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

PubChem ID

3758

Name

3-Isobutyl-1-methylxanthine

Measurement

>100μM - IC50

PubChem ID

155806

Name

8-Methoxymethyl-IBMX

Measurement

>100μM - IC50

PubChem ID

122540493

Name

DSR-141562

Measurement

0.61μM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

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Item: PP168