| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
The primary target of Oglemilast is phosphodiesterase-4 (PDE4). It acts as a potent and selective inhibitor of PDE4, with IC50 values of 2.5 nM for PDE4B and 1.7 nM for PDE4D. PDE4 is an enzyme that degrades cyclic AMP (cAMP) in immune and inflammatory cells. By inhibiting PDE4, Oglemilast increases cAMP levels, leading to anti-inflammatory effects.
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| ln Vitro |
Oglemilast (GRC 3886) has EC50 values of 11.4 nM and 4.4 nM, respectively, for PDE 4B1 and PDE 4D3 reporter cell lines [3].
In vitro, Oglemilast inhibits PDE4B and PDE4D with IC50s of 2.5 and 1.7 nM, respectively. It inhibits pulmonary cell infiltration, including eosinophilia and neutrophilia. Its activity is typically measured using PDE4 enzyme assays and cell-based inflammation models. |
| ln Vivo |
In vivo, Oglemilast is orally active and inhibits pulmonary cell infiltration. It has potential for the treatment of inflammatory airway diseases such as asthma and COPD. Its efficacy in animal models of airway inflammation has been demonstrated.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for Oglemilast involve PDE4 inhibition assays using purified PDE4B and PDE4D enzymes. The compound's inhibitory activity is measured by monitoring the hydrolysis of cAMP or a fluorescent substrate in the presence of the enzyme. IC50 values are determined from dose-response curves.
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| Cell Assay |
In vitro cellular assays for Oglemilast are conducted in immune and inflammatory cells, such as eosinophils or neutrophils. Cells are treated with the compound, and inflammatory mediator production (e.g., cytokines, chemokines) is measured. Its effects on cell infiltration and activation are assessed using chemotaxis assays or flow cytometry.
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| Animal Protocol |
In vivo animal studies for Oglemilast are conducted in animal models of airway inflammation, such as ovalbumin-induced asthma in mice or rats. Animals are administered the compound orally, and pulmonary cell infiltration (eosinophilia, neutrophilia) is assessed by bronchoalveolar lavage (BAL) fluid analysis. Airway hyperresponsiveness and inflammatory cytokine levels are also measured.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Oglemilast indicate it has a molecular weight of 516.3 and a molecular formula of C20H13Cl2F2N3O5S. It is orally active. Its solubility and other PK parameters would be determined in preclinical studies. The compound is typically stored as a powder at appropriate conditions.
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| Toxicity/Toxicokinetics |
Toxicological information for Oglemilast is derived from preclinical studies. As a PDE4 inhibitor, it may cause gastrointestinal side effects such as nausea and vomiting, which are common to this class of drugs. Comprehensive toxicology studies would be required for clinical development.
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| References |
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| Additional Infomation |
Oglemilast has been investigated for the treatment of lung diseases, including chronic obstructive pulmonary disease.
Oglemilast is a potent and orally active PDE4 inhibitor with potential for treating inflammatory airway diseases. It is also known as GRC-3886. It inhibits pulmonary cell infiltration, including eosinophilia and neutrophilia. It is available from research chemical suppliers for preclinical studies. It is not approved for clinical use. |
| Molecular Formula |
C20H13CL2F2N3O5S
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|---|---|
| Molecular Weight |
516.2968
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| Exact Mass |
514.992
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| CAS # |
778576-62-8
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| PubChem CID |
11387409
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| Appearance |
Light yellow to khaki solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
287.8±40.0 °C at 760 mmHg
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| Flash Point |
136.5±20.6 °C
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| Vapour Pressure |
0.0±0.6 mmHg at 25°C
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| Index of Refraction |
1.562
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| LogP |
1.66
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
33
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| Complexity |
810
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
OKFDRAHPFKMAJH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H13Cl2F2N3O5S/c1-33(29,30)27-9-2-4-14-11(6-9)16-10(3-5-15(18(16)31-14)32-20(23)24)19(28)26-17-12(21)7-25-8-13(17)22/h2-8,20,27H,1H3,(H,25,26,28)
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| Chemical Name |
N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)-8-(methanesulfonamido)dibenzofuran-1-carboxamide
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| Synonyms |
GRC3886; GRC-3886; GRC 3886
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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 : ~4 mg/mL (~7.75 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.4 mg/mL (0.77 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 4.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9369 mL | 9.6843 mL | 19.3686 mL | |
| 5 mM | 0.3874 mL | 1.9369 mL | 3.8737 mL | |
| 10 mM | 0.1937 mL | 0.9684 mL | 1.9369 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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