AN-2898
AN-2898 is a selective PDE4 inhibitor with IC50 of 0.027 μM over other phosphodiesterase enzymes, such as PDE1A, PDE2A and PDE3A. AN-2898 also potently inhibits PDE4 subtypes (PDE4B1, PDE4A1A and PDE4D2). AN-2898 significantly inhibits the production of TNF-α, IL-2, IFN-γ, IL-5 and IL-10. AN-2898 can be used for mild to moderate atopic dermatitis (AD) and psoriasis research.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 906673-33-4
- Formel: C15H9BN2O3
- Molecular Weight:276.05
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
PDE1A 1.7 μM (IC50) |
PDE2A 9.8 μM (IC50) |
PDE3A 4.12 μM (IC50) |
PDE4 0.027 μM (IC50) |
PDE7A 0.21 μM (IC50) |
PDE4B1 0.24 μM (IC50) |
PDE4A1 0.35 μM (IC50) |
PDE4D2 0.84 μM (IC50) |
IL-2 |
IL-10 |
IL-5 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf9 | IC50 |
0.24 μM
Compound: 19
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Inhibition of human PDE4B1 expressed in baculovirus infected sf9 cells incubated for 30 mins
Inhibition of human PDE4B1 expressed in baculovirus infected sf9 cells incubated for 30 mins
|
[PMID: 26908025] |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 906673-33-4
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Appearance Solid
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Molecular Weight 276.05
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Formel C15H9BN2O3
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Color White to off-white
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SMILES
N#CC1=CC=C(OC2=CC=C(B(O)OC3)C3=C2)C=C1C#N
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Protokoll
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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
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)