PDE4-IN-29
PDE4-IN-29 (Compound 55) is an orally active and selective PDE4 inhibitor (including subtypes such as PDE4A1, PDE4B2, PDE4D3) with IC50s of <5 nM against PDE4D3. PDE4-IN-29 inhibits the degradation of cyclic adenosine monophosphate (cAMP), increases intracellular cAMP levels, suppressing the release of inflammatory factors such as TNF-α. PDE4-IN-29 is promising for research of inflammatory diseases including psoriasis, atopic dermatitis, and chronic obstructive pulmonary disease.
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- CAS No.: 2815361-45-4
- Formule: C27H34N2O8S
- Masse moléculaire:546.63
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
IC50 & Target
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PDE4A1 |
PDE4B2 |
PDE4D3 |
Chemical Information
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CAS No. 2815361-45-4
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Masse moléculaire 546.63
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Formule C27H34N2O8S
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SMILES
O=C1N([C@@H](C2=CC(OCC)=C(OC)C=C2)CS(C)(=O)=O)C(C3=C(NC(C)=O)C=CC(C(CCCC)O)=C31)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Imiquimod-Induced Psoriasiform Dermatitis
Imiquimod (IMQ)-induced psoriasiform dermatitis is a widely used murine model in which topical application of IMQ, a Toll-like receptor 7 (TLR7) agonist, triggers innate immune activation in the skin and induces a psoriasis-like inflammatory cascade characterized by epidermal hyperplasia, immune cell infiltration, and cytokine production dominated by the IL-23/IL-17 axis. This inflammatory response is mediated through activation of dendritic cells and downstream induction of IL-23, IL-17A, IL-22, and related pro-inflammatory mediators, recapitulating key features of human plaque psoriasis and enabling mechanistic and therapeutic studies. The model is commonly induced using Aldara (5% IMQ cream) applied topically to murine skin, resulting in rapid onset of erythema, scaling, and thickening that can be quantified as disease severity indices and validated histologically.
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TPA/Croton Oil Ear Edema and Dermatitis
The TPA (12-O-tetradecanoylphorbol-13-acetate) and croton oil-induced mouse ear edema model is a well-established acute cutaneous inflammation system used to evaluate topical anti-inflammatory activity by measuring edema formation, neutrophil infiltration, vascular permeability, and cytokine-mediated skin responses in vivo. The inflammatory response is triggered by topical application of phorbol esters (TPA) or croton oil constituents, leading to rapid activation of protein kinase C signaling, leukocyte recruitment, and increased vascular permeability, which can be quantified by ear thickness, weight, dye extravasation, and biochemical markers such as myeloperoxidase (MPO) activity and pro-inflammatory mediators in ear tissue homogenates. This model is widely used for screening anti-inflammatory agents, where reductions in edema and inflammatory biomarkers reflect suppression of acute dermal inflammation and immune cell infiltration. Histological evaluation typically confirms epidermal
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)