Signaling Pathway

CaSR

CaSR

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CaSR (The 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 Inhibitors & Modulators (6)

Product Name Catalog No. Brief Description
Calcium-Sensing Receptor Antagonists I

HY-50713

Calcium-Sensing Receptor Antagonists I is an antagonist of calcium-sensing parathyroid hormone receptors.

Cinacalcet

HY-70037

Cinacalcet(AMG-073) is an orally active, second-generation calcimimetic compound; AMG 073 represents a new class of compounds for the treatment of hyperparathyroidism.

Cinacalcet hydrochloride

HY-70037A

Cinacalcet Hcl (AMG-073) is an orally active, second-generation calcimimetic compound; AMG 073 represents a new class of compounds for the treatment of hyperparathyroidism.

NPS-2143

HY-10007

NPS-2143(SB 262470A ) is a selective potent calcium ion-sensing receptor antagonist with IC50 of 43 and 41 nM for cytoplasmic Ca2+ concentrations and parathyroid hormone secretion, respectively.

NPS-2143 hydrochloride

HY-10171

NPS-2143(SB 262470A ) is a selective potent calcium ion-sensing receptor antagonist with IC50 of 43 and 41 nM for cytoplasmic Ca2+ concentrations and parathyroid hormone secretion, respectively.

Strontium Ranelate

HY-17397

Strontium ranelate(S12911) stimulates the calcium sensing receptors (CaSR) and leads to the differentiation of pre-osteoblast to osteoblast which increases the bone formation.