Biological ActivityCELT-426 is a potent and partially selective fluorescent hD2 dopamine receptor antagonist (Ki values are 89.3 nM, 194.8 nM, and 263.6 nM for D2, D3, and D4 dopamine receptors respectively in radioligand binding assay). CELT-426 can be used as a fluorescent dopamine receptor probe for fluorescence binding assays, live cell imaging, flow cytometry, and fluorescence polarization assays. It is a suitable replacement for GPCR radiolabeling ligands. Excitation and emission maxima (λ) are 560 and 571 nm, respectively. Wavelengths are compatible with use as an acceptor dye in TR-FRET assays, together with the CoraFluor™ 1 (Cat. No. 7920) TR-FRET donor.
Add 62 μL of assay buffer containing 1% of DMSO to obtain a 100 μM stock solution, and use 250 nM as working concentration.
Application of CELT-426 in high content screening assay. Competition binding assay between CELT-426 (100 nM) and increasing concentrations of haloperidol (Catalog # 0931) in live adherent CHO cells expressing hD2.
Application of CELT-426 in fluorescence polarization assay. Human dopamine D2 receptor was isolated from CHO cells by membrane preparation and incubated with CELT-426 (100 nM). Haloperidol (Catalog # 0931) was added across a range of concentrations, and the binding affinity (KD = 3 nM) determined by fluorescence polarization.
Optical Data for CELT-426
|Closest Laser line||561 nm|
|Application||Fluorescence polarization, Confocal microscopy, Flow Cytometry, High-content screening,|
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The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
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