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  1. GPCR/G Protein
  2. CaSR

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 (9):

Cat. No.Product NameEffectPurity
  • HY-10007
    NPS-2143Inhibitor 99.42%
    NPS-2143是选择性的钙敏感受体 (CaSR)拮抗剂,IC50 为 43 nM。
  • HY-70037
    CinacalcetAgonist 99.65%
    Cinacalcet 是一种可口服的 Ca receptor (CaR) 激动剂,用于治疗心血管疾病。
  • HY-70037A
    Cinacalcet hydrochlorideAgonist 99.98%
    Cinacalcet hydrochloride 是一种可口服的 Ca receptor (CaR) 激动剂,用于治疗心血管疾病。
  • HY-10171
    NPS-2143 hydrochlorideAntagonist 99.96%
    NPS-2143(SB 262470A)是选择性的Ca(2+)受体拮抗剂,IC50为43 nM。
  • HY-17613
    EvocalcetActivator 98.52%
    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-107773
    GSK3004774Agonist
    GSK3004774 是一种有效的、不能吸收的 CaSR 激动剂,对人、小鼠和大鼠 CaSR 的 pEC50 值分别为 7.3,6.6 和 6.5, 对人 CaSR 的 EC50 值为 50 nM。
  • HY-17397
    Strontium RanelateActivator 99.16%
    Strontium ranelate(S12911)能刺激钙敏受体(CaSR),促进前成骨细胞向成骨细胞分化。
  • HY-50713
    Calcium-Sensing Receptor Antagonists IAntagonist 99.02%
    Calcium-Sensing Receptor Antagonists I是钙离子敏感的甲状旁腺素受体拮抗剂。
  • HY-15105
    SB-423562Antagonist
    SB-423562 是一种短效的 (CaR) 拮抗剂。
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