(Rac)-Upacicalcet is the racemate of Upacicalcet.Upacicalcet is an intravenous calcimimetic agent. Upacicalcet suppresses excessive parathyroid hormone (PTH) secretion, thereby lowering blood PTH levels, by acting directly on parathyroid cell membrane calcium-sensing receptors. Upacicalcet can be used for researching the disease of secondary hyperparathyroidism (SHPT)[1].
Upacicalcet sodium is an intravenous calcimimetic agent. Upacicalcet suppresses excessive parathyroid hormone (PTH) secretion, thereby lowering blood PTH levels, by acting directly on parathyroid cell membrane calcium-sensing receptors. Upacicalcet can be used for researching the disease of secondary hyperparathyroidism (SHPT)[1].
Evocalcet has an activating effect on calcium sensing receptor (CaSR) extracted from patent WO 2017061621 A1, compound A.
Calcium-Sensing Receptor Antagonists I is an antagonist of calcium-sensing parathyroid hormone receptors. IC50 value:Target: CaSRCalcium-Sensing Receptor Antagonists I is useful for osteoporosis and other bone conditions
Ligustroflavone, extracted from Ligustrum lucidum, is a potential candidate as calcium-sensing receptor (CaSR) antagonist. Ligustroflavone exhibits protective effects against diabetic osteoporosis in mice[1].
Etelcalcetide (AMG 416) is a synthetic peptide as an activator of the calcium sensing receptor (CaSR). Etelcalcetide is effective in lowering parathyroid hormone (PTH) concentrations in patients receiving dialysis with secondary hyperparathyroidism receiving hemodialysis[1].
NPS-2143(SB 262470A ) 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.IC50 value: 43 nM(for Ca2+ receptor) [1]Target: CaSRin vitro: NPS 2143, even when tested at much higher concentrations (3 microM), did not affect the activity of a number of other G protein-coupled receptors, including those most structurally homologous to the Ca2+ receptor. NPS 2143 stimulated parathyroid hormone (PTH) secretion from bovine parathyroid cells (EC50 of 41 nM) over a range of extracellular Ca2+ concentrations and reversed the effects of the calcimimetic compound NPS R-467 on [Ca2+]i and on secretion of PTH [1]. The first reported calcilytic compound was NPS 2143, an orally active molecule which elicits rapid, 3- to 4-fold increases in circulating levels of PTH [2].in vivo: When infused intravenously in normal rats, NPS 2143 caused a rapid and large increase in plasma levels of PTH. Ca2+ receptor antagonists are termed calcilytics and NPS 2143 is the first substance (either atomic or molecular) shown to possess such activity [1]. When administered together with an antiresorptive agent (estradiol), NPS 2143 causes an increase in trabecular bone volume and bone mineral density in osteopenic rats [2].
Cinacalcet is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.
Calhex 231 hydrochloride is a CaSR inhibitor via negative allosteric modulation. Calhex 231 hydrochloride blocks Ca2+-induced accumulation of [3H]inositol phosphate with an IC50 of 0.39 μM in HEK293 cells. Calhex 231 hydrochloride has the potential for diabetic cardiomyopathy (DCM) treatment[1][2].
Cinacalcet hydrochloride is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.
Strontium ranelate(S12911) stimulates the calcium sensing receptors (CaSR) and leads to the differentiation of pre-osteoblast to osteoblast which increases the bone formation.IC50 value:Target: CaSRStrontium Ranelate is a bone metabolism modulator that inhibits bone resorption while maintaining bone formation. Strontium Ranelate acts by increasing bone formation and decreasing bone resorption, thus rebalancing bone turnover in favour of bone formation, an effect that results in increased bone mass and strength. Commonly used as an antiosteoporotic. Strontium Ranelate has shown efficacy in preventing early postmenopausal bone loss and reducing the risk of hip fracture in women with postmenopausal osteoporosis.
Tecalcet Hydrochloride (R 568 Hydrochloride), an orally active calcimimetic compound, allosterically and positively modulates the calcium-sensing receptor (CaSR). Tecalcet Hydrochloride (R 568 Hydrochloride) increases the sensitivity to activation by extracellular Ca2+[1][2][3].
SB-423562 is a short-acting calcium-sensing receptor (CaR) antagonist.
SB-423557 is an orally active calcium-sensing receptor (CaR) antagonist (IC50=520 nM), precursor of SB-423562 (IC50=73 nM). SB-423557 is well tolerated in human and increases plasma concentrations of exogenous parathyroid hormone (PTH) and stimulates bone formation[1].
Etelcalcetide hydrochloride (AMG 416 hydrochloride) is a synthetic peptide as an activator of the calcium sensing receptor (CaSR). Etelcalcetide hydrochloride is effective in lowering parathyroid hormone (PTH) concentrations in patients receiving dialysis with secondary hyperparathyroidism receiving hemodialysis[1].
NPS-2143 is a selective antagonist of calcium-sensing receptor (CaSR) with an IC50 of 43 nM.
AC-265347 is a calcium-sensing receptor (CaSR) agonist and positive allosteric modulator (ago-PAM) with the functional affinity (pKB) of 5.1. AC-265347 can be used for the research of hyperparathyroidism and related diseases[1].
Gadolinium chloride is a specific calcium-sensing receptor (CaSR) agonist. Gadolinium chloride can be used for the research of cardiovascular disease[1].
CaSRantagonist-1 is a calcium sensing receptor (CaSR) antagonistwith an IC50 value of 50 nM. CaSRantagonist-1 can be used for the research of disorders associated with abnormalbone or mineral homeostasis such as osteoporosis[1].
Gamma-Glu-Abu is a potent calcium sensing receptor (CaSR) agonist[1].
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[1].
Calindol hydrochloride is a positive allosteric modulator (PAM) of calcimimetic calcium-sensing receptor (CaSR) with an EC50 of 132 nM[1].