AhR/PDE4 modulator-1
AhR/PDE4 modulator-1 is a AhR/PDE4D dual-target modulator, with an AhR agonistic EC50 of 0.11 μM and a PDE4D inhibitory IC50 of 2.12 μM. AhR/PDE4 modulator-1 activates the AhR-CYP1A1 signaling pathway, promotes AhR nuclear translocation, and upregulates downstream CYP1A1; it inhibits PDE4D activity, elevates intracellular cAMP levels, and activates the downstream cAMP-PKA-CREB signaling pathway. Topical administration of AhR/PDE4 modulator-1 exerts anti-inflammatory effects in the Imiquimod (HY-B0180)-induced psoriasis-like mouse model, alleviates epidermal hyperplasia and inflammatory infiltration, and suppresses the expression of IL-17A/F. AhR/PDE4 modulator-1 can be used in research related to psoriasis.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Fòrmula: C20H14O4
- Peso molecular:318.32
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
PDE4D 2.12 μM (IC50) |
CYP1A1 |
IL-17A |
IL-17F |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | EC50 |
0.11 μM
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AhR agonistic activity in HepG2-Lucia AhR reporter cells incubated for 24 h measured via luciferase activity quantification in supernatants.
AhR agonistic activity in HepG2-Lucia AhR reporter cells incubated for 24 h measured via luciferase activity quantification in supernatants.
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42570412 |
In Vitro
AhR/PDE4 modulator-1 (0.1-20 μM; 1.5 h) promotes the concentration-dependent translocation of AhR from the cytoplasm to the nucleus in HaCaT cells[1].
AhR/PDE4 modulator-1 (1 μM; 24 h) activates the AhR-CYP1A1 signaling axis in HaCaT cells by upregulating the expression of AhR and its downstream CYP1A1 gene[1].
AhR/PDE4 modulator-1 (0.1-10 μM; 30 min) elevates cAMP levels in LPS-stimulated RAW 264.7 cells in a dose-dependent manner in vitro[1].
AhR/PDE4 modulator-1 (0.01-10 μM; 1.5 h) elevates the protein level of p-CREB in LPS-stimulated RAW 264.7 cells, without altering the expression of total CREB[1].
AhR/PDE4 modulator-1 (10 μM; 24 h) effectively inhibits the transcript expression of the pro-inflammatory cytokines Tnf-α and Il-6 in LPS-stimulated RAW 264.7 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Immortalized human HaCaT keratinocyte cells
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Concentration:0.1, 1, 10, 20 μM
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Incubation Time:1.5 h
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Result:Induced concentration-dependent nuclear translocation of AhR, with reduced AhR protein levels in the cytoplasmic fraction and correspondingly increased AhR protein levels in the nuclear fraction as concentration increased.
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Cell Line:HaCaT cells
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Concentration:1 μM
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Incubation Time:24 h
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Result:Induced a 2-fold increase in AhR mRNA levels and a 6-fold increase in CYP1A1 mRNA levels compared to vehicle control at 1 μM concentration.
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Cell Line:LPS-stimulated RAW 264.7 mouse macrophage cells
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Concentration:0.1, 1, 10 μM
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Incubation Time:30 min
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Result:Increased intracellular cAMP levels at concentrations as low as 0.1 μM, producing a dose-dependent rise in intracellular cAMP concentrations.
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Cell Line:LPS-stimulated RAW 264.7 mouse macrophage cells
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Concentration:0.01, 0.1, 1, 10 μM
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Incubation Time:1.5 h
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Result:Left total CREB protein expression unchanged across all conditions, while robustly elevating LPS-induced low baseline p-CREB levels across the 0.01 to 10 μM concentration range.
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Cell Line:LPS-stimulated RAW 264.7 cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Inhibited the transcript expression of the pro-inflammatory cytokines Tnf-α and Il-6 in LPS-stimulated RAW 264.7 cells.
Parmacokinetics
| Species | Dose | Route | Cmax | Tmax | T1/2 | AUC0-∞ |
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| Mice[1] | 10 mg/kg | p.o. | 6.38 nM | 1.00 h | 0.89 h | 30.08 nM·h |
In Vivo
AhR/PDE4 modulator-1 (10 mg/kg; p.o.; single administration) exhibits rapid absorption characteristics in female BALB/c mice, with a short terminal elimination half-life of only 0.89 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice (Female, 6-8 weeks old)[1]
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Dosage:1% (topical); 20 mg/kg (p.o.)
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Administration:topical; daily; 7 days
p.o.; daily; 7 days -
Result:Reduced macroscopic psoriasis-like skin appearance, epidermal thickening, and total PASI scores.
Suppressed IMQ-induced upregulation of pro-inflammatory cytokines Il-17a and Il-17f in lesional skin.
Attenuated the elevated spleen index caused by systemic inflammation.
Showed no significant anti-psoriasis effects in the 20 mg/kg oral group.
Caused no notable body weight loss across all groups.
Chemical Information
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Peso molecular 318.32
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Fòrmula C20H14O4
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SMILES
O=C1C=CC2=CC3=C(OC=C3)C(OCC(C4=CC=CC=C4)=C)=C2O1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AhR/PDE4 modulator-1 Related Classifications
HY-189218 Related Classifications
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Keywords
- AhR/PDE4 modulator-1
- Aryl Hydrocarbon Receptor
- Phosphodiesterase (PDE)
- Cytochrome P450
- Interleukin Related
- Epigenetic Reader Domain
- AhR
- CYPs
- IL
- HepG2-Lucia? AhR reporter cells
- HaCaT cells
- PDE4D2 enzyme
- imiquimod-induced psoriasis-like mouse model
- phosphodiesterase 4D
- RAW 264.7 cells
- BALB/c mice
- AhR-CYP1A1 signaling
- aryl hydrocarbon receptor
- IL-17A/F
- Inhibitor
- inhibitor
- inhibit