Upacicalcet

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]. IC50 & Target:calcium-sensing receptors^[1] In Vitro:Upacicalcet (0.0001-10 μM) sodium increases the intracellular Ca²⁺ and IP-1 (EC₅₀ = 26.1 nM) in the presence of 1.2mM Ca²⁺ in human CaSR-expressing HEK293T (CaSR-HEK) cells^[1]. In Vivo:Upacicalcet (0.3-30 mg/kg, i.v.; s.c., once) sodium reduces serum iPTH, Ca²⁺, and Pi levels, does not affect gastric emptying in male SD rats and double-nephrectomized SD rats^[1].
Upacicalcet (0.2-1 mg/kg, i.v., three times a week for 3 weeks) sodium reduces serum iPTH levels and inhibits parathyroid hyperplasia in Adenine- induced CKD SD rats model^[2].
Upacicalcet (1 mg/kg, s.c., once a day, 28 days) sodium reduces serum iPTH levels and inhibits ectopic calcification and cortical hole formation in Adenine- induced CKD Wistar rats model^[2].