| Hazard Information | Back Directory | [Uses]
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[1]. | [in vivo]
PDE1-IN-7 (i.p.; 2.5 mg/kg; once daily for 21 days) shows significant antifibrotic effects in a rat model of bile duct ligation-induced hepatic fibrosis[1].
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 | |
| Animal Model: | BDL-induced hepatic fibrosis rats[1] | | Dosage: | 2.5 mg/kg | | Administration: | i.p.; once daily for 21 days | | Result: | 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.
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| [IC 50]
PDEI: 10 nM (IC50) | [References]
[1] Zhao ZJ, et al. Design, Synthesis, and Evaluation of Dihydropyrimidine Derivatives as Selective PDE1 Inhibitors for the Treatment of Liver Fibrosis. J Med Chem. 2024 Apr 26. |
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