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Cat. No.: HY-189218

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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.

For research use only. We do not sell to patients.

Formula: C₂₀H₁₄O₄
Molecular Weight:318.32

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

AhR/PDE4 modulator-1 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

PDE4D

2.12 μM (IC₅₀)

CYP1A1

IL-17A

IL-17F

All Phosphodiesterase (PDE) Isoforms :

All Cytochrome P450 Isoforms :

All Interleukin Related Isoforms :

All Epigenetic Reader Domain Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	EC50	0.11 μM	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.	42570412

In Vitro

AhR/PDE4 modulator-1 (compound T29) exhibits potent AhR agonistic activity in HepG2-Lucia™ AhR reporter cells with an EC₅₀ of 0.11 μM, effectively inhibits purified PDE4D2 enzyme with an IC₅₀ of 2.12 μM, and shows high binding affinity for purified AhR protein with a K_d of 0.07 μM^[1].
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.

Western Blot Analysis^[1]

Cell Line:

Immortalized human HaCaT keratinocyte cells
Concentration:

0.1, 1, 10, 20 μM
Incubation Time:

1.5 h
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.

Real Time qPCR^[1]

Cell Line:

HaCaT cells
Concentration:

1 μM
Incubation Time:

24 h
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.

ELISA Assay^[1]

Cell Line:

LPS-stimulated RAW 264.7 mouse macrophage cells
Concentration:

0.1, 1, 10 μM
Incubation Time:

30 min
Result:

Increased intracellular cAMP levels at concentrations as low as 0.1 μM, producing a dose-dependent rise in intracellular cAMP concentrations.

Western Blot Analysis^[1]

Cell Line:

LPS-stimulated RAW 264.7 mouse macrophage cells
Concentration:

0.01, 0.1, 1, 10 μM
Incubation Time:

1.5 h
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.

RT-PCR^[1]

Cell Line:

LPS-stimulated RAW 264.7 cells
Concentration:

10 μM
Incubation Time:

24 h
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	C_max	T_max	T_1/2	AUC_0-∞
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 (compound T29) (1% / 20 mg/kg; topical administration / p.o.; once daily; 7 days) effectively ameliorates psoriasis-like pathological symptoms, including epidermal hyperplasia, inflammatory infiltration and elevated pro-inflammatory cytokine levels, in the Imiquimod (HY-B0180)-induced mouse model of psoriasis^[1].
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.

Animal Model:

BALB/c mice (Female, 6-8 weeks old)^[1]
Dosage:

1% (topical); 20 mg/kg (p.o.)
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

Molecular Weight 318.32
Formula C₂₀H₁₄O₄
SMILES

O=C1C=CC2=CC3=C(OC=C3)C(OCC(C4=CC=CC=C4)=C)=C2O1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Xian Y, et al. Structural modification of imperatorin affords promising dual AhR/PDE4 modulators for anti-inflammatory therapy. European journal of medicinal chemistry. 2026 Nov 15;318:119183.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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