TABLE 1

Antagonist activity of AMG 334 at human adrenomedullin, calcitonin, and amylin receptors

Human CGRP8-37 peptide was used as the positive control for experiments involving the adrenomedullin-1 and adrenomedullin-2 receptors. Human calcitonin8-32 peptide was used as the positive control for experiments involving the calcitonin and amylin receptors. IC50 values are expressed as mean ± S.D. n = number of replicate experiments performed.

Cell LineHuman ReceptorTest Article, Positive ControlIC50 (nM)
AM1-HEKAdrenomedullin-1AMG 334, CGRP8-37 peptide>10,000 (n = 4) 660 ± 370 (n = 4)
AM2-CHOAdrenomedullin-2AMG 334, CGRP8-37 peptide>10,000 (n = 4) 420 ± 230 (n = 4)
Calcitonin-HEKCalcitoninAMG 334, calcitonin8-32 peptide>10,000 (n = 2) 590 ± 210 (n = 2)
MCF-7AmylinAMG 334, calcitonin8-32 peptide>10,000 (n = 2) 210 ± 10 (n = 2)
  • CGRP, calcitonin gene-related peptide; CHO, Chinese hamster ovary; HEK, human embryonic kidney.