CA200773 CellAura fluorescent D1 antagonist [SKF83566-green]
(HB7822)
Product overview
| Name | CA200773 CellAura fluorescent D1 antagonist [SKF83566-green] |
| Description | Fluorescent D1 dopamine receptor antagonist |
| Biological description | Selective fluorescent D1 dopamine receptor antagonist (apparent KD values are 7.09, < 5 and 7.56 for D1, D2 and D5 receptors respectively). Also antagonizes the activity of SKF 83566, a D1 dopamine receptor agonist. Displays no intrinsic agonist activity. |
| Alternative names | CA200773 |
| Purity | >97% |
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Biological Data
| Application notes | For imaging at the D1 receptor use solutions up to 100 nM. |
| Pharmacological validation | The CellAura fluorescent D1 antagonist [SKF83566-green] ligand was shown to antagonize the activity of the D1 agonist, SKF 83566, in a recombinant CHO cell line expressing the human D1 receptor and a cyclic AMP-responsive secreted placental alkaline phosphatase (SPAP) reporter gene. The cyclic AMP-induced expression of SPAP was measured under basal and forskolin-stimulated (maximal) conditions. Addition of CellAura fluorescent D1 antagonist [SKF83566-green] to the basal or forskolin-stimulated cells did not significantly alter basal and stimulated SPAP levels, demonstrating that CellAura fluorescent D1 antagonist [SKF83566-green] has no intrinsic agonist activity. To determine the apparent KD for CellAura fluorescent D1 antagonist [SKF83566-green], cells were treated with varying concentrations of SKF 83566 alone, or in the presence of 1µM CellAura fluorescent D1 antagonist [SKF83566-green], and the cyclic AMP-induced expression of SPAP measured. The apparent KD was calculated from the rightward shift of the agonist response curve in the presence of CellAura fluorescent D1 antagonist [SKF83566-green], compared to the response curve for the agonist alone. |
Solubility & Handling
| Storage instructions | -20°C (protect from light) |
| Solubility overview | Soluble in DMSO |
| Handling | After thawing individual aliquots for use, we recommend briefly sonicating the sample to ensure it is fully dissolved and the solution is homogeneous. We do not recommend using the product after subjecting it to repetitive freeze-thaw cycles. |
| Shipping conditions | The product, supplied in a dry form, is stable at ambient temperature for periods of up to a few days and does not require shipping on ice/dry ice. |
| Important | This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use. |
Chemical Data
| Molecular Weight | 877 |
| Source | Synthetic |
| Formulation | Lyophilized film |
| Excitation | 488 nm |
| Emission | 525 / 550 nm |
Publications
These publications cite the use of CA200773 CellAura fluorescent D1 antagonist [SKF83566-green] purchased from Hello Bio:
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Development and Application of a High-Content Virion Display Human GPCR Array
Syu et al (2019) Nat Commun 10(1) : 1997PubMedID: 31040288 -
Measuring ligand binding kinetics to membrane proteins using virion nano-oscillators.
Ma et al (2018) J Am Chem Soc doi: 10.1021 : /jacs.8b07461PubMedID: 30114365 -
Implementation of fluorescence anisotropy-based assay for the characterization of ligand binding to dopamine D1 receptors
Dr. Anni Allikalt, Dr. Sergei Kopanchuk, Prof. Dr. Ago Rinken (2018) European Journal of Pharmacology In Press : In Press -
A dopamine D1 receptor binding assay using bioluminescence resonance energy transfer (BRET) with Nanoluciferase
Appelhans et al (2018) 7th Focused Meeting on Cell Signalling Poster 19 : 1(abst012P) -
High Throughput Fluorescence-Based Live Cell Binding Assays For G Protein-Coupled Receptors
Arruda et al. () Proceedings of the British Pharmacological Society
Technical guides
FAQs
CellAura Fluorescent Ligands technical FAQs (274.2 KB) Technical Documentation
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