Fluorescent GABAB antagonist (pKD = 7.97). A fluorescent GABAB receptor ligand derived from CGP-54626A GABAB antagonist. Shown to antagonize the activity of the GABA.
For imaging at the GABAB1/B2 receptor use solutions up to 100 nM.
Pharmacological validation
The CA200931 Fluorescent GABAB receptor antagonist was shown to antagonize the activity of the GABAB agonist, GABA, in a recombinant CHO cell line expressing the human GABAB1 and GABAB2 receptors and a serum-responsive secreted placental alkaline phosphatase (SPAP) reporter gene. The serum-induced expression of SPAP was measured under basal and serum-stimulated (maximal) conditions. Addition of CA200931 to the basal or serum-stimulated cells did not significantly alter basal and stimulated SPAP levels, demonstrating that the CA200931 fluorescent GABAB receptor antagonist has no intrinsic agonist activity.
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.