L791943
L791943 is a potent, selective Phosphodiesterase-4 (PDE4) inhibitor with an IC50 of 4.2 nM.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 192767-01-4
- 分子式: C24H17F10NO4
- 分子量:573.38
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
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] |
体外実験
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.
化学情報
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CAS 番号 192767-01-4
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分子量 573.38
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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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.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
L791943 関連分類
HY-U00254 関連分類
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