Biological Information
Background Information:
Phosphodiesterase 1B (PDE1B) is an enzyme that hydrolyzes cyclic nucleotides, specifically cAMP and cGMP, playing a critical role in regulating cellular signaling pathways. It is primarily expressed in the brain, where it modulates neuronal activity and synaptic plasticity. PDE1B is involved in various neurological processes, including memory, learning, and mood regulation, making it a potential therapeutic target for neurological disorders such as Alzheimer's disease, Parkinson's disease, and depression. Inhibition of PDE1B can enhance cyclic nucleotide signaling, offering a promising strategy for treating cognitive and mood disorders, and potentially improving synaptic function and brain health.
Family:
PDE
Sub Family:
Phosphodiesterase
Class:
Cyclic Nucleotide Signaling
Protein Name:
PDE1B
Uniprot Number:
Q01064
Protein Aliases:
63 kDa Cam-PDE
Gene Name:
PDE1B
Gene ID:
5153
Accession Number:
NM_000924
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 Polarization
Testing Information
Procedure Summary:
Human recombinant PDE1B expressed in insect Sf9 cells are used. Test compound and/or vehicle are preincubated with 80.4 ng/ml enzyme in Tris-HCl buffer pH 7.2 for 15 minutes at 25oC. The reaction is initiated by addition of 100 nM fluorescein labeled cGMP and incubated for another 30 minutes. The reaction is terminated by the addition of IMAP binding solution. IMAP complexes with phosphate groups on nucleotide monophosphate generated from cyclic nucleotides through PDE activity are detected. 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-cGMP
Incubation:
30 min at 25°C
Control Inhibitor:
DSR-141562
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
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