1. Signaling Pathways
  2. GPCR/G Protein
  3. CaSR

CaSR

The extracellular CaSR (calcium-sensing receptor is a unique G protein-coupled receptor (GPCR) activated by extracellular Ca2+ and by other physiological cations including Mg2+, amino acids, and polyamines. CaSR is the most important master controller of the extracellular Ca2+ homeostatic system being expressed at high levels in the parathyroid gland, kidney, gut, and bone, where it regulates parathyroid hormone (PTH) secretion, vitamin D synthesis, and Ca2+ absorption and resorption, respectively. Gain and loss of function mutations in the CaSR are responsible for severe disturbances in extracellular Ca2+ metabolism.

The CaSR stimulates two major signal transduction cascades. The first is the Gq/11-phospholipase C (PLC)-mediated generation of inositol 1,4,5-trisphosphate (IP3), which induces a rapid rise in intracellular calcium (Ca2+i) concentrations. The second is the mitogen-activated protein kinases (MAPKs), such as extracellular signal-regulated kinases 1 and 2 (ERK1/2), which phosphorylate proteins mediating cytosolic signaling and translocate into the nucleus to activate transcription factors involved in cellular proliferation and differentiation. The CaSR has been shown to activate MAPK signaling in a manner that depends on the G proteins Gq/11, and Gi/o, which inhibits cyclic adenosine monophosphate (cAMP) synthesis, and by a potentially G protein-independent mechanism involving β-arrestin types 1 and 2.

CaSR Related Products (16):

Cat. No. Product Name Effect Purity
  • HY-10007
    NPS-2143
    Antagonist 99.34%
    NPS-2143 (SB-262470A), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 (SB-262470A) blocks increases in cytoplasmic Ca2+ concentrations (IC50=43 nM) elicited by activating the Ca2+ receptor in HEK 293 cells expressing the human Ca2+ receptor.
  • HY-70037
    Cinacalcet
    Agonist 99.94%
    Cinacalcet (AMG 073) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.
  • HY-17613
    Evocalcet
    Activator 99.05%
    Evocalcet has an activating effect on calcium sensing receptor (CaSR) extracted from patent WO 2017061621 A1, compound A.
  • HY-P1955A
    Etelcalcetide hydrochloride
    Activator 99.31%
    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.
  • HY-70037A
    Cinacalcet hydrochloride
    Agonist 99.96%
    Cinacalcet hydrochloride (AMG-073 hydrochloride) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.
  • HY-103314
    Gadolinium chloride
    Agonist ≥99.0%
    Gadolinium chloride is a specific calcium-sensing receptor (CaSR) agonist. Gadolinium chloride can be used for the research of cardiovascular disease.
  • HY-10167A
    Tecalcet Hydrochloride
    Modulator 99.66%
    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+.
  • HY-10171
    NPS-2143 hydrochloride
    Antagonist 99.94%
    NPS-2143 hydrochloride (SB-262470A hydrochloride), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 hydrochloride (SB-262470A hydrochloride) blocks increases in cytoplasmic Ca2+ concentrations (IC50=43 nM) elicited by activating the Ca2+ receptor in HEK 293 cells expressing the human Ca2+ receptor.
  • HY-17397
    Strontium Ranelate
    Activator 99.93%
    Strontium Ranelate (S12911) is an antiosteoporotic agent that acts by reducing bone resorption and promoting bone formation, thereby inducing a positive bone balance. Strontium Ranelate also can activate the calcium-sensing receptor (CaSR) in non skeletal cells, resulting in the activation of inositol 1, 4, 5-triphosphate production and mitogen-activated protein kinase signaling.
  • HY-N0546
    Ligustroflavone
    Antagonist 99.41%
    Ligustroflavone, extracted from Ligustrum lucidum, is a potential candidate as calcium-sensing receptor (CaSR) antagonist. Ligustroflavone exhibits protective effects against diabetic osteoporosis in mice.
  • HY-103320A
    Calhex 231 hydrochloride
    Inhibitor ≥98.0%
    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.
  • HY-50713
    Calcium-Sensing Receptor Antagonists I
    Antagonist 99.91%
    Calcium-Sensing Receptor Antagonists I is an antagonist of calcium-sensing parathyroid hormone receptors.
  • HY-P1955
    Etelcalcetide
    Activator
    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.
  • HY-107773
    GSK3004774
    Agonist
    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.
  • HY-15106
    SB-423557
    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.
  • HY-15105
    SB-423562
    Antagonist 99.88%
    SB-423562 is a short-acting calcium-sensing receptor (CaR) antagonist. SB-423562 has the potential for osteoporosis research.
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