L791943
L791943 is a potent, selective Phosphodiesterase-4 (PDE4) inhibitor with an IC50 of 4.2 nM.
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- CAS No.: 192767-01-4
- Formule: C24H17F10NO4
- Masse moléculaire:573.38
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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PDE4 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf9 | IC50 |
4.2 nM
Compound: 11n, (L-791943)
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Inhibitory concentration against human PDE4A isoform using a construct representing the common region of spliced variants expressed as GST-fusion protein in Sf9 cells
Inhibitory concentration against human PDE4A isoform using a construct representing the common region of spliced variants expressed as GST-fusion protein in Sf9 cells
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[PMID: 12031319] |
| Sf9 | IC50 |
4.2 nM
Compound: L-791943
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Inhibition of human Phosphodiesterase 4A isoform using construct representing the common region of spliced variants expressed as GST-fusion proteins in Sf9 cells.
Inhibition of human Phosphodiesterase 4A isoform using construct representing the common region of spliced variants expressed as GST-fusion proteins in Sf9 cells.
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[PMID: 12270195] |
| Sf9 | IC50 |
4.2 nM
Compound: L-791943(1)
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Inhibitory activity against human PDE4A expressed isoform using construct representing the common region of spliced variants as GST-fusion protein in Sf9 cells.
Inhibitory activity against human PDE4A expressed isoform using construct representing the common region of spliced variants as GST-fusion protein in Sf9 cells.
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[PMID: 12639571] |
The extent of metabolism of L791943 is evaluated in vitro in rat hepatocytes and compared to the data obtaine with CDP-840. In our standard incubation conditions, >98% of the parent drug remain in the case of L791943 whereas only 11% of CDP-840 is left intact[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 192767-01-4
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Masse moléculaire 573.38
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Formule C24H17F10NO4
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SMILES
O=N1=CC=C(C=C1)CC(C2=CC=C(C(C(F)(F)F)(O)C(F)(F)F)C=C2)C3=CC(OC(F)F)=C(OC(F)F)C=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Richard Frenette, et al. Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters. Bioorg Med Chem Lett. 2002 Oct 21;12(20):3009-13. [Content Brief]
[2]. Guay D, et al. Discovery of L-791,943: a potent, selective, non emetic and orally active phosphodiesterase-4 inhibitor. Bioorg Med Chem Lett. 2002 Jun 3;12(11):1457-61. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
L791943 Related Classifications
HY-U00254 Related Classifications
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