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

CaSR (钙敏感受体)

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 相关产品 (10):

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-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-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-17397
    Strontium Ranelate Activator 99.93%
    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-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-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。
  • HY-107773
    GSK3004774 Agonist
    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。
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