PDE1-IN-7
PDE1-IN-7 (Compound 13h) is a selective inhibitor of bPDE1 (IC50= 10 nM). PDE1-IN-7 exhibits significant anti-fibrotic effects in a BDL-induced liver fibrosis rat model. PDE1-IN-7 can be used for research in liver fibrosis.
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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: 3027833-49-1
- 分子式: C32H36F2N2O6S
- 分子量:614.70
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
PDEI 10 nM (IC50) |
体外実験
PDE1-IN-7 (2.5-20 μM; 48 h) effectively inhibits TGF-β-induced myofibroblast differentiation and proliferation in LX-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:human stellate cell LX-2
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Concentration:2.5, 5, 10, 20 μM
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Incubation Time:48 h
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Result:Dose-dependently reduced the elevated expression levels of fibronectin, collagen I, and α-SMA induced by TGF-β in LX-2 cells.
体内実験
Pharmacokinetic Analysis in SD rats[1]
| Route | Dose (mg/kg) | t1/2 (h) | Cmax (ng/mL) | AUC∞ (h)(ng·/mL) | Clobs (mL/min/kg) | MRT (h) | Vss_obs (mL/kg) |
| i.v. | 2.5 | 7.51 ± 0.64 | 25,006 ± 3082 | 6317 ± 839 | 6.56 ± 0.81 | 1.77 ± 0.07 | 698 ± 104 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BDL-induced hepatic fibrosis rats[1]Dosage:2.5 mg/kgAdministration:i.p.; once daily for 21 daysResult:Significantly reduced alanine transaminase (ALT), aspartate transaminase (AST) and total bile acids (TBA) levels.
Reduced structural damage to liver tissue, decreased fibrotic foci, and lowered collagen deposition levels.
Significantly reduced protein expression levels at α-SMA and collagen I levels.
Significantly increased cAMP levels.
化学情報
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CAS 番号 3027833-49-1
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分子量 614.70
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分子式 C32H36F2N2O6S
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SMILES
O=C1N(C(C(C(OCC2CCCCC2)=O)=C(N1)C)C3=CC=C(C(OCC4CC4)=C3)OC(F)F)C(SCC5=CC=CC=C5)=O
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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)