Calcium-Sensing Receptor

Calcium-sensing receptor (CaSR) ligands act on the receptor that detects extracellular calcium levels. CaSR was cloned from bovine parathyroid and is a class C G protein-coupled receptor that controls parathyroid hormone secretion. Inactivating mutations in its gene cause familial hypocalciuric hypercalcemia and neonatal severe hyperparathyroidism. Calcimimetics are positive modulators that increase the receptor's sensitivity to calcium; examples here are cinacalcet, evocalcet and tecalcet hydrochloride. Calcilytics such as NPS-2143 and SB-423557 act in the opposite way and are used to study parathyroid and kidney calcium handling.

3 Items

  • Calhex 231 hydrochloride
    Cat. No.
    A24306

    Calhex 231 hydrochloride

    Calhex 231 hydrochloride is a potent negative allosteric modulator of the calcium-sensing receptor (CaSR), with an IC50 of 0.39 μM for inhibiting \[³H]inositol phosphate accumulation induced by CaSR activation. It transiently blocks signaling through the human wild-type CaSR and is utilized in research related to traumatic hemorrhagic shock (THS) and diabetic cardiomyopathy (DCM), where dysregulated calcium signaling contributes to disease pathology.

    5 mg
    $90.00
    10 mg
    $155.00
    All 4 sizes
  • AXT-914
    Cat. No.
    A53360

    AXT-914

    AXT-914 is an inhibitor of the calcium-sensing receptor (CaSR), primarily engaged in modulating calcium signaling pathways. This compound exhibits antiviral activity against coronaviruses, including HCoV 229E and SARS-CoV-2, while also reducing cytosolic calcium signaling linked to CaSR mutations. AXT-914 is applicable in research focused on Bartter syndrome type 5, autosomal dominant hypocalcemia (ADH), and coronavirus infections.

    5 mg
    $345.00
    10 mg
    $565.00
    All 5 sizes
  • Calhex 231
    Cat. No.
    A59494

    Calhex 231

    Calhex 231 is a potent negative allosteric modulator targeting the calcium-sensing receptor (CaSR), exhibiting an IC50 of 0.39 μM for inhibiting increases in [3H]inositol phosphates. This compound is instrumental in research applications related to traumatic hemorrhagic shock and diabetic cardiomyopathy, providing insights into the roles of CaSR in these pathophysiological conditions. Calhex 231 offers a valuable tool for investigating the modulation of CaSR signaling pathways.

    1 mg
    $125.00
    5 mg
    $325.00
    All 2 sizes

3 Items

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