casr

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].

Upacicalcet HCl is an intravesical calcium mimetic that inhibits excessive parathyroid hormone (PTH) secretion by directly acting on calcium-sensitive receptors in parathyroid cell membranes, thereby lowering PTH levels in the blood.Upacicalcet HCl can be used for the treatment of blood Upacicalcet HCl is a novel compound for the treatment of secondary hyperparathyroidism, targeting amino acid-binding sites of calcium-sensitive receptors. binding sites.

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.

Ronacaleret HCl (SB-751689) is a small molecule CaSR antagonist for the treatment of endocrine and metabolic diseases, skin and musculoskeletal disorders.

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+.

Calindol hydrochloride is a potent orthosteric modulator (EC50: 132 nM) of the putative calcium-calcium-sensitive receptor (CaSR), inhibits Pi-induced VC, and delays the progression of calcification in vascular smooth muscle cells.

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.

AC265347 is a potent calcium-sensitive receptor (CaSR) agonist and ago-PAM orthosteric modulator with antitumour activity that inhibits neuroblastoma tumour growth by inducing differentiation.AC265347 can be used to study neuroblastoma.

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

Ligustroflavone (Nuezhenoside) has anti-inflammatory activity.

Poly-D-lysine hydrobromide (MW 30000-70000) (Poly-D-lysine HBr) is an oral peptide CaSR agonist that eliminates proteinase K-resistant PrP from prion-infected SN56 neuroblastoma cells.

Calhex 231 hydrochloride is a CaSR inhibitor with potential for diabetic cardiomyopathy treatment; it blocks Ca2+-induced accumulation of [3H]inositol phosphate with an IC50 of 0.39 μM in HEK293 cells.

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

TNCA (Lycoperodine-1) is a high-affinity CaSR ligand (CaSRL) with co-agonist activity.

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-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.

GSK3004774 is a nonabsorbable agonist of CaSR (pEC50: 7.3, 6.6, and 6.5 for human, mouse, and rat CaSR). GSK3004774 shows an EC50 of 50 nM for human CaSR.

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

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