Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C19H13N5O4 |
| Molecular Weight | 375.3376 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
[O-][N+](=O)C1=CC(=CC=C1)N2C(=O)N(CC3=CC=NC=C3)C(=O)C4=C2N=CC=C4
InChI
InChIKey=YLHRMVRLIOIWTO-UHFFFAOYSA-N
InChI=1S/C19H13N5O4/c25-18-16-5-2-8-21-17(16)23(14-3-1-4-15(11-14)24(27)28)19(26)22(18)12-13-6-9-20-10-7-13/h1-11H,12H2
DescriptionCurator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/8562314 | https://www.ncbi.nlm.nih.gov/pubmed/16177223 | https://www.ncbi.nlm.nih.gov/pubmed/10079010
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/8562314 | https://www.ncbi.nlm.nih.gov/pubmed/16177223 | https://www.ncbi.nlm.nih.gov/pubmed/10079010
RS25344 is a potent and selective phosphodiesterase (PDE) 4 inhibitor. It preferentially inhibits phosphorylated PDE4D. The compound demonstrated efficacy in animal models of inflammation and anaphylaxis. RS25344 inhibited eosinophil chemotaxis, increased the progressive motility of bovine spermatozoa, inhibited leukotriene B4 biosynthesis by human polymorphonuclear leukocytes.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
| 9.3 null [pIC50] | |||
Target ID: CHEMBL291 |
7.7 null [pIC50] | ||
Target ID: CHEMBL275 |
7.5 null [pIC50] | ||
Target ID: CHEMBL254 |
7.8 null [pIC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
|||
| Primary | Unknown Approved UseUnknown |
PubMed
| Title | Date | PubMed |
|---|---|---|
| AKAP3 selectively binds PDE4A isoforms in bovine spermatozoa. | 2006-01 |
|
| Phosphodiesterase 4D forms a cAMP diffusion barrier at the apical membrane of the airway epithelium. | 2005-03-04 |
|
| Anti-inflammatory potential of the selective phosphodiesterase 4 inhibitor N-(3,5-dichloro-pyrid-4-yl)-[1-(4-fluorobenzyl)-5-hydroxy-indole-3-yl]-glyoxylic acid amide (AWD 12-281), in human cell preparations. | 2004-02 |
|
| Occupancy of the catalytic site of the PDE4A4 cyclic AMP phosphodiesterase by rolipram triggers the dynamic redistribution of this specific isoform in living cells through a cyclic AMP independent process. | 2003-10 |
|
| Phosphodiesterase 4-dependent regulation of cyclic AMP levels and leukotriene B4 biosynthesis in human polymorphonuclear leukocytes. | 1999-02-19 |
|
| Role of phosphodiesterases in the regulation of gonadotropin- releasing hormone secretion in GT1 cells. | 1998-12 |
|
| Comparison of recombinant human PDE4 isoforms: interaction with substrate and inhibitors. | 1998-06 |
|
| Enhancement of motility and acrosome reaction in human spermatozoa: differential activation by type-specific phosphodiesterase inhibitors. | 1998-05 |
|
| Activation and selective inhibition of a cyclic AMP-specific phosphodiesterase, PDE-4D3. | 1995-10 |
|
| Elevated intracellular cyclic AMP inhibits chemotaxis in human eosinophils. | 1995-07 |
Sample Use Guides
RS25344 attenuated ear oedema in mice with ED50 0.02 mg/kg
RS25344 attenuated anaphylaxis in guinea pigs with ED50 0.5 mg/kg
Route of Administration:
Oral
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152814-89-6
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DTXSID70934606
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9842556
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7KKH9V6X32
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ACTIVE MOIETY
