Biological Information

Background Information:

Phosphodiesterase type 3 (PDE3) catalyzes the conversion of cAMP or cGMP to their respective monophosphate forms.  Two isoforms of PDE3 have been identified, i.e., PDE3A and PDE3B.  PDE3A is more abundant in platelets, cardiovascular tissues, whereas PDE3B is relatively highly expressed in tissues that more connected to the regulating energy metabolism, including liver, pancreatic β cells, adipose tissues as well as immune cells.  PDE3B inhibitors potentially are useful in the treatment of metabolic syndrome, inflammatory diseases, autoimmune disorders.

Family:

PDE

Sub Family:

Phosphodiesterase

Class:

Cyclic Nucleotide Signaling

Protein Name:

PDE3B

Uniprot Number:

Q13370

Protein Aliases:

CGI-PDEB

Gene Name:

PDE3B

Gene ID:

5140

Gene Aliases:

HcGIP1

Accession Number:

NM_000922

Organism:

Human

Construct Details:

Fragment (592-end), Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

Fluorescence Polarization

Measured Response:

Fluorescence

Testing Information

Procedure Summary:

Human recombinant PDE3B expressed in insect Sf9 cells are used. Test compound and/or vehicle is preincubated with 2.5 ng/ml enzymeǂ in Tris-HCl buffer pH 7.2 for 15 minutes at 25⁰C. The reaction is initiated by addition of 100 nM fluorescein lableled cAMP for another 30 minutes incubation period and terminated by addition of IMAP binding solution. IMAP complexes with phosphate groups on nucleotide monophosphate generated from cyclic nucleotides through PDE activity. Determination of the amount of complex formed is read spectrofluorimetrically at 470 nm/525 nm. Compounds are screened at 10 μM.

Substrate:

0.1 µM FAM-cAMP

Incubation:

30 min at 25°C

Control Inhibitor:

Cilostamide

Criteria For Significance:

≥ 50% of max stimulation or inhibition

Test Concentration / Dose:

Suggested concentration for initial testing is 10 uM

Minimum Order Quantity:

2

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

2753

Name

Cilostamide

Measurement

0.099μM -

Clinical Relevance

Therapeutic Area:

Cardiovascular

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

RELATED SOLUTIONS

PDE Selectivity Screen LeadHunter Panel - TW
Item: PP168
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