78 products were found matching "K04612"!

A CaSR antagonist (IC50 = 0.012 µM in a reporter assay using PC12h cells), increases plasma levels of parathyroid hormone, prevents renal calcification, and increases bone mineral density in an ADH model using CaSR knock-in mice. SMILES:...

Recombinant CHO-K1 cells stably overexpress human calcium sensing receptor (CASR) on the surface and contain high levels of G protein Galphaq to couple with the receptor in downstream signaling pathways.

Etelcalcetide is a peptide agonist of the calcium-sensing receptor (CaSR). It is selective for CaSR over a panel of 33 receptors and ion channels, as well as the norepinephrine transporter at 10 µM. Etelcalcetide increases intracellular calcium levels in HEK293T cells expressing the human CaSR receptor with an EC50...

Cinacalcet is a calcimimetic and an allosteric agonist of the calcium-sensing receptor (CaSR, EC50 = 79.4 nM in HEK293T cells expressing the human receptor). In vivo, cinacalcet (0.1-10 mg/kg, s.c.) decreases plasma levels of parathyroid hormone (PTH) in rats. It also decreases plasma levels of PTH and parathyroid...

Calindol is a phenylalkylamine calcimimetic that facilitates the activation of the calcium-sensing receptor (CaSR), a G protein-coupled receptor that triggers phosphatidylinositol (PI)-intracellular calcium signaling and, in some cell types, cell proliferation. It potently stimulates PI hydrolysis and proliferation...

Calcium-sensing receptor (CaSR) is a G protein-coupled receptor that is involved in calcium homeostasis. Activation of CaSR on parathyroid cells decreases the secretion of parathyroid hormone (PTH), which in turn reduces blood calcium concentration. NPS 2143 is a potent and selective antagonist of CaSR (IC50 = 43...

R-568 is a calcimimetic and positive allosteric modulator of the calcium-sensing receptor (CaSR). It potentiates extracellular calcium-induced increases in intracellular calcium release and inhibits the secretion of parathyroid hormone (PTH, IC50 = 27 nM) in bovine parathyroid cells. R-568 decreases PTH and plasma...

Description: Cinacalcet (AMG 073) is an orally active, allosteric Ca receptor (CaR) agonist used in the treatment of cardiovascular disease. Target: CaSR. Smiles: [C@@H](NCCCC1=CC(C(F)(F)F)=CC=C1)(C)C=2C3=C(C=CC2)C=CC=C3. References: D.A. Bushinsky, et al. Effect of cinacalcet on urine calcium excretion and...

Anti-CASR antibody was affinity purified from monospecific antiserum by immunoaffinity chromatography. CASR antibody is human, mouse and rat reactive. At least two isoforms of CASR are known to exist. Protein function: Senses changes in the extracellular concentration of calcium ions. The activity of this receptor...

Ca2+-sensing receptor agonist.