PDE4D inhibitor 1
PDE4-IN-1 is a PDE4 inhibitor with high potency (IC50 : 8.6 nM) and selectivity over other PDE subtypes. PDE4-IN-1 inhibits the release of inflammatory cytokines and chemokines. PDE4-IN-1 greatly restores impaired cAMP-CREB signaling pathway. PDE4-IN-1 inhibits proliferation and promotes differentiation to reverse the formation of psoriasis.
For research use only. We do not sell to patients.
- Formula: C25H25F2NO7
- Molecular Weight:489.47
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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PDE4B1 5.3 nM (IC50) |
PDE4D2 8.6 nM (IC50) |
PDE4A10 100 nM (IC50) |
PDE4C1 747 nM (IC50) |
PDE5A1 1730 nM (IC50) |
PDE10A2 1953 nM (IC50) |
PDE7A1 5913 nM (IC50) |
PDE1B2 >10000 nM (IC50) |
PDE2A >10000 nM (IC50) |
PDE3A >10000 nM (IC50) |
PDE8A1 >10000 nM (IC50) |
PDE9A2 >10000 nM (IC50) |
PDE4-IN-1 (Compound L30) (5-20 μM, 2 h) reduces the mRNA levels of the inflammatory cytokines (IL-1β , IL-6, and TNF-α) in LPS-induced Raw264.7 cells[1].
PDE4-IN-1 (5-20 μM, 24 h) reduces the mRNA levels of the inflammatory cytokines (CXCL-2, IL-17, and TNF-α) in M5-stimulated HaCaT cells[1].
PDE4-IN-1 (0-20 μM, 24 h) inhibits the proliferation of M5-stimulated HaCaT cells[1].
PDE4-IN-1 (20 μM, 24 h) decreases the protein expressions of K6 and K17 whilst upregulating the expression of differentiation protein (K1 and K10) in M5-stimulated HaCaT cells[1].
PDE4-IN-1 (20 μM, 2 h) with Roflumilast (HY-15455) restores cAMP levels and enhances phosphorylation of downstream CREB in M5-stimulated HaCaT cells[1].
PDE4-IN-1 (0-80 μM, 24 h) shows low cytotoxicities for RAW264.7 and HaCaT cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c mice models (6-8 weeks old, weighing 20-22 g each, a total of 40 mice) with 5% IMQ-containing cream for 7 days [1]
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Dosage:0.3% ointment-100 mg
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Administration:Topical administrations
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Result:Alleviated psoriatic symptoms and was more potent to decrease the thickness, scales, and erythema scores than Roflumilast (20 mg/kg) in the last 4 days.
Downregulated inflammatory cytokines and chemotaxis such as TNF-α, IL-1β, IL-6, IL-17, CXCL-2, and CCL-20.
Reduced protein expression of K6 and K17.
Reversed expression level of K1 and K10.
Exerted antipsoriasis effects by inhibiting the excessive proliferation and promoting poor differentiation.
Partly reversed the body weight loss and reduced skin thickness induced by IMQ suggesting low risk of toxicity in vivo.
Chemical Information
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Molecular Weight 489.47
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Formula C25H25F2NO7
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SMILES
COC([C@H]1C[C@@H](OC2=C3OC(C4=CC=C(OC(F)F)C(OCC5CC5)=C4)=CC3=CC=C2O)CN1)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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