2. Metabolic Enzyme/Protease TGF-beta/Smad Stem Cell/Wnt Immunology/Inflammation Apoptosis Cytoskeleton
  3. Phosphodiesterase (PDE) PKA Interleukin Related TNF Receptor Collagen
  4. Phosphodiesterase-IN-5

Phosphodiesterase-IN-5 is a potent, orally active and selective phosphodiesterase 10A (PDE10A) inhibitor with an IC50 of 6.2 nM. Phosphodiesterase-IN-5 shows >1612-fold selectivity over other PDEs. Phosphodiesterase-IN-5 exhibits potent antifibrotic efficacy in a Bleomycin (BLM) (HY-108345)-induced murine model of pulmonary fibrosis (PF) by blocking myofibroblast differentiation via the cAMP/PKA/CREB signaling pathway. Phosphodiesterase-IN-5 can be used for the research of PF.

For research use only. We do not sell to patients.

Phosphodiesterase-IN-5

Phosphodiesterase-IN-5 Chemical Structure

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Phosphodiesterase-IN-5 Related Antibodies

Top Publications Citing Use of Products

View All Phosphodiesterase (PDE) Isoform Specific Products:

View All Isoforms
PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

View All PKA Isoform Specific Products:

View All Isoforms
PKA PKAR PKACα

View All Interleukin Related Isoform Specific Products:

View All Isoforms
IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

View All TNF Receptor Isoform Specific Products:

View All Isoforms
TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Phosphodiesterase-IN-5 is a potent, orally active and selective phosphodiesterase 10A (PDE10A) inhibitor with an IC50 of 6.2 nM. Phosphodiesterase-IN-5 shows >1612-fold selectivity over other PDEs. Phosphodiesterase-IN-5 exhibits potent antifibrotic efficacy in a Bleomycin (BLM) (HY-108345)-induced murine model of pulmonary fibrosis (PF) by blocking myofibroblast differentiation via the cAMP/PKA/CREB signaling pathway. Phosphodiesterase-IN-5 can be used for the research of PF[1].

IC50 & Target[1]

PDE10A

6.2 nM (IC50)

In Vitro

Phosphodiesterase-IN-5 (compound QC-3) (5-20 μM; 48 h) exhibits antifibrotic activity in TGF-β1 (HY-163536)-stimulated MRC-5 cells via activation of the cAMP/PKA/CREB pathway, which inhibits myofibroblast differentiation and ECM deposition[1].
Phosphodiesterase-IN-5 binds the catalytic domain of PDE10A, forming hydrogen bonds with Gln726 and hydrophobic interactions with Ile692, while the 6-F substituent enables halogen bonding with Asp674 via a water molecule[1].

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

Phosphodiesterase-IN-5 Related Antibodies

Cell Viability AssayWestern Blot AnalysisCell Proliferation AssayApoptosis AnalysisCell Cytotoxicity AssayCell Cycle AnalysisRT-PCRCell Autophagy AssayImmunofluorescenceCell Differentiation AssayCell [1]

Cell Line: MRC-5 cells
Concentration: 3.125, 6.25, 12.5, 25, 50, 100, 200 μM
Incubation Time: 48 h
Result: Showed no cytotoxic in MRC-5 cells at concentrations up to 200 μM.

Western Blot Analysis[1]

Cell Line: TGF-β1-stimulated MRC-5 cells
Concentration: 5, 10, 20 μM
Incubation Time: 48 h
Result: Demonstrated concentration-dependent reductions in FN, COL-I, and α-SMA protein expression.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-t AUC0-∞ MRT0-t CL Vss F
Rat[1] 5.0 mg/kg p.o. 1.04 h 0.5 h 680.1 ng/mL 1351.6 ng·h/mL 1356.3 ng·h/mL 1.68 h 3.87 L/h/kg 5.86 L/kg 47.3 %
Rat[1] 1.0 mg/kg i.v. 1.12 h 0.08 h 962.0 ng/mL 573.3 ng·h/mL 573.3 ng·h/mL 0.60 h 1.75 L/h/kg 2.76 L/kg /
In Vivo

Phosphodiesterase-IN-5 (10 mg/kg, i.g., daily for 21 days) exhibts potent antifibrotic efficacy in a BLM-induced murine model of PF by blocking myofibroblast differentiation via the cAMP/PKA/CREB signaling pathway[1].

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

Animal Model: Male C57BL/6 mice (7-9 weeks old, 20-24 g) induced by BLM[1]
Dosage: 2.5, 5, 10 mg/kg
Administration: i.g.; daily for 21 days
Result: Dose-dependently reversed BLM-induced changes in Penh, endexpiratory pause (EEP), relaxation time (RT), andfrequency (f), nearly restoring them to normal levels.
Mitigated BLM-induced body weight loss and elevated lung coefficient in a dose-dependent manner.
Reduced IL-6 and TGF-β levels in broncho alveolar lavage fluid (BALF), and restored pulmonary cAMP levels.
Markedly reduced BLM-induced increases in IL-6 and TGF-β levels in BALF, with the mos pronounced inhibition observed at the 10 mg/kg dose.
Restored pulmonary cAMP levels.
Improved pulmonary morphology.
Effectively reduced the level of alveolar wall thickening, inflammatory cell infiltration, and collagen deposition.
Showed a dose-dependent reduction in fibrotic lesions.
Significantly suppressed the BLM- induced overexpression of fibrotic markers such as FN, COL-I, and α-SMA, with the most pronounced effect observed at a dose of 10 mg/kg.
Molecular Weight

471.53

Formula

C26H26FN7O
SMILES

O=C(C1=C(C2CN(C3=NC(C)=C4C=CC=CC4=N3)C2)N=C5C=CC(F)=CN51)N(C6)CCNC76CC7
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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Phosphodiesterase-IN-5 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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.

Keywords:

Phosphodiesterase-IN-5Phosphodiesterase (PDE)PKAInterleukin RelatedTNF ReceptorCollagenProtein kinase AILTumor Necrosis Factor ReceptorTNFRphosphodiesteraseBleomycinpulmonary fibrosisCREBcAMPInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Phosphodiesterase-IN-5
Cat. No.:
HY-179645
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.