PDE/TRPA1/CHIT1-IN-1

PDE/TRPA1/CHIT1-IN-1 is a phosphodiesterases (PDEs), TRPA1, and hCHIT1 (KD of 37.7 μM) inhibitor. PDE/TRPA1/CHIT1-IN-1 is a broad-spectrum PDE inhibitor, potently targeting key isoforms including PDE4B, PDE7A, PDE3A, and PDE8A with IC50s of 15.54, 15.15, 8.39 and 16.46 μM. PDE/TRPA1/CHIT1-IN-1 suppresses NLRP3 inflammasome activation and inhibits NF-κB phosphorylation, downregulating the expression of pro-inflammatory genes (TNF-α and IL-6) in vivo. PDE/TRPA1/CHIT1-IN-1 can be used for chronic obstructive pulmonary disease (COPD) and related inflammatory lung disorders research[1].

Product Specifications

UNSPSC

12352005

Target

Interleukin Related; NF-κB; NOD-like Receptor (NLR) ; Phosphodiesterase (PDE) ; TNF Receptor; TRP Channel

Related Pathways

Apoptosis; Immunology/Inflammation; Membrane Transporter/Ion Channel; Metabolic Enzyme/Protease; Neuronal Signaling; NF-κB

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Smiles

O=C(OC(C)(C)C)C1=CC=C(NC(CCCN2C(NCC3=NC=CC=C3)=NC(N(C)C(N4C)=O)=C2C4=O)=O)C=C1

Molecular Formula

C28H33N7O5

Molecular Weight

547.61

References & Citations

[1]Chłoń-Rzepa G, er al. Purine-2,6-dione-based multitarget-directed ligands inhibiting PDE/TRPA1/CHIT1 as a new approach for the treatment of COPD. Bioorg Chem. 2025 Dec;167:109209.1