CaSR biased allosteric modulator (pEC50
= 7.8-8.1). Calcimimetic. Displays ability to bias signalling towards the accumulation of PERK1/2 and IP1
. Reduces parathyroid hormone (PTH) levels in rat serum without inducing the release of calcitonin. Exhibits no significant activation of human GABAB
or type I PTH receptors. Orally active.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Characterization of highly efficacious allosteric agonists of the human calcium-sensing receptor.
Ma et al.
Biased allosteric modulation at the CaS receptor engendered by structurally diverse calcimimetics.
Cook et al.
Towards a structural understanding of allosteric drugs at the human calcium-sensing receptor.
Leach et al.