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Calcium-sensing receptor (CaSR) ligands act on the receptor that detects extracellular calcium levels. CaSR was cloned from bovine parathyroid and is a class C G protein-coupled receptor that controls parathyroid hormone secretion. Inactivating mutations in its gene cause familial hypocalciuric hypercalcemia and neonatal severe hyperparathyroidism. Calcimimetics are positive modulators that increase the receptor's sensitivity to calcium; examples here are cinacalcet, evocalcet and tecalcet hydrochloride. Calcilytics such as NPS-2143 and SB-423557 act in the opposite way and are used to study parathyroid and kidney calcium handling.
Synonyms: SB262470
NPS-2143 is a selective Ca2+-sensing receptor antagonist, shown to block increases in cytoplasmic Ca2+ concentrations elicited by human Ca2+ receptors expressed in HEK293 cells with an IC50 of 43 nM.
Synonyms: SB-262470A hydrochloride
NPS-2143 hydrochloride (SB-262470A hydrochloride), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist.
SB-423557 is an orally active calcium-sensing receptor (CaR) antagonist (IC50=520 nM), precursor of SB-423562 (IC50=73 nM).
TAK-075 is an orally active and highly potent calcium-sensing receptor (CaSR) antagonist with an IC50 of 0.94 nM. It promotes transient parathyroid hormone (PTH) secretion in rats and effectively prevents the sustained suppression of PTH caused by the buildup of active metabolites, thereby preserving normal PTH secretion dynamics. TAK-075 is a valuable compound for research in metabolic bone diseases, including osteoporosis.
Synonyms: SB 751689
Ronacaleret (SB 751689) is an orally active, potent, and selective calcium-sensing receptor (CaSR) antagonist that stimulates the endogenous release of parathyroid hormone (PTH) from the parathyroid glands. By modulating calcium homeostasis and enhancing PTH secretion, Ronacaleret is used in the study of postmenopausal osteoporosis and other bone-related metabolic disorders.
Synonyms: SB 751689A
Ronacaleret hydrochloride (SB 751689A) is an orally active, potent, and selective antagonist of the calcium-sensing receptor (CaSR). It stimulates the endogenous release of parathyroid hormone (PTH) from the parathyroid glands, supporting its use in the study of postmenopausal osteoporosis and related metabolic bone disorders.
Synonyms: CLTX-305; JTT-305; MK-5442; JIT-305
Encaleret (CLTX-305) is an orally active and highly potent antagonist of the calcium-sensing receptor (CaSR), with an IC50 of 0.012 μM. It promotes the secretion of parathyroid hormone (PTH) by inhibiting CaSR activity and is being investigated for the treatment of conditions such as osteoporosis and autosomal dominant hypocalcemia type 1 (ADH1).
Synonyms: CLTX-305 sodium; JTT-305 sodium; MK-5442 sodium
Encaleret sodium is a potent antagonist of the calcium-sensing receptor (CaSR), demonstrating an IC50 of 12 nM. By inhibiting the excessive activity of gain-of-function CaSR variants, it effectively restores blood calcium levels, stimulates parathyroid hormone secretion, and enhances magnesium and phosphorus metabolism. This compound is valuable in research related to osteoporosis and autosomal dominant hypocalcemia type 1, providing insights into calcium homeostasis and its implications in bone health and mineral metabolism.
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CaSR antagonist-1 is a potent antagonist of the calcium-sensing receptor (CaSR) with an IC50 value of 50 nM. This compound is valuable for investigating disorders linked to abnormal bone and mineral homeostasis, including osteoporosis. Its ability to modulate CaSR activity makes it a useful tool in research exploring the pathways involved in calcium metabolism and skeletal health.
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