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 (33):

Cat. No. Product Name Effect Purity
  • HY-70037
    Cinacalcet Agonist 99.97%
    Cinacalcet (AMG 073) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease research.
  • HY-10007
    NPS-2143 Antagonist 99.33%
    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[1][2].
  • HY-70037A
    Cinacalcet hydrochloride Agonist 99.99%
    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
    Gadolinium chloride is a specific calcium-sensing receptor (CaSR) agonist. Gadolinium chloride can be used for the research of cardiovascular disease[1].
  • HY-P1955A
    Etelcalcetide hydrochloride Activator 99.61%
    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[1].
  • HY-14752
    Ronacaleret Antagonist
    Ronacaleret (SB 751689) is an orally active, potent, and selective calcium-sensing receptor (CaSR) antagonist that stimulates endogenous parathyroid hormone release from the parathyroid glands. Ronacaleret (SB 751689) is used for the study of postmenopausal osteoporosis[1].
  • HY-12557
    γ-Glutamylvaline Activator 99.73%
    γ-Glutamylvaline is an activator of CaSR with anti-inflammatory activity. γ-Glutamylvaline inhibits TNF-α-induced proinflammatory cytokine production and increases Wnt5a expression. γ-Glutamylvaline activates calcium-sensing receptor pathways in adipocytes of 3T3-L1 mice and prevents low-grade chronic inflammation[1].
  • HY-15104
    Ronacaleret hydrochloride Antagonist
    Ronacaleret hydrochloride (SB 751689A) is an orally active, potent, and selective calcium-sensing receptor (CaSR) antagonist that stimulates endogenous parathyroid hormone release from the parathyroid glands. Ronacaleret hydrochloride (SB 751689A) is used for the study of postmenopausal osteoporosis[1].
  • HY-17613
    Evocalcet Activator 98.39%
    Evocalcet (KHK7580) is an orally active calcium sensing receptor (CaSR) agonist. Evocalcet inhibits the secretion of parathyroid hormone (PTH) from parathyroid gland cells. Evocalcet can be used for the research of hyperparathyroidism[1][2].
  • HY-109106B
    (Rac)-Upacicalcet
    (Rac)-Upacicalcet is the racemate of Upacicalcet.Upacicalcet is an intravenous calcimimetic agent. Upacicalcet suppresses excessive parathyroid hormone (PTH) secretion, thereby lowering blood PTH levels, by acting directly on parathyroid cell membrane calcium-sensing receptors. Upacicalcet can be used for researching the disease of secondary hyperparathyroidism (SHPT)[1].
  • HY-10167A
    Tecalcet Hydrochloride Modulator 99.74%
    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+[1][2][3].
  • 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[1].
  • HY-70037S
    Cinacalcet-D3 Agonist
    Cinacalcet-d3 is the deuterium labeled Cinacalcet. Cinacalcet (AMG 073) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.
  • HY-112171
    γ-L-Glutamyl-L-alanine Modulator
    γ-L-Glutamyl-L-alanine, composed of gamma-glutamate and alanine, is a proteolytic breakdown product of larger proteins. γ-L-Glutamyl-L-alanine is a natural substrate of the γ-Glutamylcyclotransferase. γ-L-Glutamyl-L-alanine is a positive modulator of calcium-sensing receptor (CaR) function[1][2][3][4].
  • 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[1].
  • HY-10171
    NPS-2143 hydrochloride Antagonist 99.80%
    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[1][2].
  • HY-17397
    Strontium Ranelate Activator 99.99%
    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 can also 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[1][2].
  • HY-109106A
    Upacicalcet sodium
    Upacicalcet sodium is an intravenous calcimimetic agent. Upacicalcet suppresses excessive parathyroid hormone (PTH) secretion, thereby lowering blood PTH levels, by acting directly on parathyroid cell membrane calcium-sensing receptors. Upacicalcet can be used for researching the disease of secondary hyperparathyroidism (SHPT)[1].
  • HY-122819
    Calindol hydrochloride Agonist 99.88%
    Calindol hydrochloride is a positive allosteric modulator (PAM) of calcimimetic calcium-sensing receptor (CaSR) with an EC50 of 132 nM[1].
  • HY-109106
    Upacicalcet
    Upacicalcet is an intravenous calcimimetic agent. Upacicalcet suppresses excessive parathyroid hormone (PTH) secretion, thereby lowering blood PTH levels, by acting directly on parathyroid cell membrane calcium-sensing receptors. Upacicalcet can be used for researching the disease of secondary hyperparathyroidism (SHPT)[1].