• Catalog Number:

  E1KS2633

• Amount:

  10mg1​ PHYSICAL AND CHEMICAL PROPERTIES

2​ Biological Activity NPS-2143 is a selective potent calcium ion-sensing receptor antagonist with IC50 of 43 and 41 nM for cytoplasmic Ca2+ concentrations and parathyroid hormone secretion, respectively. NPS-2143 blocks increases in cytoplasmic Ca2+ concentrations elicited by human Ca2+ receptors expressed in HEK293 cells NPS 2143 , even at much higher concentrations (3 μM), did not influence the activity of a number of other G protein-coupled receptors, including those most structurally homologous to the Ca2+ receptor. NPS 2143 also stimulates parathyroid hormone secretion from bovine parathyroid cells . In addition, administration of NPS-2143 resulted in moderate but sustained increases in plasma PTH levels and marked increases in bone formation and resorption with no net bone gain or loss. [1][2] 3​ References: Calcilytic compounds: potent and selective Ca2+ receptor antagonists that stimulate secretion of parathyroid hormone. Nemeth EF et al. J Pharmacol Exp Ther. 2001 Oct;299(1):323-31. Rescue of calcium-sensing receptor mutants by allosteric modulators reveals a conformational checkpoint in receptor biogenesis. Huang Y et al. J Biol Chem. 2007 Mar 30;282(13):9517-25. The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.