Fluorescent M3 muscarinic receptor antagonist (apparent KD values are 7.97, 6.29 and 6.24 for M3, M5 and M1 receptors respectively). Antagonizes the activity of carbachol, a muscarinic receptor agonist. Displays no intrinsic activity.
HB7827 (30 nM) binding to live CHO cells expressing muscarinic M3 receptors. Binding blocked by the unlabelled competitor 4-DAMP (10 µM). Nucli counter-stained with Hoechst.
HB7827 (30 nM) binding to live CHO cells expressing muscarinic M3 receptors. Binding blocked by the unlabelled competitor 4-DAMP (10 µM). Nucli counter-stained with Hoechst.
For imaging at the M3 receptor use solutions up to 100 nM.
Pharmacological validation
The CellAura fluorescent M3 antagonist [pirenzepine] ligand was shown to antagonize the activity of the muscarinic agonist, carbachol, in a recombinant CHO cell line expressing the human M3 receptor 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 CellAura fluorescent M3 antagonist [pirenzepine] to the basal or serum-stimulated cells did not significantly alter basal and stimulated SPAP levels, demonstrating that CellAura fluorescent M3 antagonist [pirenzepine] has no intrinsic agonist activity. To determine the apparent KD for CellAura fluorescent M3 antagonist [pirenzepine], cells were treated with varying concentrations of carbachol alone, or in the presence of 1µM CellAura fluorescent M3 antagonist [pirenzepine], and the serum-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 M3 antagonist [pirenzepine], 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.
![CellAura fluorescent M3 antagonist [pirenzepine] product vial image | Hello Bio](https://hellobio.com/media/catalog/product/c/e/cellaura_fluorescent_m3_antagonist_pirenzepine_hb7827_product_vial_image.jpg "CellAura fluorescent M3 antagonist [pirenzepine] product vial image | Hello Bio")
CellAura Fluorescent Ligands technical FAQs (274.2 KB) 
