Upacicalcet

• Description :

  Upacicalcet is a non-peptide calcimimetic that acts as a CaSR agonist (EC50 = 10.8 nM) . Upacicalcet reduces serum intact parathyroid hormone (iPTH) and serum Ca2+ levels, reducing hypocalcemia and gastrointestinal complications. Upacicalcet improves vascular calcification and bone disorders in the Adenine (HY-B0152) -induced secondary hyperparathyroidism (SHPT) rat model. Upacicalcet inhibits cortical pore formation and reduces bone fibrosis in rats with chronic kidney disease (CKD) . Upacicalcet is useful for studying SHPT[1][2].

• Product Name Alternative :

  SK-1403 (free acid) ; AJT240 (free acid) ; PLS240 (free acid)

• UNSPSC :

  12352005

• Target :

  CaSR

• Type :

  Reference compound

• Related Pathways :

  GPCR/G Protein

• Applications :

  Metabolism-protein/nucleotide metabolism

• Field of Research :

  Endocrinology

• Assay Protocol :

  https://www.medchemexpress.com/upacicalcet.html

• Solubility :

  10 mM in DMSO

• Smiles :

  O=C(NC[C@H](N)C(O)=O)NC1=CC(S(=O)(O)=O)=CC(Cl)=C1C

• Molecular Formula :

  C11H14ClN3O6S

• Molecular Weight :

  351.76

• References & Citations :

  [1]Goto M, et al. Pharmacological profile of upacicalcet, a novel positive allosteric modulator of calcium-sensing receptor, in vitro and in vivo. Eur J Pharmacol. 2023 Oct 5;956:175936.|[2]Sato H, et al. Upacicalcet, a positive allosteric modulator of the calcium-sensing receptor, prevents vascular calcification and bone disorder in a rat adenine-induced secondary hyperparathyroidism model. Bone. 2023 Feb;167:116613.

• Shipping Conditions :

  Room temperature

• Scientific Category :

  Reference compound1

• Clinical Information :

  Launched

• CAS Number :

  [1333218-50-0]