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Cat. No. Product Name CAS No. Information
PC-35260

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.

PC-63560

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.

Hyperparathyroidism

Approved

PC-62910

Calindol hydrochloride

729610-18-8 Calindol hydrochloride is a calcimimetic acting agent and positive allosteric modulator (agonist) of CaSR with EC50 of 0.31 uM (stimulated 3H IP accumulation in CHO cells at 2 mM Ca2+); activates an extracellular ligand-binding domain-deleted rhodopsin-like seven-transmembrane structure in the absence of Ca(2+); produces concentration-dependent hyperpolarizations of vascular myocytes from rat isolated mesenteric and porcine coronary arteries.
PC-62909

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.

Hyperparathyroidism

Phase 2 Discontinued

PC-62908

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.

Hyperparathyroidism

Phase 2 Discontinued

PC-62907

AC-265347

1253901-26-6 AC-265347 is a calcimimetic acting agent and highly efficacious, orally active allosteric agonist (PAM) of CaSR with IC50 of 10 nM in PI hydrolysis assays; activates CaSR signaling in cellular proliferation with IC50 of 30 nM; significantly stimulates greater responses than Cinacalcet or Calindol at each of four loss-of-function human polymorphic CaSR variants, and does not inhibit the CYP2D6 cytochrome P450 isozyme; reduced serum parathyroid hormone (PTH) in rats, also reduces plasma ionizable calcium ([Ca(2+)](o)).
PC-62905

Calhex-231

652973-93-8 Calhex-231 is a potent negative allosteric modulator of CaSR that blocks calcium-mediated activation with IC50 of 0.39 uM; inhibits myocyte hyperpolarization to the CaSR activator calindol and R-568.

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