PDE10A2 TR-FRET Assay Kit

Catalog #

60710

$405 *

Size: 96 reactions

Qty

Bulk/Custom

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*US Pricing only. For international pricing, please contact your local distributor.

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Description

Phosphodiesterases (PDEs) play an important role in dynamic regulation of cAMP and cGMP signaling. PDE10A is a dual substrate PDE highly expressed in striatal medium spiny neurons. PDE10A inhibitors can improve the cognitive symptoms of schizophrenia, and exhibit potential therapeutic value for Huntington’s disease. PDE10A2 is located in cytosol, whereas PDE10A2 is a membrane-associated protein.

The PDE10A2 TR-FRET Assay Kit is designed for identification of inhibitors of PDE10A2 using TR-FRET (Time Resolved Fluorescence Resonance Energy Transfer) technology. The assay is based on the generation of FAM-labeled nucleotide monophosphates by the phosphodiesterase. These phosphate groups bind to terbium-labeled nanoparticles, resulting in energy transfer from the terbium to the FAM, which emits a fluorescent signal at 520 nm. The change in fluorescent intensity can be easily measured using a fluorescence plate reader.

Using this kit, only two simple steps on a microtiter plate are required for the PDE10A2 activity assay. First, the fluorescent-labeled cAMP is incubated with a sample containing PDE10A2 for 1 hour. Second, a binding agent and a terbium donor are added to the reaction mix and incubated for 1 hour. Then, fluorescence intensity can be measured using a fluorescence reader.

Need us to run inhibitor screens or profile your compounds against PDE10A2? Check out our Phosphodiesterase Screening Services.

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Synonyms

inhibitor screening, FRET assay kit, PDE10A2, HTRF, PDE10-A2, PDE

Product Info

Storage and Usage

Citations

Assay Kit Format

TR-FRET

Species

Human

Supplied As

The PDE10A2 TR-FRET Assay Kit comes in a convenient 96-well format, with purified PDE10A2 enzyme, fluorescently labeled PDE substrate (cAMP), binding agent, and PDE assay buffer for 100 enzyme reactions.

Materials Required But Not Supplied

Fluorescent microplate reader capable of measuring Time Resolved Fluorescence Resonance Energy Transfer (TR-FRET)

Format

Catalog #	Component	Amount	Storage
60100	PDE10A2 recombinant enzyme	1 µg	-80°C	Avoid freeze/ thaw cycles!
60200	FAM-Cyclic-3′, 5′-AMP: 20 µM	50 µl	-80°C
60393	PDE assay buffer	25 ml	-20°C
60394	Tb donor	50 µl	-80°C
60390	Binding Agent	200 µl	+4°C
78422	Binding Buffer A	20 ml	+4°C
78423	Binding Buffer B	20 ml	+4°C
79685	Black, low binding NUNC microtiter pla	1	Room Temp.

UniProt #

Q9Y233

References

1. Akinori Nishi and Gretchen L. Snyder. J Pharmacol Sci., 2010, 114: 6 – 16.
2. Kenji Omori and Jun Kotera. Circulation Research. 2007; 100: 309-327.

Storage/Stability

At least 6 months from date of receipt, when stored as directed.

Applications

Great for screening small molecular inhibitors for drug discovery and HTS applications.

Shipping Temperature

-80°C

Warnings

Avoid freeze/thaw cycles

Disclaimers and Limitations

BPS Bioscience assay kits are validated using the listed components according to our specific protocol. Any deviations to kit components or protocols, such as using different proteins, cell/tissue lysates, or buffers (including using the same component from other commercial sources) will void any warranties on the performance of the assay kit and is not recommended.

End-users should immediately report any issues to [email protected] upon receipt of the kit, such as missing components, damaged vials, no dry ice, etc.

Scientific Category

PDE

Regulatory Status

Research Use Only

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PDE10A2 TR-FRET Assay Kit

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