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 (52):

Cat. No. Product Name Effect Purity
  • HY-70037
    Cinacalcet Agonist 99.93%
    Cinacalcet (AMG 073) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease research.
  • HY-10007
    NPS-2143 Antagonist 99.94%
    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 99.98%
    Cinacalcet hydrochloride (AMG-073 hydrochloride) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.
  • HY-139201A
    Poly-D-lysine hydrobromide (MW 70000-150000) Agonist
    Poly-D-lysine hydrobromide (MW 70000-150000) is a synthetic polymeric substrate and is one of the most widely used substrate in neural cell culture. Poly-D-lysine hydrobromide is a CaSR agonist peptide[1][2].
  • HY-P1955A
    Etelcalcetide hydrochloride Activator 99.61%
    Etelcalcetide hydrochloride (AMG 416 hydrochloride; KAI-4169 hydrochloride) is a synthetic calcimimetic 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, which is promising for research in the field of secondary hyperparathyroidism and chronic kidney disease[1][2].
  • HY-139201E
    Poly-D-lysine hydrobromide (MW 150000-300000)
    Poly-D-lysine hydrobromide (PDLHB) (MW 150000-300000) is a synthetic polymeric substrate and is one of the most widely used substrate in neural cell culture. Poly-D-lysine hydrobromide is a CaSR agonist peptide[1].
  • HY-171446
    TAK-075 Antagonist
    TAK-075 is an orally active CaSR antagonist with an IC50 value of 0.94 nM. TAK-075 can stimulate the transient secretion of parathyroid hormone (PTH) in rats and can effectively prevent a significant reduction in PTH secretion caused by the accumulation of active metabolites, maintaining the normal secretion pattern of PTH. TAK-075 can be used in the research of metabolic diseases and osteoporosis[1].
  • HY-139201H
    Poly-D-lysine hydrobromide (MW ≥300000)
    Poly-D-lysine hydrobromide (PDLHB) (MW ≥300000) is a synthetic polymeric substrate and is one of the most widely used substrate in neural cell culture. Poly-D-lysine hydrobromide is a CaSR agonist peptide[1].
  • HY-17613S
    Evocalcet-d4 Activator
    Evocalcet-d4 (KHK7580-d4) is deuterium labeled Evocalcet. 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-121584
    Lycoperodine-1 Agonist 99.82%
    Lycoperodine-1 (Cyclomethyltryptophan) is an active product that can be isolated from tomato fruits (Lycopersicon sculentum). Lycoperodine-1 act as an agonist of Ca2+ sensing receptors (CaSR)[1].
  • HY-N0546R
    Ligustroflavone (Standard) Antagonist
    Ligustroflavone (Standard) is the analytical standard of Ligustroflavone. This product is intended for research and analytical applications. Ligustroflavone, extracted from Ligustrum lucidum, is a potential candidate as calcium-sensing receptor (CaSR) antagonist. Ligustroflavone exhibits protective effects against diabetic osteoporosis in mice[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-P4376A
    Gamma-Glu-Abu TFA Agonist
    Gamma-Glu-Abu TFA is the TFA salt form of Gamma-Glu-Abu (HY-P4376). Gamma-Glu-Abu TFA is an agonist for calcium sensing receptor (CaSR), that activates the CaSR with an EC50 of 0.21 μM in HEK-293 cell[1].
  • 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+[1][2][3].
  • HY-103320B
    (1R,2R)-Calhex 231 hydrochloride Control 99.07%
    (1R,2R)-Calhex 231 hydrochloride is the isomer of Calhex 231 hydrochloride (HY-103320A), and can be used as an experimental control. 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[1][2].
  • HY-15105A
    SB-423562 hydrochloride Antagonist
    SB-423562 hydrochloride is a short-acting calcium-sensing receptor (CaR) antagonist. SB-423562 hydrochloride has the potential for osteoporosis research.
  • 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].