PDE4-IN-30
PDE4-IN-30 is a selective PDE4 inhibitor with an IC50 of 2.7 nM for PED4D2, targeting PDE4 through halogen bonding and metal coordination. PDE4-IN-30 exhibits at least 67-fold selectivity for other PDE subfamilies. PDE4-IN-30 can be used for the research of idiopathic pulmonary fibrosis.
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。
- 分子式: C14H17BrN8O2
- 分子量:409.24
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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
[1]|
PDE4D2 2.7 nM (IC50) |
PDE10A 181.8 nM (IC50) |
PDE8A 1156 nM (IC50) |
PDE5A 7491 nM (IC50) |
体外実験
PDE4-IN-30 (compound 13c) (5-20 μM; 48 hours) effectively inhibits TGF-β1-induced fibroblast-to-myofibroblast transition (FMT) and epithelial-mesenchymal\r
transition (EMT) in MRC-5 and A549 cells[1].
PDE4-IN-30 (5-20 μM; 48 hours) significantly attenuates TGF-β1-induced A549 cell proliferation and cell migration[1].
PDE4-IN-30 exhibits good cell permeability and favorable drug-likeness properties in Caco-2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MRC-5 and A549 cell lines
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Concentration:5 μM, 10 μM, 20 μM
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Incubation Time:48 h
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Result:Significantly inhibited the overexpression of α-smooth muscle actin (α-SMA), COL1A1, and FN markers.
Downregulatedthe expression of N-cadherin and vimentin while it restored E-cadherin. expression to baseline levels.
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Cell Line:A549 cell lines
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Concentration:5 μM, 10 μM, 20 μM
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Incubation Time:48 h
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Result:Significantly attenuated TGF-β1-induced A549 cell proliferation and migration.
Parmacokinetics
| Species | Dose | Route | Note | Cmax | Tmax | T1/2 | AUC0-t | CL |
|---|---|---|---|---|---|---|---|---|
| Mice | 2.5 mg/kg | i.v. | 文献审核 | 104 ng/mL | 0.0833 h | 0.0737 h | 25.8 ng·h/mL | 110268 mL/h/kg |
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6J (6-8 weeks old; 18-22 g) were induced by a single intratracheal instillation of BLM (3 mg/kg)[1]
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Dosage:2.5 mg/kg
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Administration:Intraperitoneal injection; 3 weeks of treatment starting from the second day post-BLM induction
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Result:Significantly reduced lung coefficient, hydroxyproline levels, and fibrotic markers (FN1, COL1A1, α-SMA, N-cadherin, vimentin) while increasing E-cadherin expression.
Improved lung function parameters (inspiratory capacity (IC), forced vital capacity (FVC), lung compliance (Cchord), vital capacity (VC), peakexpiratory flow (PEF)) and reduced airway resistance.
Histological analysis showed reduced alveolar fibrosis and inflammatory infiltration.
化学情報
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分子量 409.24
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分子式 C14H17BrN8O2
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SMILES
NC1=C(C(NCCCC(NO)=O)=NC2=C(C=NN12)C3=CN(N=C3)C)Br
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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.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
PDE4-IN-30 関連分類
HY-179639 関連分類
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