Calhex 231 hydrochloride is a CaSR inhibitor with the potential for diabetic cardiomyopathy treatment. It blocks Ca2+-induced accumulation of [3H]inositol phosphate (IC50: 0.39 μM in HEK293 cells).
Etelcalcetide (AMG 416) is a synthetic peptide that serves as an activator of the calcium-sensing receptor (CaSR) and is used as a calcimimetic drug for treating secondary hyperparathyroidism in patients undergoing hemodialysis.
GSK3004774 is a nonabsorbable agonist of CaSR (pEC50: 7.3, 6.6, and 6.5 for human, mouse, and rat CaSR). GSK3004774 shows an EC50 of 50 nM for human CaSR.