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Referencia número: HY-161506

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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.

Para uso exclusivo en investigación. No vendemos a pacientes.

No. CAS: 3027833-49-1
Fòrmula: C₃₂H₃₆F₂N₂O₆S
Peso molecular:614.70

Almacenamiento:

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

Data Sheet (279 KB)

PDE1-IN-7 Chemical Structure

No. CAS: 3027833-49-1

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureza y Documentación
Referencias
Calculators
Help & FAQs
Classifications
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Actividad biológica

Descripciòn

IC₅₀ & Target

^[1]

PDEI

10 nM (IC₅₀)

Ver todos los productos específicos de isoformas Phosphodiesterase (PDE) :

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)	t_1/2 (h)	C_max (ng/mL)	AUC_∞ (h)(ng·/mL)	Cl_obs (mL/min/kg)	MRT (h)	V_{ss_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.

Chemical Information

No. CAS 3027833-49-1
Peso molecular 614.70
Fòrmula C₃₂H₃₆F₂N₂O₆S
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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (279 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[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. [Content Brief]

Calculators

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

Minimum order quantity

100 mg

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