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You are here:Home-Inhibitors & Agonists-GPCR-Calcium-sensing Receptor (CaSR)

Request The Product List ofCalcium-sensing Receptor (CaSR) Calcium-sensing Receptor (CaSR)

Calcium-sensing Receptor (CaSR) is a Class C G-protein coupled receptor which senses extracellular levels of calcium ion. In theparathyroid gland, the calcium-sensing receptor controls calcium homeostasis by regulating the release of parathyroid hormone (PTH). The release of PTH is inhibited in response to elevations in plasma calcium concentrations and activation of the calcium receptor. Increased calcium binding on the extracellular side gives a conformational change in the receptor, which, on the intracellular side, initiates the phospholipase C pathway, presumably through a Gqα type of G protein, which ultimately increases intracellular concentration of calcium, which inhibits vesicle fusion and exocytosis of parathyroid hormone. It also inhibits the cAMP dependent pathway.

Cat. No. Product Name CAS No. Information
GY06730

GSK3004774

2138814-32-9

GSK3004774 (GSK-3004774) is a potent, nonabsorbable, gastrointestinally-restricted agonist agonist of calcium-sensing receptor (CaSR) with pEC50 of 7.3; demonstrates low permeability and low portal drug concentrations and high luminal stability and high fecal drug recovery in vivo DMPK experiments.

GY06649

Velcalcetide

1262780-97-1

Velcalcetide (AMG-416, Velcalcetide, Etelcalcetide, KAI-4169) is a potent, peptide agonist of CaSR, dose-dependenty increases IP1 accumulation with EC50 of 25 uM in cell based assays; reduces parathyroid hormone (PTH) levels and corresponding decreases serum calcium, regardless of the baseline level of PTH in vivo.

GY06615

Tecalcet

148717-54-8

Tecalcet (R-568;NPS R-568;KRN-568;NPS-568) is a calcimimetic acting agent and potent, selective positive allosteric modulator (agonist) of CaSR; potentiates the effects of extracellular Ca2+ on [Ca2+]i and PTH secretion (IC50=27 nM in bovine parathyroid cells) without effect in the absence of extracellular Ca2+, does not affect responses elicited by the homologous mGluRs.

GY06593

Tecalcet hydrochloride

177172-49-5

Tecalcet (R-568;NPS R-568;KRN-568;NPS-568) is a calcimimetic acting agent and potent, selective positive allosteric modulator (agonist) of CaSR; potentiates the effects of extracellular Ca2+ on [Ca2+]i and PTH secretion without effect in the absence of extracellular Ca2+, does not affect responses elicited by the homologous mGluRs; prevents parathyroid hyperplasia in rats with severe secondary hyperparathyroidism.

GY06488

Ronacaleret hydrochloride

702686-96-2

Ronacaleret hydrochloride is a potent calcium sensing receptor (CaSR) negative allosteric modulator with IC50 of 146 nM for hCaSR; stimulates parathyroid hormone (PTH) release and increases bone formation markers; act as an effective oral anabolic agent to enhance fracture healing.

GY06481

Ronacaleret

753449-67-1

Ronacaleret is a potent calcium sensing receptor (CaSR) negative allosteric modulator with IC50 of 146 nM for hCaSR; stimulates parathyroid hormone (PTH) release and increases bone formation markers; act as an effective oral anabolic agent to enhance fracture healing.

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