PDE3/4-IN-4
PDE3/4-IN-4 is an orally active PDE3A and PDE4B inhibitor with IC50 values of 10 nM and 9.4 nM, respectively. PDE3/4-IN-4 shows selective activity relative to most other PDE family members. PDE3/4-IN-4 modulates the cAMP/PKA/CREB signaling pathway. PDE3/4-IN-4 inhibits pro-inflammatory factor IL-6. PDE3/4-IN-4 reduces expression of inflammatory markers in liver tissue. PDE3/4-IN-4 attenuates liver fibrosis. PDE3/4-IN-4 limits liver damage in cholestatic and sepsis-induced liver disease mice models. PDE3/4-IN-4 can be used for the research of liver injury, cholestatic liver diseases, sepsis-induced liver injury.
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- No. CAS: 3088024-27-2
- Fòrmula: C30H27F2N5O4
- Peso molecular:559.56
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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]|
PDE3A 10 nM (IC50) |
PDE4B 9.4 nM (IC50) |
PDE10A 477.9 nM (IC50) |
PDE6C 5739 nM (IC50) |
PDE1A >10000 nM (IC50) |
PDE2A >10000 nM (IC50) |
PDE5A >10000 nM (IC50) |
PDE7A >10000 nM (IC50) |
PDE8A >10000 nM (IC50) |
PDE11A >10000 nM (IC50) |
IL-6 |
In Vitro
PDE3/4-IN-4 (compound D5) (10-60 μM; 24 h) does not exhibit significant toxicity in LO2 human normal liver cells at concentrations up to 60 μM after 24 h treatment[1].
PDE3/4-IN-4 (compound D5) inhibits IL-6 secretion in Lipopolysaccharides (LPS) (HY-D1056)-stimulated LO2 cells with an IC50 of 14.89 μM[1].
PDE3/4-IN-4 (compound D5) (15 μM; 12 h pre-treatment before 4 h LPS stimulation) increases p-CREB and p-PKA expression in LPS-induced LO2 cells[1].
PDE3/4-IN-4 (compound D5) possesses adequate metabolic stability in mouse, rat, dog, monkey, and human liver microsomes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LPS-induced LO2 cells
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Concentration:15 μM (pre-treatment before LPS stimulation)
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Incubation Time:12 h (pre-treatment before 4 h LPS stimulation)
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Result:Markedly increased the expression of phosphorylated CREB (p-CREB) and phosphorylated PKA (p-PKA) compared to LPS-induced cells; confirmed increased p-CREB expression via immunofluorescence staining.
Parmacokinetics
In Vivo
PDE3/4-IN-4 (10-40 mg/kg; p.o.; daily; 7 days) reduces hepatic inflammation and injury in cecal ligation and puncture (CLP) mice, with 40 mg/kg being more effective[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 18-22 g, bile duct ligation surgery)[1]
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Dosage:10 mg/kg; 40 mg/kg
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Administration:p.o.; daily; 7 days
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Result:Significantly reduced hepatic mRNA expression of IL-6 and IL-1β; reduced total bile acid (TBA) and alanine aminotransferase (ALT) levels; partially restored liver architecture (HE staining); increased hepatic p-CREB and p-PKA expression; reduced collagen deposition (Masson staining, 40 mg/kg only); showed greater efficacy at 40 mg/kg.
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Animal Model:C57BL/6 (male, 18-22 g, cecal ligation and puncture surgery)[1]
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Dosage:10 mg/kg; 40 mg/kg
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Administration:p.o.; daily; 7 days
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Result:Reduced hepatic mRNA expression of IL-6 and IL-1β; reduced total bile acid (TBA), aspartate aminotransferase (AST), and alanine aminotransferase (ALT) levels; increased hepatic p-CREB and p-PKA expression; reduced hepatic inflammatory cell infiltration and restored hepatocyte structure (HE staining, 40 mg/kg only); reduced collagen deposition (Masson staining, 40 mg/kg only); showed greater efficacy at 40 mg/kg.
Chemical Information
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No. CAS 3088024-27-2
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Peso molecular 559.56
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Fòrmula C30H27F2N5O4
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SMILES
CC1CC(NN=C1C2=CC=C(C=C2)NC(C3=CC=CC4=C3N=C(N4)C5=CC(OCC6CC6)=C(C=C5)OC(F)F)=O)=O
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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)
PDE3/4-IN-4 Related Classifications
HY-181088 Related Classifications
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