PDE1C Human Phosphodiesterase Enzymatic LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Phosphodiesterase 1C (PDE1C) is an enzyme that regulates the degradation of cyclic nucleotides, such as cAMP and cGMP, which are essential for intracellular signaling. Predominantly expressed in smooth muscle cells and various tissues, PDE1C plays a key role in regulating vascular tone, smooth muscle contraction, and other physiological processes. By modulating cyclic nucleotide levels, PDE1C influences cardiovascular function and neurotransmission. Given its involvement in smooth muscle function and vascular regulation, PDE1C is being explored as a therapeutic target for disorders such as hypertension, erectile dysfunction, and other cardiovascular conditions, where modulation of cyclic nucleotide signaling could offer benefits.
Family:
PDE
Sub Family:
Phosphodiesterase
Class:
Cyclic Nucleotide Signaling
Protein Name:
PDE1C
Uniprot Number:
Q14123
Protein Aliases:
Hcam3
Gene Name:
PDE1C
Gene ID:
5137
Gene Aliases:
Hcam3
Accession Number:
NM_001191056
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 PDE1C expressed in insect Sf9 cells are used. Test compound and/or vehicle are preincubated with 5.41 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:
Cardiovascular
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
RELATED SOLUTIONS
PDE Selectivity Screen LeadHunter Panel - TW
Item: PP168
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