 15;8(11):2381-2392. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1815 mL | 15.9074 mL | 31.8147 mL | 79.5368 mL |
| 5 mM | 0.6363 mL | 3.1815 mL | 6.3629 mL | 15.9074 mL | |
| 10 mM | 0.3181 mL | 1.5907 mL | 3.1815 mL | 7.9537 mL | |
| 15 mM | 0.2121 mL | 1.0605 mL | 2.1210 mL | 5.3025 mL | |
| 20 mM | 0.1591 mL | 0.7954 mL | 1.5907 mL | 3.9768 mL | |
| 25 mM | 0.1273 mL | 0.6363 mL | 1.2726 mL | 3.1815 mL | |
| 30 mM | 0.1060 mL | 0.5302 mL | 1.0605 mL | 2.6512 mL | |
| 40 mM | 0.0795 mL | 0.3977 mL | 0.7954 mL | 1.9884 mL | |
| 50 mM | 0.0636 mL | 0.3181 mL | 0.6363 mL | 1.5907 mL | |
| 60 mM | 0.0530 mL | 0.2651 mL | 0.5302 mL | 1.3256 mL | |
| 80 mM | 0.0398 mL | 0.1988 mL | 0.3977 mL | 0.9942 mL | |
| 100 mM | 0.0318 mL | 0.1591 mL | 0.3181 mL | 0.7954 mL |
Roflupram Related Classifications
HY-115383 Related Classifications
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