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
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
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PDE4 |
Cellular Effect
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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] |
In Vitro
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. Further protocols information, click here.
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.
Protocole
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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.
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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