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Reagent Details

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Catalogue number: CA200887
Product: M3 antagonist [pirenzepine]
Selectivity: M1: 6.24 | M3: 7.97 | M5: 6.29

 

 
Pharmacophore Pirenzepine-derivative Catalogue Number Pack Size Price
Molecular Weight 1014 CA200887-TK0* 0.05 mg £137.50*
Purity ≥97% CA200887-020 0.2 mg £500
Excitation 633 nm CA200887-050 0.5 mg £1200
Emission 650 nm CA200887-100 1.0 mg £2150
 
* Ordered as part of a TestKit comprising a selection of 4 ligands, listing 4 catalogue numbers ending in -TK0
 

Imaging information

For imaging at the M3 receptor use solutions up to 100 nM.

Pharmacological Validation

The CA200887 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 CA200887 to the basal or serum-stimulated cells did not significantly alter basal and stimulated SPAP levels, demonstrating that CA200887 has no intrinsic agonist activity.

To determine the apparent KD for CA200887, cells were treated with varying concentrations of carbachol alone, or in the presence of 1µM CA200887, 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 CA200887, compared to the response curve for the agonist alone.

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