PDE7A Human Phosphodiesterase Enzymatic LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Phosphodiesterase type 7A (PDE7A) catalyzes the conversion of cAMP or cGMP to their respective monophosphate forms. PDEs from mammalian tissues have been subdivided into 11 families derived from separate gene families, such as PDE7A and PDE7B. PDE7A is expressed in multiple tissues including muscle, spleen, brain, lung, thymus and various lymphocytes populations. Inhibition of PDE7A may be useful in treatment of inflammatory diseases in immune cells and tissues as brain or skeletal muscle.
Family:
PDE
Sub Family:
Phosphodiesterase
Class:
Cyclic Nucleotide Signaling
Protein Name:
PDE7A
Uniprot Number:
Q13946
Gene Name:
PDE7A
Gene ID:
5150
Gene Aliases:
HCP1
Accession Number:
NM_002603
Organism:
Human
Construct Details:
Fragment (122-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 PDE7A expressed in insect Sf9 cells are used. Test compound and/or vehicle is preincubated with 8 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:
3-Isobutyl-1-methylxanthine
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
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
RELATED SOLUTIONS
PDE Selectivity Screen LeadHunter Panel - TW
Item: PP168
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