1333218-50-0
Chemical Structure
Upacicalcet
Synonym(s): SK-1403 free acid; AJT240 free acid; PLS240 free acid
- CAS No.: 1333218-50-0
- Formula:C11H14ClN3O6S
- Molecular Weight:351.76
IUPAC Name: (S)-2-amino-3-(3-(3-chloro-2-methyl-5-sulfophenyl)ureido)propanoic acid
InChIKey: LHEYGVSDVBEYQF-QMMMGPOBSA-N
SMILES: O=C(NC[C@H](N)C(O)=O)NC1=CC(S(=O)(O)=O)=CC(Cl)=C1C
Biological Activity: 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].
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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. | |||||||||||||||||||||
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- [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. [Content Brief]
- [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. [Content Brief]
Keywords
