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


CaSR (calcium-sensing receptor) is a Class C G-protein coupled receptor which senses extracellular levels of calcium ion. In theparathyroid gland, the calcium-sensing receptor controls calcium homeostasis by regulating the release of parathyroid hormone (PTH). The release of PTH is inhibited in response to elevations in plasma calcium concentrations and activation of the calcium receptor. Increased calcium binding on the extracellular side gives a conformational change in the receptor, which, on the intracellular side, initiates the phospholipase C pathway, presumably through a Gqα type of G protein, which ultimately increases intracellular concentration of calcium, which inhibits vesicle fusion and exocytosis of parathyroid hormone. It also inhibits the cAMP dependent pathway.

CaSR 相关产品 (11):

Cat. No. Product Name Effect Purity
  • HY-10007
    NPS-2143 Antagonist 99.34%
    NPS-2143 (SB-262470A),口服活性溶钙剂, 是选择性的钙敏感受体 (CaSR) 拮抗剂。NPS-2143 (SB-262470A) 通过激活表达人 Ca2+ 受体的 HEK 293 细胞中的 Ca2+ 受体而引起的胞浆 Ca2+ 浓度增加 (IC50=43 nM)。
  • HY-70037
    Cinacalcet Agonist 99.94%
    Cinacalcet (AMG 073) 是一种可口服的 Ca receptor (CaR) 激动剂,用于心血管疾病研究。
  • HY-17613
    Evocalcet Activator 99.05%
    Evocalcet 对钙敏感受体 (CaSR) 具有激活作用来自专利 WO 2017061621 A1,化合物 A。
  • HY-70037A
    Cinacalcet hydrochloride Agonist 99.96%
    Cinacalcet hydrochloride (AMG 073 hydrochloride) 是一种可口服的 Ca receptor (CaR) 激动剂,用于心血管疾病研究。
  • HY-P1955A
    Etelcalcetide hydrochloride Activator 98.85%
    Etelcalcetide hydrochloride (AMG 416 hydrochloride) 是一种合成肽,有钙敏感受体 (CaSR) 活化剂的作用。Etelcalcetide hydrochloride 可有效降低接受血液透析的继发性甲状旁腺功能亢进患者的甲状旁腺激素 (PTH) 浓度。
  • HY-10167A
    Tecalcet Hydrochloride Modulator 99.66%
    Tecalcet Hydrochloride (R 568 Hydrochloride) 是一个口服有效的拟钙剂,变构正调控钙敏感受体 (CaSR)。Tecalcet Hydrochloride (R 568 Hydrochloride) 可提高激活细胞外Ca2+的敏感性。
  • HY-10171
    NPS-2143 hydrochloride Antagonist 99.94%
    NPS-2143 hydrochloride (SB-262470A hydrochloride),口服活性溶钙剂,是选择性的钙敏感受体 (CaSR) 拮抗剂。NPS-2143 hydrochloride (SB-262470A hydrochloride) 通过激活表达人 Ca2+ 受体的 HEK 293 细胞中的 Ca2+ 受体而引起的胞浆 Ca2+ 浓度增加 (IC50=43 nM)。
  • HY-N0546
    Ligustroflavone Antagonist 99.41%
    Ligustroflavone 可从Ligustrum lucidum 中提取得到,是一种潜在的钙敏感受体(CaSR) 拮抗剂。Ligustroflavone对糖尿病性骨质疏松症小鼠有保护作用。
  • HY-17397
    Strontium Ranelate Activator 99.16%
    Strontium Ranelate (S12911) 是一种抗骨质疏松药物,其作用是通过减少骨吸收并促进骨形成,从而诱导正骨平衡。Strontium Ranelate 还可以激活非骨骼细胞中的钙敏感受体 (CaSR),从而导致肌醇 1、4、5-三磷酸生成和丝裂原活化的蛋白激酶信号转导。
  • HY-103320A
    Calhex 231 hydrochloride Inhibitor >98.0%
    Calhex 231 hydrochloride 是一种通过负变构调节来抑制 CaSR 的。Calhex 231 hydrochloride 在 HEK293 细胞中阻断 Ca2+ 诱导的肌醇磷酸酯的积累,IC50 为 0.39 μM。Calhex 231 hydrochloride 可用于糖尿病性心肌病 (DCM) 的研究。
  • HY-50713
    Calcium-Sensing Receptor Antagonists I Antagonist 99.91%
    Calcium-Sensing Receptor Antagonists I是钙离子敏感的甲状旁腺素受体拮抗剂。
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