PDE2A Human Phosphodiesterase Enzymatic LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Phosphodiesterase type 2A (PDE2A) catalyzes the conversion of cAMP or cGMP to their respective monophosphate forms. PDE2Ais expressed in brain and to a lesser extent in heart, placenta, lung, pulmonary artery, skeletal muscle, kidney and pancreas. Further, numerous studies have shown the presence of PDE2A in a variety of microvessels of significance for maintenance of endothelial barrier function. Thus, increase in PDE2 (e.g., through TNF-alpha stimulation) may impair endothelial barrier function. Consequently, inhibition of PDE2A may be useful in the prevention and/or treatment of sepsis and acute respiratory distress syndrome (ARDS).
Family:
PDE
Sub Family:
Phosphodiesterase
Class:
Cyclic Nucleotide Signaling
Protein Name:
PDE2A
Uniprot Number:
O00408
Gene Name:
PDE2A
Gene ID:
5138
Accession Number:
NM_002599
Organism:
Human
Construct Details:
Full Length, 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 PDE2A expressed in insect Sf9 cells are used. Test compound and/or vehicle is preincubated with 40 ng/ml enzyme‡ 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:
EHNA
Criteria For Significance:
≥ 50% of max stimulation or inhibition
Test Concentration / Dose:
Suggested concentration for initial testing is 10 uM
Test Sample Requirements:
Minimum for 1) Screen: 25 μl of 10 mM stock -OR- 1 mg (pre-weighed). 2) Dose Response: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed).
Minimum Order Quantity:
2
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
CNS/Addiction/Pain
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
RELATED SOLUTIONS
PDE Selectivity Screen LeadHunter Panel - TW
Item: PP168
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