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.
For research use only. We do not sell to patients.
- CAS No.: 3027833-49-1
- Formula: C32H36F2N2O6S
- Molecular Weight:614.70
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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PDEI 10 nM (IC50) |
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.
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.
Chemical Information
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CAS No. 3027833-49-1
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Molecular Weight 614.70
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)