CCK2 receptor ligand binding assay
Cholecystokinin (CCK) is a neuropeptide and gut hormone that regulates pancreatic enzyme secretion and gastrointestinal motility, and acts as a satiety signal. It is released simultaneously from intestinal cells and neurons in response to a meal. The precursor molecule prepro-CCK can be cleaved to generate a variety of biologically active forms of CCK including CCK-33, CCK-8 (CCK octapeptide), CCK-39 and CCK-58. Two CCK receptor subtypes, CCK1 and CCK2, mediate the physiological actions of CCK and the related peptide gastrin. The CCK1 receptor has a high affinity for sulfated CCK analogs, whereas the CCK2 receptor has similar affinity for sulfated and non-sulfated forms.
Cholecystokinin CCK2 binding assay starter pack
| Products | Product reference | Product insert | MSDS |
| Tag-lite CCK receptors red agonist - 5000 tests | L0013RED | ||
| Tag-lite CCK2 - 1 Million labeled cells | C1TT1CCK2 | - | |
| Tag-lite buffer - 100 ml (5X) | LABMED | - | - |
The binding assay starter pack consists of three references, the labeled cells, the fluorescent ligand and the Tag-lite buffer. Each component must be ordered separately. The cells express the SNAP-receptor labeled with terbium cryptate (labeling performed with Tag-lite SNAP-Lumi4 Tb). The labeled cells are proposed in a 1 million cell pack, to achieve a minimum of 100 tests at a cell density of 10,000 cells/well.
- This agonist is a CCK derivative labeled with a red emitting HTRF fluorescent probe
- This ligand has been successfully used both in CCK1 and CCK2 Cholecystokinin receptors Tag-lite binding assays.
- Concentration: 10µM
- Buffer: H2O
- Molecular Weight: 1811.8
Assay Validation:
Cholecystokinin CCK2 receptor ligand binding assay was performed using the starter pack reagents.
Kd was determined and signal inhibition (IC50) by agonist and antagonist was performed with L0013RED (Tag-lite Cholecystokinin receptors red agonist) 10nM. Results obtained with radioligand assay and Tag-lite platform were very similar.
| Family | Receptor | Compounds | Radioactivity( Ki nM) | Tag-lite (Ki nM) |
| Cholecystokinin | CCK2 | Sulfated CCK-8 (1) - Agonist | 0.46 | 2.9 |
| PD-135158 (1) - Antagonist | 1.17 | 3.1 |
(1) Dunlop et al. Neuropeptides, 1996
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