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=CC=CN=C24
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 |
|---|---|---|
| Elevated intracellular cyclic AMP inhibits chemotaxis in human eosinophils. | 1995 Jul |
|
| Activation and selective inhibition of a cyclic AMP-specific phosphodiesterase, PDE-4D3. | 1995 Oct |
|
| Role of phosphodiesterases in the regulation of gonadotropin- releasing hormone secretion in GT1 cells. | 1998 Dec |
|
| Comparison of recombinant human PDE4 isoforms: interaction with substrate and inhibitors. | 1998 Jun |
|
| Enhancement of motility and acrosome reaction in human spermatozoa: differential activation by type-specific phosphodiesterase inhibitors. | 1998 May |
|
| Phosphodiesterase 4-dependent regulation of cyclic AMP levels and leukotriene B4 biosynthesis in human polymorphonuclear leukocytes. | 1999 Feb 19 |
|
| AKAP3 selectively binds PDE4A isoforms in bovine spermatozoa. | 2006 Jan |
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
