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Upacicalcet

CAT: 0804-HY-109106Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-109106Size:1 Each
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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 -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].
CAS Number
1333218-50-0
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