177172-49-5

Calcium-sensing receptor (CaSR) is a G protein-coupled receptor that is involved in calcium homeostasis. Activation of CaSR on parathyroid cells decreases the secretion of parathyroid hormone (PTH), which in turn reduces blood calcium concentration. R-568 is a calcimimetic compound that can allosterically activate or positively modulate the human CaSR. It dose-dependently decreases circulating levels of PTH in both normal individuals and patients with primary hyperparathyroidism in clinical trials. R-568 is used in research to explore novel actions of CaSR.

Treatment of hyperparathyroidism and related disorders, such as hypercalcemia (reduction of PTH secretion through modulation of calcium ion receptors on parathyroid cells).

Norcalcin (Amgen).

Store at -20°C

[1] E F NEMETH. Calcimimetics with potent and selective activity on the parathyroid calcium receptor.[J]. Proceedings of the National Academy of Sciences of the United States of America, 1998, 95 7: 4040-4045. DOI: 10.1073/pnas.95.7.4040
[2] J FOX. NPS R-568: a type II calcimimetic compound that acts on parathyroid cell calcium receptor of rats to reduce plasma levels of parathyroid hormone and calcium.[J]. Journal of Pharmacology and Experimental Therapeutics, 1999, 290 2: 473-479.
[3] M WADA. The calcimimetic compound NPS R-568 suppresses parathyroid cell proliferation in rats with renal insufficiency. Control of parathyroid cell growth via a calcium receptor.[J]. Journal of Clinical Investigation, 1997, 100 12: 2977-2983. DOI: 10.1172/jci119851