calcium-sensing

Calcium-Sensing Receptor Antagonists I functions as an antagonist to the parathyroid hormone receptors that sense calcium.

Strontium chloride is an agonist of Calcium sensing receptor (CaSR) and directly affects C-type nerve fibers.

Gadolinium chloride is a calcium-sensing receptor (CaSR) agonist

Cinacalcet (AMG 073) is an orally active, allosteric Ca receptor (CaR) agonist used in the treatment of cardiovascular disease.

Strontium ranelate (S12911), a strontium (II) salt of the ranelic acid, is a medication for osteoporosis. Studies indicate it can also slow the course of osteoarthritis of the knee. The drug is unusual in that it both increases deposition of new bone by osteoblasts and reduces the resorption of bone by osteoclasts. It is therefore promoted as a dual action bone agent (DABA) indicated for use in the treatment of severe osteoporosis.

Cinacalcet hydrochloride (AMG-073 hydrochloride) is a naphthalene derivative and calcimimetic agent that enhances the sensitivity of parathyroid gland calcium-sensing receptors to serum calcium, thereby reducing parathyroid hormone secretion and decreasing serum calcium in the treatment of parathyroid diseases.

(Rac)-Upacicalcet is a racemate of Upacicalcet, which serves as an intravenous calcimimetic agent. Upacicalcet acts by directly targeting calcium-sensing receptors on parathyroid cell membranes, effectively suppressing the release of excessive parathyroid hormone (PTH) and reducing blood PTH levels. This compound holds the potential for researching secondary hyperparathyroidism (SHPT) [1].

Tecalcet Hydrochloride (R-568 hydrochloride) is an allosteric and positive modulator of the calcium-sensing receptor(CaSR). Tecalcet Hydrochloride increases the sensitivity to the activation of extracellular Ca2+.

SB-423562 is a calcium-sensing receptor (CaSR) antagonist and can be used in studies about osteoporosis.

Evocalcet (KHK7580) has an activating effect on the calcium-sensing receptor (CaSR).

Etelcalcetide hydrochloride (AMG 416 hydrochloride) is a synthetic peptide that serves as an allosteric modulator of the calcium-sensing receptor (CaSR), effectively reducing parathyroid hormone (PTH) levels in patients with secondary hyperparathyroidism undergoing hemodialysis.

NPS2390 is a first generation quinoxaline derivative that acts as a noncompetitive antagonist of mGluR1 and mGluR5 (IC50 of 5.2 and 82 nM, respectively)

SB-423562 is a calcium-sensing receptor antagonist.

NPS-2143 hydrochloride (NPS-2143 HCL) is a selective potent calcium ion-sensing receptor antagonist.

Ligustroflavone (Nuezhenoside) has anti-inflammatory activity.

SB-423557 is an orally active antagonist of the calcium-sensing receptor (CaR), demonstrating an IC50 of 520 nM.

Etelcalcetide (AMG 416) is a synthetic peptide that serves as an activator of the calcium-sensing receptor (CaSR) and is used as a calcimimetic drug for treating secondary hyperparathyroidism in patients undergoing hemodialysis.

PyCTZ TFA, a pyridyl Coelenterazine (CTZ) analog, is an ATP-independent pyridyl substrate of LumiLuc luciferase. It produces intense blue bioluminescence when luciferases are present, making it suitable for aequorin-based calcium sensing[1].

Encaleret( JIT-305) is an antagonist of oral calcium-sensing receptor (CaSR), it is used for the treatment of osteoporosis.

Upacicalcet (sodium) is an intravenous calcimimetic agent that acts directly on parathyroid cell membrane calcium-sensing receptors to suppress excessive parathyroid hormone (PTH) secretion, thereby lowering blood PTH levels. It is indicated for the research of secondary hyperparathyroidism (SHPT).

CaSR Antagonist-1 is a potent inhibitor of the calcium-sensing receptor (CaSR) with an inhibitory concentration (IC50) of 50 nM, suitable for the investigation of diseases related to dysregulated bone or mineral homeostasis, including osteoporosis [1].

Strontium Malonate, a calcium-sensing receptor agonist, is used potentially for the treatment of postmenopausal osteoporosis.

Gamma-Glu-Abu is a potent calcium sensing receptor (CaSR) agonist [EMD 386088].

NPS-2143 (SB 262470A) is a novel potent and selective antagonist of Ca(2+) receptor.