2. Metabolic Enzyme/Protease Neuronal Signaling Membrane Transporter/Ion Channel Immunology/Inflammation NF-κB Apoptosis
  3. Phosphodiesterase (PDE) TRP Channel NOD-like Receptor (NLR) NF-κB TNF Receptor Interleukin Related
  4. 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.

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PDE/TRPA1/CHIT1-IN-1

PDE/TRPA1/CHIT1-IN-1 Chemical Structure

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PDE/TRPA1/CHIT1-IN-1 Related Antibodies

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Description

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].

IC50 & Target

PDE4B

15.54 μM (IC50)

PDE7A

15.15 μM (IC50)

PDE3A

8.39 μM (IC50)

PDE8A

16.64 μM (IC50)

PDE1B

54.47 μM (IC50)

PDE2A

79.61 μM (IC50)

PDE4D

130.50 μM (IC50)

PDE5A

26.86 μM (IC50)

PDE10A

36.13 μM (IC50)

In Vitro

PDE/TRPA1/CHIT1-IN-1 (compound 39) (10 μM, 1 h) possesses anti-inflammatory activity in Lipopolysaccharides (LPS) (HY-D1056)-stimulated RAW264.7 macrophages[1].
PDE/TRPA1/CHIT1-IN-1 inhibits PDE1B, PDE2A, PDE4B, PED7A, PDE3A, PDE4D, PDE5A, PDE8A and PDE10A with IC50s of 54.47, 79.61, 15.54, 15.15, 8.39, 130.50, 26.86, 16.46 and 36.13 μM, respectively[1].
PDE/TRPA1/CHIT1-IN-1 (1-50 μM, 1 h) inhibits bronchial smooth muscle cell (BSMC) hyperplasia and hypertrophy, reduces extracellular matrix (ECM) component secretion in both BSMC and human lung fibroblast cell line (MRC-5) cells, and inhibits the fibroblast-to-myofibroblast transition[1].
PDE/TRPA1/CHIT1-IN-1 shows bronchorelaxant effects with IC50 values of 1.56 μM, and maximal relaxation of precontracted tracheal segments with the maximal relaxation of 100 % in rat tracheal segments[1].
PDE/TRPA1/CHIT1-IN-1 possesses high metabolic stability (t₁/₂ = 53.42 min, Clint = 32.43 μL/min/mg), negligible hepatocytotoxicity (IC50 = 34.70 μM in HepG2 cells), and medium membrane permeability (logPe = -5.305)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PDE/TRPA1/CHIT1-IN-1 Related Antibodies

ELISA Assay[1]

Cell Line: LPS-stimulated RAW264.7 macrophages
Concentration: 10 μM
Incubation Time: 1 h
Result: Caused an almost twofold reduction in TNF-α and IL-6 levels in LPS-induced RAW264.7 cells, lowering TNF-α concentrations to 381.74 pg/mL and decreasing IL-6 concentrations to 141.02 pg/mL.

Cell Proliferation Assay[1]

Cell Line: FBS induced-MRC-5, FBS induced-BSMC, TGF-β induced- MRC-5 and TGF-β induced-BSMC
Concentration: 1, 10 and 50 μM
Incubation Time: 1 h
Result: Reduced BSMC and MRC-5 proliferation by 38 % and 32 % at a concentration of 10 μM.
Reduced TGF-β-induced expression of COL1A1 and FN1 genes in both cell lines.
Decreased TGF-β-induced ACTA2 expression in BSMCs by almost a 3-fold.
Reduce TGF-β-induced ACTA2 expression in lung fibroblasts.
In Vivo

PDE/TRPA1/CHIT1-IN-1 (compound 39) (25 mg/kg, i.p., once daily, for 2 weeks) shows anti-inflammatory properties and regulates the NLRP3 inflammasome in elastase-induced pulmonary emphysema model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: PPE (HY-B2118) (intranasally,i.n. once a week for 4 week) induced-Balb/c male mice (8-10 weeks, 23-25 g)[1]
Dosage: 25 mg/kg
Administration: i.p., once daily; for 2 weeks
Result: Protected against elastase-induced emphysema with a mean linear intercept (MLI) values of 50.36 μM.
Ameliorated the elastase-induced increase in total inflammatory cells in in bronchoalveolar lavage fluid (BALF).
Reduced the total number of all inflammatory cells in BALF collected from the PPE-induced model.
Acted as a relatively strong inhibitor of PDE7A and PDE3A, as well as a TRPA1 antagonist.
Reduced the PPE-induced transcript levels of key inflammatory genes in lung homogenates to control levels.
Decrease in Tnfa, Cxcl2, Il6, and Il1b expression.
Limited the levels of NLRP3 inflammasome components and consequently reduced the activation of NLRP3 inflammasome components.
Reduced the PPE-induced level of cleaved caspase-1, which may have inhibited the formation of interleukin 1β (IL-1β), a hallmark cytokine of NLRP3 inflammasome activation.
Reduced NF-κB phosphorylation, as well as the expression of various proinflammatory genes, including Tnfa, Cxcl2, Il6, and Il1b.
Molecular Weight

547.61

Formula

C28H33N7O5
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
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
References
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PDE/TRPA1/CHIT1-IN-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PDE/TRPA1/CHIT1-IN-1Phosphodiesterase (PDE)TRP ChannelNOD-like Receptor (NLR)NF-κBTNF ReceptorInterleukin RelatedTransient receptor potential channelsNuclear factor-κBNuclear factor-kappaBTumor Necrosis Factor ReceptorTNFRILPDEsTRPA1hCHIT1NLRP3TNF-αIL-6COPDlung diseaseInhibitorinhibitorinhibit

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