787584-62-7
Chemical Structure
Encaleret sodium
Synonym(s): CLTX-305 sodium; JTT-305 sodium; MK-5442 sodium
- CAS No.: 787584-62-7
- Formula:C29H32ClFNNaO4
- Molecular Weight:536.01
InChIKey: PEFWOLTYQNICOP-JENXBZAWSA-M
SMILES: FC(C=C1CC(C)(C)NC[C@@H](O)CO[C@@H](C2=C(C3=CC(C)=C(C=C3)C(O[Na])=O)C=CC=C2)C)=C(C=C1)Cl
Biological Activity: Encaleret (CLTX-305) sodium is an orally active antagonist of the calcium-sensing receptor (CaSR), with an IC50 of 12 nM. Encaleret sodium exerts its effect by inhibiting the excessive activity of functional gain-of-function CaSR variants, and can restore blood calcium levels, promote the secretion of parathyroid hormone, improve magnesium and phosphorus metabolism, and increase urinary calcium excretion. Encaleret sodium can be used in the research of diseases such as osteoporosis and autosomal dominant hypocalcemia type 1[1][2].
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Encaleret sodium | Encaleret (CLTX-305) sodium is an orally active antagonist of the calcium-sensing receptor (CaSR), with an IC50 of 12 nM. Encaleret sodium exerts its effect by inhibiting the excessive activity of functional gain-of-function CaSR variants, and can restore blood calcium levels, promote the secretion of parathyroid hormone, improve magnesium and phosphorus metabolism, and increase urinary calcium excretion. Encaleret sodium can be used in the research of diseases such as osteoporosis and autosomal dominant hypocalcemia type 1. | |||||||||||||||||||||
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- [1]. Shinagawa Y, et al. Discovery of a potent and short-acting oral calcilytic with a pulsatile secretion of parathyroid hormone. ACS Med Chem Lett. 2010 Dec 29;2(3):238-42. [Content Brief]
- [2]. Gafni RI, et al. Efficacy and Safety of Encaleret in Autosomal Dominant Hypocalcemia Type 1. N Engl J Med. 2023 Sep 28;389(13):1245-1247. [Content Brief]
Keywords
