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
- 화학식: C24H17F10NO4
- 분자량:573.38
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
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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분자량 573.38
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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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.
순도&문서
References
[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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