Calcium-Sensing Receptor

AMG-073 HCl (Cinacalcet HCl) represents a new class of compounds for the treatment of hyperparathyroidism known as calcimimetics, which reduce parathyroid hormone (PTH) synthesis and secretion by increasing the sensitivity of the parathyroid calcium-sensing receptor (CaR) to extracellular calcium.

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.

AMG-073 (Cinacalcet) represents a new class of compounds for the treatment of hyperparathyroidism.

NPS-2143 hydrochloride (SB-262470A hydrochloride), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist.

Strontium ranelate is an antiosteoporotic agent which both increases bone formation and reduces bone resorption, resulting in a rebalance of bone turnover in favor of bone formation. This is similar to the effects of choline stabilized orthosilicic acid.

Evocalcet is a calcium-sensing receptor agonist. The calcium-sensing receptor (CaSR) is a Class C G-protein coupled receptor which senses extracellular levels of calcium ion.

GSK3004774 is a potent, nonabsorbable agonist of CaSR, with an pEC50 of 7.3, 6.6 and 6.5 for human, mouse and rat CaSR, respectively. GSK3004774 shows an EC50 of 50 nM for human CaSR.

γ-L-Glutamyl-L-alanine, composed of gamma-glutamate and alanine, is a proteolytic breakdown product of larger proteins.

SB-423557 is an orally active calcium-sensing receptor (CaR) antagonist (IC50=520 nM), precursor of SB-423562 (IC50=73 nM).

Tecalcet Hydrochloride (R 568 Hydrochloride), an orally active calcimimetic compound, allosterically and positively modulates the calcium-sensing receptor (CaSR).

Calhex 231 hydrochloride is a potent negative allosteric modulator of the calcium-sensing receptor (CaSR), with an IC50 of 0.39 μM for inhibiting \[³H]inositol phosphate accumulation induced by CaSR activation. It transiently blocks signaling through the human wild-type CaSR and is utilized in research related to traumatic hemorrhagic shock (THS) and diabetic cardiomyopathy (DCM), where dysregulated calcium signaling contributes to disease pathology.

AC-265347 is a calcium-sensing receptor (CaSR) agonist and positive allosteric modulator (ago-PAM) with a functional affinity (pK\_B) of 5.1. It enhances CaSR activation and is useful for research into disorders related to calcium metabolism, such as hyperparathyroidism and other CaSR-associated diseases.

Calindol hydrochloride is a positive allosteric modulator (PAM) of the calcium-sensing receptor (CaSR), acting as a calcimimetic compound. It enhances CaSR activation with an EC50 of 132 nM, making it a valuable tool for studying calcium homeostasis and related signaling pathways.

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).

Lycoperodine-1 (Cyclomethyltryptophan) is a bioactive compound isolated from tomato fruits (*Lycopersicon esculentum*). It functions as an agonist of calcium-sensing receptors (CaSR), making it a useful molecule for studying CaSR-mediated signaling pathways and calcium homeostasis.

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.

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.

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.

H-Glu-Thr-OH, also known as L-α-Glutamyl-L-threonine, is a dipeptide composed of glutamic acid and threonine linked by a peptide bond. It functions as an agonist for the extracellular calcium-sensing receptor (CaSR), playing a critical role in calcium homeostasis. This compound is valuable for research applications investigating CaSR signaling pathways and the physiological effects of calcium regulation in various biological systems.