1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. 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.

PDE1-IN-7 Chemical Structure

PDE1-IN-7 Chemical Structure

CAS No. : 3027833-49-1

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Description

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].

IC50 & Target[1]

PDEI

10 nM (IC50)

In Vitro

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.

Western Blot Analysis[1]

Cell Line: human stellate cell LX-2
Concentration: 2.5, 5, 10, 20 μM
Incubation Time: 48 h
Result: Dose-dependently reduced the elevated expression levels of fibronectin, collagen I, and α-SMA induced by TGF-β in LX-2 cells.
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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

614.70

Formula

C32H36F2N2O6S

CAS No.
Unlabeled Cas

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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PDE1-IN-7 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
PDE1-IN-7
Cat. No.:
HY-161506
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