A potent and selective antagonist of CaSR (IC50 = 43 nM) that stimulates PTH secretion from parathyroid cells in vitro (EC50 = 39 nM); causes a sustained increase in plasma PTH in rats when given intravenously

NPS 2143 (hydrochloride) – 1 mg

Brand:
Cayman
CAS:
324523-20-8
Storage:
-20
UN-No:
De Minimis - 3077 / 9

Calcium-sensing receptor (CaSR) is a G protein-coupled receptor that is involved in calcium homeostasis.{29237,26276} Activation of CaSR on parathyroid cells decreases the secretion of parathyroid hormone (PTH), which in turn reduces blood calcium concentration.{29237,26276} NPS 2143 is a potent and selective antagonist of CaSR (IC50 = 43 nM) that stimulates PTH secretion from parathyroid cells in vitro (EC50 = 39 nM).{29235,29236} It is effective in vivo, causing a sustained increase in plasma PTH in rats when given intravenously.{29235,29236} Daily oral administration of NPS 2143 to osteopenic ovariectomized rats results in a dramatic increase in bone turnover, as well as increased circulating PTH levels.{29235}  

 

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Description

A potent and selective antagonist of CaSR (IC50 = 43 nM) that stimulates PTH secretion from parathyroid cells in vitro (EC50 = 39 nM); causes a sustained increase in plasma PTH in rats when given intravenously

Formal name: 2-chloro-6-[(2R)-3-[[1,1-dimethyl-2-(2-naphthalenyl)ethyl]amino]-2-hydroxypropoxy]-benzonitrile, monohydrochloride

Synonyms:  SB-262470A

Molecular weight: 445.4

CAS: 324523-20-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Endocrinology & Metabolism|Bone Growth & Remodeling

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