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PDE10A Assay Kit
PDE10A Assay Kit
Artikelnummer
BPS60400
Verpackungseinheit
96 rxns.
Hersteller
BPS Bioscience
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Applications: Great for studying enzyme kinetics and screening small molecular inhibitors for drug discovery and HTS applications.
Background: Phosphodiesterases (PDEs) play an important role in the dynamicregulation of cAMP and cGMP signaling. PDE10A is a dual substrate PDE highlyexpressed in striatal medium spiny neurons. PDE10A inhibitors can improve thecognitive symptoms of schizophrenia, and exhibit potential therapeutic value forHuntington's Disease. Phosphodiesterases catalyze the hydrolysis of the phosphodiester bond in dye-labeledcyclic monophosphates. Beads selectively bind the phosphate group in the nucleotideproduct. This increases the size of the nucleotide relative to unreacted cyclicmonophosphate. In the polarization assay, dye molecules with absorption transitionvectors parallel to the linearly-polarized excitation light are selectively excited. Dyesattached to the rapidly-rotating cyclic monophosphates will obtain random orientationsand emit light with low polarization. Dyes attached to the slowly-rotating nucleotide-beadcomplexes will not have time to reorient and therefore will emit highly polarized light.
Contraindications: DMSO >1%, strong acids or bases, ionic detergents, high salt
Description: The PDE10A Assay Kit is designed for identification of PDE10A inhibitors using fluorescence polarization. The assay is based on the binding of a fluorescent nucleotide monophosphate generated by PDE10A to the binding agent. The key to the PDE10A Assay Kit is the specific binding agent. Using this kit, only two simple steps on a microtiter plate are required for PDE10A reactions. First, the fluorescently labeled cAMPis incubated with a sample containing PDE10A for 1 hour. Second, a binding agent isadded to the reaction mix to produce a change in fluorescent polarization that can then bemeasured using a fluorescence reader equipped for the measurement of fluorescence polarization.
Storage Stability: At least 6 months from date of receipt, when stored as directed. Kit components require different storage conditions. Be sure to store each component at the proper temperature upon arrival.
Supplied As: The PDE10A inhibitor screening assay kit comes in a convenient 96-well format, with purified PDE10A enzyme, fluorescently labeled PDE10A substrate (cAMP), binding agent, and PDE assay buffer for 100 enzyme reactions.
Warnings: Avoid freeze/thaw cycles.
Biosafety Level: Not applicable (BSL-1)
References: 1. Threlfell S, Sammut S, Menniti FS, Schmidt CJ, West AR. J Pharmacol Exp Ther 2009; 328(3):785-95.
2. Menniti FS, Chappie TA, Humphrey JM, Schmidt CJ. Curr Opin Investig Drugs 2007; 8(1):54-9. Application Reference(s):
Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility (2014)
Applications: Great for studying enzyme kinetics and screening small molecular inhibitors for drug discovery and HTS applications.
Background: Phosphodiesterases (PDEs) play an important role in the dynamicregulation of cAMP and cGMP signaling. PDE10A is a dual substrate PDE highlyexpressed in striatal medium spiny neurons. PDE10A inhibitors can improve thecognitive symptoms of schizophrenia, and exhibit potential therapeutic value forHuntington's Disease. Phosphodiesterases catalyze the hydrolysis of the phosphodiester bond in dye-labeledcyclic monophosphates. Beads selectively bind the phosphate group in the nucleotideproduct. This increases the size of the nucleotide relative to unreacted cyclicmonophosphate. In the polarization assay, dye molecules with absorption transitionvectors parallel to the linearly-polarized excitation light are selectively excited. Dyesattached to the rapidly-rotating cyclic monophosphates will obtain random orientationsand emit light with low polarization. Dyes attached to the slowly-rotating nucleotide-beadcomplexes will not have time to reorient and therefore will emit highly polarized light.
Contraindications: DMSO >1%, strong acids or bases, ionic detergents, high salt
Description: The PDE10A Assay Kit is designed for identification of PDE10A inhibitors using fluorescence polarization. The assay is based on the binding of a fluorescent nucleotide monophosphate generated by PDE10A to the binding agent. The key to the PDE10A Assay Kit is the specific binding agent. Using this kit, only two simple steps on a microtiter plate are required for PDE10A reactions. First, the fluorescently labeled cAMPis incubated with a sample containing PDE10A for 1 hour. Second, a binding agent isadded to the reaction mix to produce a change in fluorescent polarization that can then bemeasured using a fluorescence reader equipped for the measurement of fluorescence polarization.
Storage Stability: At least 6 months from date of receipt, when stored as directed. Kit components require different storage conditions. Be sure to store each component at the proper temperature upon arrival.
Supplied As: The PDE10A inhibitor screening assay kit comes in a convenient 96-well format, with purified PDE10A enzyme, fluorescently labeled PDE10A substrate (cAMP), binding agent, and PDE assay buffer for 100 enzyme reactions.
Warnings: Avoid freeze/thaw cycles.
Biosafety Level: Not applicable (BSL-1)
References: 1. Threlfell S, Sammut S, Menniti FS, Schmidt CJ, West AR. J Pharmacol Exp Ther 2009; 328(3):785-95.
2. Menniti FS, Chappie TA, Humphrey JM, Schmidt CJ. Curr Opin Investig Drugs 2007; 8(1):54-9. Application Reference(s):
Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility (2014)
| Artikelnummer | BPS60400 |
|---|---|
| Hersteller | BPS Bioscience |
| Hersteller Artikelnummer | 60400 |
| Green Labware | Nein |
| Verpackungseinheit | 96 rxns. |
| Mengeneinheit | PAK |
| Produktinformation (PDF) | Download |
| MSDS (PDF) |
|
Immer für Sie da
Gernot Ensinger, M.Sc.
Laurent Haze
