LEO 29102
LEO 29102 is a potent phosphodiesterase 4 (PDE4) inhibitor with an IC50 value of 5 nM. LEO 29102 inhibits TNFα release. LEO 29102 has the potential for the research of atopic dermatitis.
For research use only. We do not sell to patients.
- CAS No.: 1035572-38-3
- Formula: C20H22Cl2N2O5
- Molecular Weight:441.31
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
PDE4 5 nM (IC50) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| PBMC | IC50 |
16 nM
Compound: 20
|
Inhibition of LPS-induced TNFalpha release in human PBMC preincubated for 30 mins before LPS stimulation measured after 18 hrs by TR-FRET assay
Inhibition of LPS-induced TNFalpha release in human PBMC preincubated for 30 mins before LPS stimulation measured after 18 hrs by TR-FRET assay
|
[PMID: 24984230] |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 1035572-38-3
-
Molecular Weight 441.31
-
Formula C20H22Cl2N2O5
-
SMILES
COC1=C(C=CC(C(CC2=C(C=NC=C2Cl)Cl)=O)=C1OCC(NCCC)=O)OC
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
-
TPA/Croton Oil Ear Edema and Dermatitis
The TPA (12-O-tetradecanoylphorbol-13-acetate) and croton oil-induced mouse ear edema model is a well-established acute cutaneous inflammation system used to evaluate topical anti-inflammatory activity by measuring edema formation, neutrophil infiltration, vascular permeability, and cytokine-mediated skin responses in vivo. The inflammatory response is triggered by topical application of phorbol esters (TPA) or croton oil constituents, leading to rapid activation of protein kinase C signaling, leukocyte recruitment, and increased vascular permeability, which can be quantified by ear thickness, weight, dye extravasation, and biochemical markers such as myeloperoxidase (MPO) activity and pro-inflammatory mediators in ear tissue homogenates. This model is widely used for screening anti-inflammatory agents, where reductions in edema and inflammatory biomarkers reflect suppression of acute dermal inflammation and immune cell infiltration. Histological evaluation typically confirms epidermal
Purity & Documentation
References
[1]. Felding J, et al. Discovery and early clinical development of 2-{6-[2-(3,5-dichloro-4-pyridyl)acetyl]-2,3-dimethoxyphenoxy}-N-propylacetamide (LEO 29102), a soft-drug inhibitor of phosphodiesterase 4 for topical treatment of atopic dermatitis. J Med Chem. 2014 Jul 24;57(14):5893-903. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)